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Leishmaniases comprise a group of infectious parasitic diseases caused by various species of Leishmania and are considered a significant public health problem worldwide. Only a few medications, including miltefosine, amphotericin B, and meglumine antimonate, are used in current therapy. These medications are associated with severe side effects, low efficacy, high cost, and the need for hospital support. Additionally, there have been occurrences of drug resistance. Additionally, only a limited number of drugs, such as meglumine antimonate, amphotericin B, and miltefosine, are available, all of which are associated with severe side effects. In this context, the need for new effective drugs with fewer adverse effects is evident. Therefore, this study investigated the anti-Leishmania activity of a dichloromethane fraction (DCMF) extracted from Arrabidaea brachypoda roots. This fraction inhibited the viability of L. infantum, L. braziliensis, and L. Mexicana promastigotes, with IC 50 values of 10.13, 11.44, and 11.16 µg/mL, respectively, and against L. infantum amastigotes (IC 50 = 4.81 µg/mL). Moreover, the DCMF exhibited moderate cytotoxicity (CC 50 = 25.15) towards RAW264.7 macrophages, with a selectivity index (SI) of 5.2. Notably, the DCMF caused damage to the macrophage genome only at 40 µg/mL, which is greater than the IC 50 found for all Leishmania species. The results suggest that DCMF demonstrates similar antileishmanial effectiveness to isolated brachydin B, without causing genotoxic effects on mammalian cells. This finding is crucial because the isolation of the compounds relies on several steps and is very costly while obtaining the DCMF fraction is a simple and cost-effective process. Furthermore, In addition, the potential mechanisms of action of brachydins were also investigated. The computational analysis indicates that brachydin compounds bind to the Triosephosphate isomerase (TIM) enzyme via two main mechanisms: destabilizing the interface between the homodimers and interacting with catalytic residues situated at the site of binding. Based on all the results, DCMF exhibits promise as a therapeutic agent for leishmaniasis due to its significantly reduced toxicity in comparison to the adverse effects associated with current reference treatments., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

This study carried out to investigate the anti-inflammatory and antinociceptive effect of tropane alkaloid (EB7) isolated from E. bezerrae. It evaluated the toxicity and possible involvement of ion channels in the antinociceptive effect of EB7, as well as its anti-inflammatory effect in adult zebrafish (Zfa). Docking studies with EB7 and COX-1 and 2 were also performed. The tested doses of EB7 (4, 20 and 40 mg/kg) did not show any toxic effect on Zfa during the 96h of analysis (LD50>40 mg/kg). They did not produce any alteration in the locomotor behavior of the animals. Furthermore, EB7 showed promising pharmacological effects as it prevented the nociceptive behavior induced by hypertonic saline, capsaicin, formalin and acid saline. EB7 had its analgesic effect blocked by amiloride involving the neuromodulation of ASICs in Zfa. In evaluating the anti-inflammatory activity, the edema induced by κ-carrageenan 3.5 % was reduced by the dose of 40 mg/kg of EB7 observed after the fourth hour of analysis, indicating an effect similar to that of ibuprofen. Molecular docking results indicated that EB7 exhibited better affinity energy when compared to ibuprofen control against the two evaluated targets binding at different sites in the cocrystallized COX-1 and 2 inhibitors., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.)

Flavonoids are secondary metabolites that are widely found in various medicinal plants. They are known for their medicinal benefits and have been extensively used in healthcare industries and in the management of age-related diseases. This paper focuses on flavonoids from Oroxylum indicum , a significant medicinal tree in the practice of traditional Indian medicine. O. indicum has been utilized in a variety of polyherbal formulations for the management of musculoskeletal disorders, however the mechanism of action of its bioactive flavonoids remains unknown. The present study aimed to identify the flavonoids of O. indicum with the potential to target sclerostin, an antagonist of canonical Wnt signaling pathway for the treatment of bone-related disorders. Molecular docking, coarse-grained and molecular dynamics simulations were performed to screen the major flavonoids and investigate their interaction with sclerostin. Flavonoids with highest binding affinity and interacting with at least one of the amino acids of the PNAIG motif residues were selected from docking studies and subjected to further drug likeness and ADMET screening. Further screening from coarse-grained and molecular dynamic simulations results showed that baicalein, compared to other screened flavonoids, stably binds with the important residues of the LRP6 binding site of sclerostin, resulting in pronounced structural changes in the protein. These findings suggest that baicalein from O. indicum can potentially inhibit sclerostin and can elicit skeletal protective effects, providing an insight for further in vitro and in vivo studies.Communicated by Ramaswamy H. Sarma.

E6 and E7 human papillomavirus (HPV) oncoproteins play a significant role in the malignant transformation of infected cervical cancer cells via suppression of tumour suppressor pathways by targeting p53 and pRb, respectively. This study aimed to investigate the anticancer effects of Oroxylum indicum (OI) leaves' methanol extract on SiHa cervical cancer cells. Expression of apoptosis-related proteins (Bcl-2, caspase (cas)-3, and cas-9), viral oncoproteins (E6 and E7), and tumour suppressor proteins (p53 and pRb) were evaluated using western blot analysis before and after E6/E7 small interfering RNAs (siRNAs) transfection. In addition, the E6/E7 mRNA expression levels were assessed with real-time (RT)-PCR. The present study showed that the OI extract effectively hindered the proliferation of SiHa cells and instigated increments of cas-3 and cas-9 expressions but decreased the Bcl-2 expressions. The OI extract inhibited E6/E7 viral oncoproteins, leading to upregulation of p53 and pRb tumour suppressor genes in SiHa cells. Additionally, combinatorial treatment of OI extract and gossypin flavonoid induced restorations of p53 and pRb. Treatment with OI extract in siRNA-transfected cells also further suppressed E6/E7 expression levels and further upregulations of p53 and pRb proteins. In conclusion, OI extract treatment on siRNAs-transfected SiHa cells can additively and effectively block E6- and E7-dependent p53 and pRb degradations. All these data suggest that OI could be explored for its chemotherapeutic potential in cervical cancer cells with HPV-integrated genomes., (© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.)

The brain-derived neurotrophic factor (BDNF) plays a crucial role during neuronal development as well as during differentiation and synaptogenesis. They are important proteins present in the brain that support neuronal health and protect the neurons from detrimental signals. The results from the present study suggest BDNF expression can be increase up to ~8-fold by treating the neuroblastoma cells SHSY-5Y with an herbal extract of Oroxylum indicum (50 μg/mL) and ~5.5-fold under lipopolysaccharides (LPS)-induced inflammation conditions. The Oroxylum indicum extract (Sabroxy) was standardized to 10% oroxylin A, 6% chrysin, and 15% baicalein. In addition, Sabroxy has shown to possess antioxidant activity that could decrease the damage caused by the exacerbation of radicals during neurodegeneration. A mode of action of over expression of BDNF with and without inflammation is proposed for the Oroxylum indicum extract, where the three major hydroxyflavones exert their effects through additive or synergistic effects via five possible targets including GABA, Adenoside A2A and estrogen receptor bindings, anti-inflammatory effects, and reduced mitochondrial ROS production.

One new iridoid named aureanin ( 1 ) was isolated from the leaves of Tabebuia aurea (Silva Manso) Benth. & Hook.f. ex S.Moore, together with eight known compounds, isoquercetin ( 2 ), astragalin ( 3 ), callicoside B ( 4 ), amphipaniculoside E ( 5 ), rehmaglutin D ( 6 ), quercetin-3-sambubioside ( 7 ), rutin ( 8 ), kaempferol-3- O -rutinoside ( 9 ). The structures of the isolated compounds were elucidated and confirmed by spectroscopic methods, including 1 D and 2 D NMR experiments, as well as HR-ESI-MS. Compounds 1-9 were evaluated for their in vitro cytotoxic activity against three human cancer cell lines (A549, HepG2, and MCF-7) and Leishmania major . Compound 4 showed activity against A549 (IC 50 : 36.8 ± 1.5 μg/mL, etoposide (positive control): 28.1 ± 4.2 μg/mL), however, none of the compounds were active against L. major .

Phytochemical investigation of Bignonia binata leaves led to the isolation of three new compounds: including a glycoside of simple alcohol, namely binatoside ( 2 ), 3,4-dihydroxy- N -methyl piperidin-2-one ( 7 ), and a phenyl ethanoid glycoside, namely bignanoside C ( 8 ), alongside with five known compounds; including a glycoside of simple alcohol; (2 S ) propane-1,2-diol 1- O -(6- O -caffeoy1)- β -D-glucopyranoside ( 1 ), phenyl ethanoids; leucosceptoside A ( 3 ) and plantainoside C ( 4 ), and iridoids; ipolamiide ( 5 ) and strictoloside ( 6 ). The structure of the isolated compounds was elucidated by various spectroscopic methods, including 1 D and 2 D NMR experiments, HR-ESI-MS as well as by comparison with the literature.

Flavones are major compounds found in several parts of Oroxylum indicum ( O. indicum ). The quantification of multiple components by one marker (QAMS) method and the high-performance liquid chromatography (HPLC) method were developed for the quantitative analysis of extracts from the young fruits, green mature fruits, dry pod coats and seeds of O. indicum . Oroxin A, oroxin B and chrysin-7- O -glucuronide were identified in the O. indicum extracts. Oroxylin A and 5-hydroxymethylfurfural were isolated and structurally identified from the pod coat and young fruit extracts, respectively. From the HPLC analysis of the seven major flavones in the extracts, baicalin was the major compound in all extracts investigated (0.4-11% w / w of the extract). All flavone contents were low in the young fruit extract (<1% w / w of the extract). The green mature fruit and dry pod coat extracts showed similar constituent compositions. They contained small amounts of baicalin and oroxylin A, which were found only in these two extracts. Oroxylin A could be used as a marker to indicate the maturity of O. indicum fruits, while 5-hydroxymethylfurfural could be used as a marker for the young fruits. Baicalin was found to be a suitable single marker to calculate the contents of all flavones in the O. indicum extracts.

Six new iridoid derivatives (1-6)，together with twelve known compounds (7-18), were isolated and identified from the dried fruits of Catalpa ovata G. Don. Their chemical structures were mainly established through the relative spectroscopic data, while the absolute configurations of compounds 2 and 3 were elucidated on the electronic circular dichroism calculations. Their antioxidant activities were evaluated by activating the Nrf2 transcriptional pathway in 293 T cells in vitro. Among them, Compounds 1, 3, 4, 6-8, 10-12, 14, 15, 17 and 18 showed significant Nrf2 agonistic effect compared with the control group at 25 μM. Finally, The hypothetical biosynthetic pathway for 1-13 was discussed., Competing Interests: Declaration of Competing Interest The authors declare no conflict of interest., (Copyright © 2023 Elsevier B.V. All rights reserved.)

This study was designed to appraise the antioxidant and anticancer competence of solvent extracts of Tecoma stans (Linn) and analyze the phytoligands interaction against Bcl 2 VEGFR2 through in silico studies. The phytochemical analysis revealed that the ethyl acetate extract contains more number of pharmaceutically valuable phytochemicals than other solvent extracts. Among the various phytochemicals, flavonoid was found as a predominant component, and UV-Vis- spectrophotometer analysis initially confirmed it. Hence, the column chromatogram was performed to purify the flavonoid, and High-performance liquid chromatography (HPLC) was performed. It revealed that the flavonoid enriched fraction by compared with standard flavonoid molecules. About 84.69% and 80.43% of antioxidant activity were found from ethyl acetate extract of bark and flower at the dosage of 80 μg mL -1 with the IC 50 value of 47.24 and 43.40 μg mL -1, respectively. In a dose-dependent mode, the ethyl acetate extract of bark and flower showed cytotoxicity against breast cancer cell line MCF 7 (Michigan Cancer Foundation-7) as up to 81.38% and 80.94% of cytotoxicity respectively. Furthermore, the IC 50 was found as 208.507 μg mL -1 and 207.38 μg mL -1 for bark and flower extract correspondingly. About 10 medicinal valued flavonoid components were identified from bark (6) and flower (4) ethyl acetate extract through LC-MS analysis. Out of 10 components, the 3,5-O-dicaffeoylquinic acid (ΔG -8.8) and Isorhamnetin-3-O-rutinoside (ΔG -8.3) had the competence to interact with Bcl 2 (B-Cell Lymphoma 2) and VEGFR2 (Vascular Endothelial Growth Factor Receptor 2) respectively with more energy. Hence, these results confirm that the ethyl acetate extract of bark and flower of T. stans has significant medicinal potential and could be used as antioxidant and anticancer agent after some animal performance study., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Inc. All rights reserved.)

Objective: Kigelia africana (Lam.) Benth. (Bignoniaceae) syn. Kigelia pinnata (Jacq. DC) is a tropical plant that is native to tropical Africa. The aim of this study was to determine if a methanolic extract prepared from Kigelia africana (KAE) can promote wound healing in treated human normal epidermal keratinocyte (HaCaT) cells and human normal foreskin fibroblast cell line (BJ) cells compared with untreated cells., Method: Experimental steps included: the methanolic extraction of the leaf and fruit of the Kigelia africana plant; the preparation of HaCaT and BJ cell lines; cell culture with a stable tetrazolium salt-based proliferation assay; and the evaluation of the wound healing effect of KAE (2μg/ml) in BJ and HaCaT cells. The phytochemical contents of KAE were determined using liquid chromatography quadrupole time-of-flight mass spectrometry., Results: The following molecules were identified as being present in the KAE, among others: cholesterol sulfate; lignoceric acid; embelin; isostearic acid; linoleic acid; dioctyl phthalate; arg-pro-thr; 15-methyl-15(S)-PGE1; sucrose; benzododecinium (Ajatin); and 9-Octadecenamide (oleamide). KAE effected faster wound healing in treated cells compared with untreated cells for both cell lines. HaCaT cells that had been mechanically injured and treated with KAE healed completely in 48 hours compared with 72 hours for untreated HaCaT cells. Treated BJ cells healed completely in 72 hours compared with 96 hours for untreated BJ cells. Concentrations of KAE up to 300μg/ml had a very low cytotoxic effect on treated BJ and HaCaT cells., Conclusion: The experimental data in this study support the potential of KAE-based wound healing treatment to accelerate wound healing.

Tecoma stans (L.), popularly known as ipê-mirim, is used in traditional medicine for the treatment of diabetes and digestive problems. The components of the hexane (HE) and methanol (ME) extracts obtained from the pericarp of T . stans were identified by gas chromatography-mass spectrometry (GC-MS) in their methyl ester forms (FAME). The antioxidant and cytotoxic activities of extracts, fatty acids, and methyl esters were evaluated. Methyl linolenate, methyl linoleate, and methyl palmitate were the major compounds in the HE, while methyl hexacosanoate was the main component in the ME. The samples exhibited significant antioxidant potential by DPPH assay. In the Artemia salina larvae bioassay, FAME (HE) and FAME (ME) were considered toxic. This study showed, for the first time to our knowledge, the chemical composition of the hexane and methanol extracts from T. stans pericarp, as well as the antioxidant and cytotoxic activities of the extracts, fatty acids, and methyl esters.

Objectives: Markhamia lutea ( M. lutea , Bignoniaceae) is mainly found in tropical/neotropical regions of America, Africa and Asia. The plant's leaves, stems or roots are used to treat anaemia, bloody diarrhoea, parasitic and microbial infections. This study evaluates anti-inflammatory properties ( in vitro ) of Markhamia lutea and their curative effects on paclitaxel-induced intestinal toxicity ( in vivo )., Methods: The anti-inflammatory potential of Markhamia lutea was tested over cytokines (TNF-alpha, IL-6, IL-1β, IL-10), reactive oxygen species (ROS) and enzymes (cyclooxygenase and 5-lipoxygenase). While in vivo , intestinal toxicity was induced for 10 days by oral administration of paclitaxel (3 mg/kg, 0.05 mL). Animals in each group were further treated with aqueous (300 mg/kg) and ethanolic (300 mg/kg) leaves extracts of Markhamia lutea during 7 days and clinical symptoms were recorded, hematological, biochemical and histological analysis were subsequently performed., Results: In vitro , aqueous (250 μg/mL) and ethanolic (250 μg/mL) extracts of Markhamia lutea inhibited the activities of cyclooxygenase 1 (56.67 % and 69.38 %), cyclooxygenase 2 (50.67 % and 62.81 %) and 5-lipoxygenase (77.33 % and 86.00 %). These extracts inhibited the production of intracellular ROS, extracellular ROS and cell proliferation with maximum IC 50 of 30.83 μg/mL, 38.67 μg/mL and 19.05 μg/mL respectively for the aqueous extract, then 25.46 μg/mL, 27.64 μg/mL and 7.34 μg/mL respectively for the ethanolic extract. The extracts also inhibited the production of proinflammatory cytokines (TNFα, IL-1β and IL-6) and stimulated the production of anti-inflammatory cytokines (IL-10). In vivo , after administration of paclitaxel, the aqueous and ethanolic extracts of Markhamia lutea significantly reduced the weight loss, the diarrheal stools and the mass/length intestines ratio of the treated animals compared to the animals of the negative control group. Biochemically, the extracts lead to a significant drop in serum creatinine and alanine aminotransferase levels, followed by a significant increase in alkaline phosphatase. In addition to bringing the haematological parameters back to normal values after disturbance by paclitaxel, the extracts caused tissue regeneration in the treated animals., Conclusions: In vitro , aqueous and ethanolic extracts of Markhamia lutea showed anti-inflammatory properties (inhibition of COX1, COX2, 5-LOX activities, inhibition of ROS production and cell proliferation); in vivo , the same extracts showed curative properties against intestinal toxicity caused by paclitaxel., (© 2023 Walter de Gruyter GmbH, Berlin/Boston.)

A novel monoterpene alkaloid, named incarvine G, was isolated from the Incarvillea sinensis Lam. Its chemical structure was elucidated using comprehensive spectroscopic methods. Incarvine G is an ester compound comprised of a monoterpene alkaloid and glucose. This compound showed evident inhibition on cell migration, invasion, and cytoskeleton formation of human MDA-MB-231 with low cytotoxicity., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

Millingtonia hortensis L.f. and Oroxylum indicum (L.) Kurz (Bignoniaceae) are native species from the Asian continent. They are popularly used in traditional medicine and their extracts are rich in flavonoids. In this work, ethanolic extracts of stems and leaves of these species were evaluated against the Chikungunya, Zika and Mayaro virus. The extracts were subjected to analysis by ultra-efficient liquid chromatography coupled to mass spectrometry. Additionally, M. hortensis leaves extract was fractionated, leading to the isolation of hispidulin. Anti-arboviral activity against the three viruses was detected for M. hortensis leaves extract with EC 50 ranging from 37.8 to 134.1 µg/mL and for O. indicum stems extract with EC 50 ranging from 18.6 to 55.9 µg/mL. Hispidulin inhibited viral cytopathic effect of MAYV (EC 50 value 32.2 µM) and CHIKV (EC 50 value 78.8 µM). In LC-DAD-ESI-MS/MS analysis we characterized 25 flavonoids confirming once again the presence of these substances in extracts of these species.

Oroxylum indicum is a traditionally used plant in Ayurvedic and folk medicines. The plant is useful for the management of gastrointestinal diseases as well as skin diseases. In the present study, we analyzed the antitumor potential of O. indicum in Dalton's lymphoma ascites tumor cells (DLA) and Ehrlich ascites carcinoma (EAC)-induced solid and ascites tumors. Further, the potential of O. indicum extract (OIM) on skin papilloma induction by dimethyl benz(a) anthracene (DMBA) and croton oil was evaluated. The chemical composition of the extract was analyzed using UPLC-Q-TOF-MS. The predominant compounds present in the extract were demethoxycentaureidin 7- O -rutinoside, isorhamnetin-3- O -rutinoside, baicalein-7- O -glucuronide, 5,6,7-trihydroxyflavone, 3-Hydroxy-3',4',5'-trimethoxyflavone, 5,7-dihydroxy-3-(4-methoxyphenyl) chromen-4-one, and 4'-Hydroxy-5,7-dimethoxyflavanone. Treatment with high-dose OIM enhanced the percentage of survival in ascites tumor-bearing mice by 34.97%. Likewise, high and low doses of OIM reduced the tumor volume in mice by 61.84% and 54.21%, respectively. Further, the skin papilloma formation was brought down by the administration of low- and high-dose groups of OIM (by 67.51% and 75.63%). Overall, the study concludes that the Oroxylum indicum root bark extract is a potentially active antitumor and anticancer agent.

A new glycoiridoid ( 1 ) together with seven (7) known compounds were isolated from the methanol crude extract of the root bark of Stereospermum kunthianum using chromatography methods. Their structures were elucidated using HR-ESI-MS, 1 D- & 2 D-NMR spectroscopies in comparison with previous literature. The antioxidant activity was investigated by using FRAP, DPPH, ABTS and HRSA methods while the antibacterial activity was assays on Escherichia coli (ATCC25922) and Salmonella typhimurium (ATCC14028) strains. The results showed that the isolated compounds had significantly ( p  < 0.01) high radical scavenging (IC 50 ) and reducing power activity. All bacteria strains showed important minimal inhibitory concentration activity against isolated compounds started at 5 mg/mL with an inhibition zone of 6 mm. Thus, the isolated compounds in S. kunthianum justify the use of the plant in traditional medicine for the treatment of various diseases in humans. These isolated compounds can be used for formulation of new drug discovery to treat infectious diseases.

Chemical investigation of the petroleum ether extract of heartwood of Tecomella undulata led to the isolation of tectonaquinone B (1), 2-methylquinizarin (2) along with tecomaquinone I (3), lapachol (4), 2-isopropenylnaphtho[2,3-b]-furan-4,9-quinone (5), dehydro-α-lapachone (6), α-lapachone (7), and β-lapachone (8). This is the first report of isolation of tectonaquinone B and 2-methylquinizarin from this plant. The structures of compounds were elucidated by advanced spectroscopic methods. Molecular docking study for potential inhibitory action toward CDK7 (cyclin-dependent kinase 7) were performed, which proved that these compounds have high binding affinities with the receptor protein (CDK7). 2-Methylquinizarin exhibited best docking score (-7.70 kcal/mol) among all the tested compounds. The present study showed that 2-methylquinizarin may exhibit potent anticancer activity through inhibiting CDK7 via interaction with Met94.

Plant extracts are complex mixtures that are difficult to characterize, and mass spectrometry is one of the main techniques currently used in dereplication processes. Fridericia chica is a species with medicinal uses in Latin American countries, used in the treatment of inflammatory and infectious diseases. Extracts of this plant species are characterized by the presence of anthocyanidins. In this study, using high-resolution mass spectrometry coupled with liquid chromatography, it was possible to determine the molecular formula of thirty-nine flavonoids. Fragmentation analysis, ultraviolet spectrum and nuclear magnetic resonance data allowed the partial characterization of the structures of these compounds. The spectral dataset allowed the identification of a series of flavones in addition to the desoxyanthocyanidins common in extracts of the species. The occurrence of some of the proposed structures is uncommon in extracts of species of the Bignoniaceae family, and they are reported for the first time in the extract of this species. Quantitative analyses of total flavonoids confirmed the high content of these constituents in the species, with 4.09 ± 0.34 mg/g of dry plant material. The extract under study showed low in vitro cytotoxicity with CC 50 ≥ 296.7 ± 1.4 µg/mL for Vero, LLC-MK2 and MRC-5 cell lines. In antiviral activity assays, inhibition of the cytopathic effects of Dengue, Zika and Mayaro viruses was observed, with EC 50 values ranging between 30.1 and 40.9 µg/mL. The best result was observed against the Mayaro virus, with an EC 50 of 30.1 µg/mL.

In this work, a metabolic profile of Mansoa hirsuta was investigated, and in vitro assays and theoretical approaches were carried out to evaluate its antioxidant potential. The phytochemical screening detected saponins, organic acids, phenols, tannins, flavonoids, and alkaloids in extracts of leaves, branches, and roots. Through LC-MS analysis, the triterpenes oleanolic acid ( m / z 455 [M-H] - ) and ursolic acid ( m / z 455 [M-H] - ) were identified as the main bioactive components. The extracts of the leaves, branches, and roots revealed moderate antioxidant potential in the DPPH test and all extracts were more active in the ABTS test. The leaf extracts showed better antioxidant capacity, displaying IC 50 values of 43.5 ± 0.14, 63.6 ± 0.54, and 56.1 ± 0.05 µg mL -1 for DPPH, ABTS, and kinetics assays, respectively. The leaf extract showed higher total flavonoid content (TFC) (5.12 ± 1.02 mg QR/g), followed by branches (3.16 ± 0.88 QR/g) and roots (2.04 ± 0.52 QR/g/g). The extract of the branches exhibited higher total phenolic content (TPC) (1.07 ± 0.77 GAE/g), followed by leaves (0.58 ± 0.30 GAE/g) and roots (0.19 ± 0.47 GAE/g). Pharmacophore and molecular docking analysis were performed in order to better understand the potential mechanism of the antioxidant activity of its major metabolites.

Background: Pyrostegia venusta (Ker Gawl.) Miers occurs in threatened biodiversity hotspots of Cerrado and Atlantic forest biomes in Brazil and is used in traditional medicine to treat various respiratory and skin diseases., Methods and Results: This study (i) examined the genetic diversity and structure of six natural populations of P. venusta from different Brazilian regions using sequence-related amplified polymorphism (SRAP) markers; and (ii) compared the intra- and inter-populational levels of the bioactive component verbascoside using high-performance liquid chromatography. The population from Nova Mutum, Mato Grosso, presented the highest genetic variability (Nei index H = 0.2759; Shannon index I = 0.4170; 85.14% polymorphic loci), whereas the population from Araxá, Minas Gerais, presented the lowest genetic variability (H = 0.1811; I = 0.2820; 70.27% polymorphic loci). The intra-populational variability (79%) was significantly higher (p = 0.001) than the inter-populational variability (21%). The populations were clustered into two groups but their genetic differentiation was not associated with geographical origin (Mantel test, r = 0.328; p > 0.05). The verbascoside content significantly differed (p > 0.05) among the six populations and between the individuals from each population. The highest verbascoside levels (> 200 µg/mg extract) were detected in populations from Araxá and Serrana, while the lowest verbacoside levels were detected in populations from Paranaíta and Sinop., Conclusions: This is the first report on the use of SRAP markers to analyze genetic variability in the family Bignoniaceae. Our findings shall help to better understand the genetic and chemical diversity of P. venusta populations, as well as provide useful information to select the most appropriate individuals to prepare phytomedicines., (© 2022. The Author(s), under exclusive licence to Springer Nature B.V.)

Plants of the species Fridericia chica (Bonpl.) L. G. Lohmann (Bignoniaceae), which are widely distributed in Brazil and named crajiru in the state of Amazonas, are known in folk medicine as a traditional medicine in the form of a tea for the treatment of intestinal colic, diarrhea, and anemia, among other diseases. The chemical analysis of extracts of the leaves has identified phenolic compounds, a class of secondary metabolites that provide defense for plants and benefits to the health of humans. Several studies have shown the therapeutic efficacy of F. chica extracts, with antitumor, antiviral, wound healing, anti-inflammatory, and antioxidant activities being among the therapeutic applications already proven. The healing action of F. chica leaf extract has been demonstrated in several experimental models, and shows the ability to favor the proliferation of fibroblasts, which is essential for tissue repair. The anti-inflammatory activity of F. chica has been clearly demonstrated by several authors, who suggest that it is related to the presence of 3-deoxyanthocyanidins, which is capable of inhibiting pro-inflammatory pathways such as the kappa B (NF-kB) nuclear transcription factor pathway. Another important effect attributed to this species is the antioxidant effect, attributed to phenolic compounds interrupting chain reactions caused by free radicals and donating hydrogen atoms or electrons. In conclusion, the species Fridericia chica has great therapeutic potential, which is detailed in this paper with the objective of encouraging new research and promoting the sum of efforts for the inclusion of herbal medicines in health systems around the world.

Spathodea campanulata is an important medicinal plant with traditional uses in the tropical zone. In the current work, we aimed to determine the chemical profiles and biological effects of extracts (methanolic and infusion (water)) from the leaves and stem bark of S. campanulata . The chemical components of the tested extracts were identified using LC-ESI-QTOF-MS. Biological effects were tested in terms of antioxidant (radical scavenging, reducing power, and metal chelating), enzyme inhibitory (cholinesterase, amylase, glucosidase, and tyrosinase), antineoplastic, and antiviral activities. Fifty-seven components were identified in the tested extracts, including iridoids, flavonoids, and phenolic acids as the main constituents. In general, the leaves-MeOH extract was the most active in the antioxidant assays (DPPH, ABTS, CUPRAC, FRAP, metal chelating, and phosphomolybdenum). Antineoplastic effects were tested in normal (VERO cell line) and cancer cell lines (FaDu, HeLa, and RKO). The leaf infusion, as well as the extracts obtained from stem bark, showed antineoplastic activity (CC 50 119.03-222.07 µg/mL). Antiviral effects were tested against HHV-1 and CVB3, and the leaf methanolic extract (500 µg/mL) exerted antiviral activity towards HHV-1, inhibiting the viral-induced cytopathic effect and reducing the viral infectious titre by 5.11 log and viral load by 1.45 log. In addition, molecular docking was performed to understand the interactions between selected chemical components and viral targets (HSV-1 DNA polymerase, HSV-1 protease, and HSV-1 thymidine kinase). The results presented suggest that S. campanulata may be a bright spot in moving from natural sources to industrial applications, including novel drugs, cosmeceuticals, and nutraceuticals.

Background: Tecoma stans (L.) Juss. ex Kunth is a well-known medicinal plant found in tropical and subtropical regions. It contains a broad range of bioactive compounds that exhibit many biological effects, including antidiabetic, antibacterial, and antioxidative activities. However, the effect of natural peptides from T. stans against cancer progression and free radical production is unknown. This study aims to evaluate the cytotoxic, anti-metastatic, and antioxidative activities of natural peptides from T. stans on A549 cells., Methods: The natural peptides were extracted from the flower of T. stans using the pressurized hot water extraction (PHWE) method, followed by size exclusion chromatography and solid-phase extraction-C18. The cytotoxic and anti-metastatic effects of natural peptides were evaluated using MTT and transwell chamber assays, respectively. The free radical scavenging activity of natural peptides was determined using ABTS, DPPH, and FRAP assays. The cells were pretreated with the IC 50 dosage of natural peptides and stimulated with LPS before analyzing intracellular reactive oxygen species (ROS) and proteomics., Results: Natural peptides induced cell toxicity at a concentration of less than 1 ng/ml and markedly reduced cell motility of A549 cells. The cells had a migration rate of less than 10% and lost their invasion ability in the treatment condition. In addition, natural peptides showed free radical scavenging activity similar to standard antioxidants and significantly decreased intracellular ROS in the LPS-induced cells. Proteomic analysis revealed 1,604 differentially expressed proteins. The self-organizing tree algorithm (SOTA) clustered the protein abundances into eleven groups. The volcano plot revealed that the cancer-promoting proteins (NCBP2, AMD, MER34, ENC1, and COA4) were down-regulated, while the secretory glycoprotein (A1BG) and ROS-reducing protein (ASB6) were up-regulated in the treatment group., Conclusion: The anti-proliferative and anti-metastatic activities of natural peptides may be attributed to the suppression of several cancer-promoting proteins. In contrast, their antioxidative activity may result from the up-regulation of ROS-reducing protein. This finding suggests that natural peptides from T. stans are viable for being the new potential anti-cancer and antioxidative agents., Competing Interests: Wattanapong Sittisaree is employed by Merck Life Science Thailand, Merck Ltd. The remaining authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (© 2022 Krobthong et al.)

Structure-guided isolation of a CH 2 Cl 2 -soluble fraction of the heartwood of Catalpa bungei "Jinsi" provided two new naphthoquinones, 9-hydroxy-4-oxo-α-lapachone (1) and 6-hydroxy-4-oxo-α-lapachone (2), together with three undescribed ones (3-5) and six known ones (6-11). The structures were elucidated on the basis of spectroscopic methods including electronic circular dichroism calculation. The antiproliferative effects of these isolates were evaluated in human breast adenocarcinoma cells MCF7. (4R)-4,9-dihydroxy-α-lapachone (5) and (4S)-4,9-dihydroxy-α-lapachone (6) exhibited the significant activities with IC 50 values of 2.19 and 2.41 μM, respectively. The structure-activity relationship of 1-11 in the antiproliferative assay was then discussed. The most potent 5 and 6 were found to induce cell arrest in G1 phage through DNA damage. The findings provided some valuable insights for the discovery and structural modification of α-lapachone as antiproliferative lead compounds against human breast adenocarcinoma cells., (Copyright © 2022. Published by Elsevier B.V.)

Two new phenolic glycosides, oroxylumosides A ( 1 ) and B ( 2 ), along with four known compounds darendoside A ( 3 ), leucosceptoside A ( 4 ), acteoside ( 5 ) and decaffeoylacteoside ( 6 ) were isolated from the stem bark of Oroxylum indicum . Their structures were elucidated by extensive analysis of the 1 D and 2 D NMR as well as HR-ESI-QTOF-MS. In addition, compounds 1  -  4 exhibited inhibitory effects on NO production in LPS-stimulated BV2 microglial cell line with IC 50 values of 58.2 ± 2.9, 70.6 ± 3.5, 56.8 ± 2.8 and 61.1 ± 3.1 µM, respectively.

Three new monoterpene alkaloids, delavatines C-E (1-3), along with five known ones (4-8), were separated from the whole plants of Incarvillea delavayi. All compounds were deduced by interpretation of comprehensive NMR spectral data and X-Ray single crystal diffraction, in combination with a quantum chemical calculation of NMR chemical shift coupled with an advanced statistical procedure DP4+. Compounds 1-8 were assessed NO suppressive effect in LPS-stimulated BV2 microglia cells. Compounds 2, 3, 6, and 8 exhibited significant inhibition against NO production in LPS-induced BV2 cells with IC 50 values of 25.62, 17.29, 19.94 and 23.88 μM, stronger than or comparable to the positive control (AG) with IC 50 value of 26.13 μM., (© 2022 Wiley-VHCA AG, Zurich, Switzerland.)

Despite the breakthrough in the development of anticancer therapies, plant-derived chemotherapeutics continue to be the basis of treatment for most types of cancers. Fridericia platyphylla is a shrub found in Brazilian cerrado biome which has cytotoxic, anti-inflammatory, and analgesic properties. The aim of this study was to investigate the antiproliferative potential of the crude hydroethanolic extract, subfraction (containing 59.3% of unusual dimeric flavonoids Brachydin E and 40.7% Brachydin F), as well as Brachydin E and Brachydin F isolated from F. platyphylla roots. The cytotoxic activity was evaluated in glioblastoma, lung, prostate, and colorectal human tumor cell lines. The crude hydroethanolic extract did not present cytotoxic activity, but its subfraction presented lower IC50 values for glioblastoma (U-251) and prostate adenocarcinoma (PC-3) cell lines. Brachydins E and F significantly reduced cell viability, proliferation, and clonogenic potential of PC-3, inducing them to the process of regulated cell death. In silico studies have indicated nuclear receptors as targets for Brachydins E and F, and molecular docking has pointed out their binding into glucocorticoid receptor (GR) ligand pocket. Targeting GR pathway has been described as a therapeutic strategy, especially for prostate cancer. These results suggest that Brachydin E and Brachydin F are promising compounds to be further explored for their antitumor effects., Competing Interests: The authors declare no conflicts of interest., (Copyright © 2022 Carolina A. de Lima et al.)

Chemical investigation of the ethanol extract of the leaves of Newbouldia laevis (P. Beauv) led to the isolation of two new caffeic acid glycosides, Newboulasides A (1) and B (2) . The structures of these compounds were determined on the basis of extensive spectroscopic methods, including 1D-, 2D-NMR and MS data. The extracts and fractions and the isolated compounds were evaluated for their inhibition of α-amylase enzyme activity. The extract showed inhibition of α-amylase activity with IC 50 value of 102.91 µg/mL, while the isolated compounds ( 1 and 2) exhibited pronounced inhibition with IC 50 values of 4.95 and 4.44 µg/mL respectively, comparable to the standard - Acarbose with IC 50 value of 4.05 µg/mL. Our findings demonstrated that the inhibition of α-amylase activity may be part of the mechanisms through which N. leavis exhibits antidiabetic effect.

Administration of Chemotherapeutics, especially doxorubicin (DOX) and cyclophosphamide (CPS), is commonly associated with adverse effects such as myelosuppression and cardiotoxicity. At this time, few approved therapeutic options are currently available for the management of chemotherapy-associated cardiotoxicity. Thus, identification of novel therapeutics with potent cardioprotective properties and minimal adverse effects are pertinent in treating Doxorubicin and Cyclophosphamide-induced cardiotoxicity. Oroxylum indicum extract (OIE, Sabroxy®) is a natural product known to possess several beneficial biological functions including antioxidant, anti-inflammatory and cytoprotective effects. We therefore set to investigate the cardioprotective effects of OIE against Doxorubicin and Cyclophosphamide-induced cardiotoxicity and explore the potential cardioprotective mechanisms involved. Adult male mice were treated with DOX and CPS in combination, OIE alone, or a combination of OIE and DOX & CPS. Swimming test was performed to assess cardiac function. Markers of oxidative stress were assessed by levels of reactive oxygen species (ROS), nitrite, hydrogen peroxide, catalase, and glutathione content. The activity of interleukin converting enzyme and cyclooxygenase was determined as markers of inflammation. Mitochondrial function was assessed by measuring Complex-I activity. Apoptosis was assessed by Caspase-3 and protease activity. Mice treated with DOX and CPS exhibited reduced swim rate, increased oxidative stress, increased inflammation, and apoptosis in the heart tissue. These cardiotoxic effects were significantly reduced by co-administration of OIE. Furthermore, computational molecular docking studies revealed potential binding of DOX and CPS to tyrosine hydroxylase which validated our in vivo findings regarding the inhibition of tyrosine hydroxylase activity. Our current findings indicated that OIE counteracts Doxorubicin and Cyclophosphamide-induced cardiotoxicity-through inhibition of ROS-mediated apoptosis and by blocking the effect on tyrosine hydroxylase. Taken together, our findings suggested that OIE possesses cardioprotective effects to counteract potentially fatal cardiac complications associated with chemotherapy treatment., (© 2021. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.)

Mansoa hirsuta is a medicinal plant native to the Brazilian semi-arid region. This approach aimed to investigate the in vitro and in vivo toxicity and anti-inflammatory and analgesic actions of the M. hirsuta fraction (MHF). In vitro cell viability was assessed in 3T3 cells. In vivo, the acute toxicity test, a single dose of the MHF was administered. For the subchronic toxicity test, three doses of were administered for 30 days. Locomotion and motor coordination were assessed using open field and rota-rod. The anti-inflammatory activity was evaluated in carrageenan-induced paw edema and zymosan-induced air-pouch models. Myeloperoxidase (MPO) and total proteins were also measured. The antinociceptive activity MHF was determined using acid acetic-induced abdominal writhing and formalin models. In the cytotoxicity assay, MHF showed no significative impairment of cell viability and in the acute toxicity study, did not cause mortality or signs of toxicity. Repeated exposure to MHF did not cause relevant toxicological changes. The evaluation in the open field test showed that the MHF did not alter the locomotor activity and there was no change in motor coordination and balance of animals. MHF significantly reduced edema, MPO production, the migration of leukocytes and protein leakage. In addition, MHF reduced abdominal writhing and significantly inhibited the first and second stage of the formalin test. The results of this study indicated that MHF has an anti-inflammatory and analgesic potential without causing acute or subchronic toxic effects and it can be a promising natural source to be explored., (Copyright © 2021 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)

Oroxylum indicum is one of the valuable Dai pharmaceuticals; the dry seeds and bark of O. indicum were used to treat acute cough, sore throat and so on. Of the seven compounds from O. indicum were determined and obtained using the bioassay-guided method. Among them, compound 7 was obtained from the plant for the first time. Eight bacterial strains and one yeast fungi were exposed to the compounds. Minimum inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) or minimum fungicidal concentrations were determined according to the standard broth microdilution method. Baicalein (2) exhibited relative strong antibacterial activities with MIC of 8 μg ml -1 and MBC of 16 μg ml -1 against three MRSA strains of Staphylococcus aureus of SCCmec III type, whereas flavonoids 3, 5 and 7 showed some degree of activities against methicillin-susceptible S. aureus (MSSA, ATCC 25923). The findings may offer new evidence that why O. indicum was used widely in Dai peoples' life., (© 2021 Society for Applied Microbiology.)

Infections caused by microorganisms are a major cause of morbidity and mortality worldwide, and natural products continue to be important sources for the discovery of new antimicrobial agents. Ursolic acid is a triterpene with known antibacterial action, being naturally found in plants, such as Jaracanda oxyphylla and Jacaranda caroba (Bignoniaceae). Ursolic acid derivative esters have revealed potential biological activities, such as antitumor, antiviral, and antibacterial activity. In this study, sixteen esters (1-16) were synthesized from ursolic acid using DIC/DMAP and characterized by infrared (IR), nuclear magnetic resonance ( 1 H- and 13 C-NMR) and mass spectrometry. All ursolic acid esters were evaluated against Bacillus cereus, Staphylococcus aureus, Escherichia coli, Salmonella typhimurium, and the yeast Candida albicans. Six compounds are herein described for the first time (3, 9, 11, 13, 14 and 16) with yields up to 91.6 %. Compounds 11 (3β-(3,4-dimethoxybenzoyl)ursolic acid) and 15 (3β-nicotinoylursolic acid) displayed promising antifungal activity, with inhibition of C. albicans growth of 93.1 and 95.9 %, respectively., (© 2021 Wiley-VHCA AG, Zurich, Switzerland.)

Oroxylum indicum , of the Bignoniaceae family, has various ethnomedical uses such as an astringent, anti-inflammatory, anti-bronchitis, anti-helminthic and anti-microbial, including anticancer properties. The druggability of OI stem bark extract was determined by its molecular docking interactions with PARP and Caspase-3, two proteins involved in cell survival and death. Note that 50 µg/mL of Oroxylum indicum extract (OIE) showed a significant ( p < 0.05%) toxicity to HSC-3 cells. MTT aided cell viability and proliferation assay demonstrated that 50 µg/mL of OIE displayed significant ( p < 0.5%) reduction in cell number at 4 h of incubation time. Cell elongation and spindle formation was noticed when HSC-3 cells were treated with 50 µg/mL of OIE. OIE initiated DNA breakage and apoptosis in HSC-3 cells, as evident from DNA ladder assay and calcein/EB staining. Apoptosis potential of OIE is confirmed by flow cytometer and triple-staining (live cell/apoptosis/necrosis) assay. Caspase-3/7 fluorescence quenching (LANCE) assay demonstrated that 50 µg/mL of OIE significantly enhanced the RFU of caspases-3/7, indicating that the apoptosis potential of OIE is probably through the activation of caspases. Immuno-cytochemistry of HSC-3 cells treated with 50 µg/mL of OIE showed a significant reduction in mitochondrial bodies as well as a reduction in RFU in 60 min of incubation time. Immunoblotting studies clearly showed that treatment of HSC-3 cells with OI extract caused caspase-3 activation and PARP deactivation, resulting in apoptotic cell death. Overall, our data indicate that OIE is an effective apoptotic agent for human squamous carcinoma cells and it could be a future cancer chemotherapeutic target.

The polyphenolic distribution on different organs of Argylia radiata , an extremophile plant from the Atacama "Flowering Desert", is presented herein for the first time. For this purpose, the total phenolic content and antioxidant capacity of ethanolic extracts from leaves, tuberous root and flowers of different colors were evaluated. Orange and red flowers showed the highest polyphenolic and flavonoid content. The maximum anthocyanin concentration was found in red flowers and the antioxidant activity (FRAP) of extracts changed according to the organ. The UPLC-MS/MS analysis of the extracts allowed to identify 10 new polyphenols belonging to different families. Rutin was identified as the most abundant polyphenol in all plant organs, followed by quercetin and coumaric acid. Their role in plant response to abiotic and biotic stress, as well as their potential biotechnological application are discussed.

Fridericia chica (Bignoniaceae) is a traditional medicinal plant. The aim of this research was to determine the protective effects of the hydroethanolic extract from the F. chica leaves (HEFc) against the cytotoxicity of zearalenone (α-ZEL) and β-ZEL on SH-SY5Y cells. Free radical scavenging activity of HEFc was evaluated using the DPPH method. The cytotoxicity of both zearalenone metabolites and HEFc was examined using MTT test, as was the cytoprotective effects of the HEFc on cells treated with these mycotoxins. The chemical composition of HEFc was determined using UPLC-QTOF-MS/MS. HEFc elicited good DPPH radical scavenging activity following a concentration-dependent relationship. Cells exposed to α-ZEL exhibited a viability ˂50% after 48 h of treatment (25 and 50 µM), while those exposed to β-ZEL showed viability ˂50% (100 µM) and ˂25% (25-100 µM) after 24 and 48 h of exposure, respectively. HEFc showed a significant increase in cell viability after exposure to α-ZEL (25 and 50 µM) and β-ZEL (6-100 µM) ( p < 0.05). UPLC-QTOF-MS/MS analyses allowed the identification of 10 phytochemical components in the HEFc. In short, the hydroethanolic extract of F. chica grown in Colombian Caribbean can protect against the effects of mycotoxins and it is a valuable source of compounds with antioxidant properties.

Oroxylum indicum (Sonapatha) is traditionally used to cure several human ailments. Therefore, the cell killing effect of chloroform, ethanol, and water extracts of Sonapatha was studied in cultured HeLa cells treated with 0-100 µg/mL of these extracts/doxorubicin by MTT assay. Since ethanol extract was most cytotoxic its effect was further investigated by clonogenic, apoptosis, necrosis, and lactate dehydrogenase assays. The mechanism of cytotoxicity of Sonapatha was determined at the molecular level by estimation of caspase 8 and 3 activities and Western blot analysis of NF-κB, COX-2, Nrf2, and RASSF7 which are overexpressed in neoplastic cells. HeLa cells treated with Sonapatha extract exhibited a concentration and time-dependent rise in the cytotoxicity as indicated by the MTT assay. Ethanol extract of Sonapatha (0, 20, 40, and 80 μg/mL) reduced clonogenicity, increased DNA fragmentation, apoptotic and necrotic indices, lactate dehydrogenase release, caspase 8 and 3 activities and inhibited the overexpression of NF-κB, COX-2, Nrf2, and RASSF7 in HeLa cells concentration-dependently., (Copyright © 2021 Elsevier Inc. All rights reserved.)

Background: The incidence of nonalcoholic fatty liver disease (NAFLD), especially nonalcoholic steatohepatitis (NASH), has significantly increased in recent years and has become an important public health issue. However, no U.S. Food and Drug Administration (FDA)-approved first-line drug is currently available for the treatment of NAFLD and NASH; therefore, research on new drugs is currently a hot topic. Oroxylum indicum (Linn.) Kurz is extensively distributed in South China and South Asia and has many biological activities. However, its effects on NAFLD or even NASH and the corresponding mechanisms are still not clear., Purpose: To investigate the effect and mechanism of O. indicum seed extract (OISE) on preventing anti-inflammatory action in the progression from simple nonalcoholic fatty liver (NAFL) to NASH., Methods: A network pharmacology method to construct ingredient-target networks and the protein-protein interaction (PPI) network of OISE in NASH were constructed for topological analyses and hub-target screening. Enrichment analyses were performed to identify the critical biological processes and signaling pathways. Simultaneously, in vitro and in vivo experiments investigated the effect and mechanism of OISE, baicalein, and chrysin on inflammation by biochemical indicator detection, luciferase reporters, pathological staining, and immunoblotting in oleic acid-stimulated HepG2 cells or in high-fat diet-fed rats., Results: The network pharmacology showed that OISE prevented the development and progression of NAFL into NASH through various pathways and targets and that the nuclear factor NF-κB (NF-κB) pathway regulated by baicalein and chrysin played an important role in the treatment of NASH. In in vitro experiments, we further showed that OISE and its ingredients, namely, baicalein and chrysin, all improved the inflammatory status in oleic acid-stimulated HepG2 cells, inhibited the nuclear transcriptional activities of NF-κB, increased the IκB level, and decreased the phosphorylation level of NF-κB. Furthermore, in a high-fat diet-induced NASH model in rats, we also showed that OISE prevented the development and progression of NASH by inhibiting the nuclear transcriptional activity of NF-κB., Conclusion: OISE suppressed inflammatory responses and prevented the development and progression of NAFL into NASH through inhibition of the nuclear transcriptional activity of NF-κB. OISE may be used to treat NAFLD through many functions, including an increase in insulin sensitivity, a decrease in lipid accumulation in the liver, suppression of inflammation, and clearance of free radicals., (Copyright © 2021. Published by Elsevier GmbH.)

The aqueous extract of fallen leaves from Fridericia chica (Bonpl.) L.G. Lohmann is utilized as a remedy in communities at northern Colombia. Traditional uses include wound healing, gastrointestinal inflammation, leukemia and psoriasis, among others. The aims of this research were to evaluate the potential of the aqueous extract of fallen leaves of F. chica (AEFchica) to inhibit ethoxylated nonylphenol (Tergitol)-induced toxicity in Caenorhabditis elegans; and to identify its main components. The pharmacological properties of AEFchica was evaluated using a Tergitol-induced toxicity model in Caenorhabditis elegans. Lethality, locomotion, reproduction, and DAF-16 nuclear translocation were quantified. The chemical composition of AEFchica was carried out using ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. AEFchica induced very little lethality on C. elegans (5.6%) even at high concentrations (10,000 μg/mL). The extract had no effect on locomotion impairing induced by ethoxylated nonylphenol. However, AEFchica (1000 μg/mL) abrogated Tergitol-induced mortality, recovering up to 53.3% of the nematodes from lethality induced by 10 mM Tergitol. Similarly, it also blocked Tergitol-dependent reproduction inhibition (82.1% recovery), as well as DAF-16 nuclear translocation (>95%), suggesting a prominent role on oxidative stress control. The chemical analysis indicated the presence of a great variety of molecules with known antioxidant, metabolic and immune modulator properties, such as hydroxylated methoxy flavones, N-methyl-1-deoxynojirimycin, and rehmaionoside A. In short, the aqueous extract of F. chica protects C. elegans from the deleterious effects of Tergitol on lethality, reproduction and oxidative stress involving DAF-16-mediated pathway. This extract is a promising source of bioactive phytochemicals for multi-target pharmacological purposes., (Copyright © 2021 Elsevier Inc. All rights reserved.)

Background: The growth or multiplication of harmful microorganisms in addition to harmful human activities has led to many disorders in humans. Consequently, there is a search for medications to treat these disorders. Interestingly, medicines of plant origin are known to be among the most attractive sources of new drugs and have shown promising results in the treatment of various diseases including peptic ulcers. This review, therefore, is aimed at obtaining knowledge on some Ghanaian ethnomedicinal plants used to treat peptic ulcers, their folkloric uses, their phytochemicals, and their antiulcer and related pharmacological activities as well as finding areas for prospective studies., Methods: Published peer-reviewed articles on ethnomedicinal plants used for the management of peptic ulcers in Ghana from 1967 to 2020 were sourced and used for the study., Results: In this review, 13 plants were identified which belong to 10 different families including Sapindaceae, Apocynaceae, and Bignoniaceae. The parts most often used for most preparations were the leaves (53%), followed by stem bark and roots (both having the same percentage of use of 17.6%), the whole plant (5.9%), and the rhizomes (5.9%). Azadirachta indica was the only plant that had undergone some patient studies in addition to animal studies . Conclusion . A discussion of various antiulcer activity studies using ulcer models carried out on selected medicinal plants used for the management of peptic ulcer disease in addition to brief information on their folkloric uses and their phytochemical and other pharmacological properties is presented. These medicinal plants may be used in developing herbal products for the management of peptic ulcer disease., Competing Interests: The authors declare that no conflict of interest exists for the publication of this article., (Copyright © 2021 Mavis Boakye-Yiadom et al.)

Oroxylin A, a major flavonoid in the extracts of Oroxylum indicum as well as Scutellaria baicalensis possesses useful medicinal properties. Many of the published routes claiming the synthesis of Oroxylin A ( 1 ) have in fact led to a regioisomer Negletein that was misinterpreted as Oroxylin A. In the present work, we describe a novel, straight-forward and scalable semi-synthetic approach for rapid access to the title compound, the structure of which is unambiguously secured by NMR and X-ray crystallographic analysis of a derivative. This work also encompasses the synthesis of a glycosylated derivative of Oroxylin A viz OAGME ( 2 ), which has marked pharmacological importance.

Bignonia nocturna (Bignoniaceae) is a plant used for medicinal purposes by the Amazonian indigenous peoples. To date, there have been no reported studies on its toxicity. The present study aimed to evaluate the chemical composition of essential oils obtained from Bignonia nocturna by different extraction techniques. In addition, an in silico study of the molecular interactions was performed using molecular docking and molecular dynamics. The extractions were carried out by hydrodistillation, simultaneous distillation-extraction, and steam distillation, using samples collected from the Amazon in summer and winter. The chemical composition was analyzed by GC/FID and GC/MS, and the cytotoxic activity in Artemia salina Leach was evaluated. The maximum yield (1.38 % w/w) was obtained by hydrodistillation. The results indicated that benzaldehyde predominated in all the fractions of both the volatile concentrate and the essential oils. In addition, the oil proved to be highly toxic to Artemia salina. The computer simulation results indicated that benzaldehyde strongly interacts with acetylcholinesterase, which is the likely interaction mechanism responsible for the cytotoxicity., (© 2021 Wiley-VHCA AG, Zurich, Switzerland.)

Kigelia africana plant is widely used as a herbal remedy in preventing the onset and the treatment of cancer-related infections. With the increase in the research interest of the plant, the specific chemical compound or metabolite that confers its anticancer properties has not been adequately investigated. The ethyl acetate and butanol fractions of the fruit extracts were evaluated by 2-(4,5-dimethylthiazol-2-yl)-3,5-diphenyl-2H-tetrazolium bromide assay against four different cell lines, with the ethyl acetate fraction having inhibition concentration values of 0.53 and 0.42 μM against Hep G2 and HeLa cells, respectively. More than 235 phytoconstituents were profiled using UHPLC-TOF-MS, while more than 15 chemical compounds were identified using GC-MS from the fractions. Molecular docking studies revealed that physostigmine, fluazifop, dexamethasone, sulfisomidine, and desmethylmirtazapine could favorably bind at higher binding energies of -8.3, -8.6, -8.2, and -8.1 kcal/mol, respectively, better than camptothecin with a binding energy of -7.9 kcal/mol. The results of this study showed that physostigmine interacted well with topoisomerase IIα and had a high score of pharmacokinetic prediction using absorption, distribution, metabolism, excretion, and toxicity profiles, thereby suggesting that drug design using physostigmine as a base structure could serve as an alternative against the toxic side effects of doxorubicin and camptothecin., (© 2020 John Wiley & Sons, Ltd.)

For the first time, the cytotoxic and phytochemical investigation of the leaves of Stereospermum binhchauensis V.S. Dang, a new species discovered in Viet Nam were finalized and led to purify nine compounds, including one furancoumarin (1) , one chromone (3) , two triterpenoids (2, 4) , two flavonoids (5 , 8) , two flavanoids (6, 7) and one iridoid (9) using various chromatography methods. Their structures were verified by HR-ESI-MS, NMR experiments and compared with previous literatures. For the first time, compounds ( 5 - 8) were realized from the genus Stereospermum, while compounds ( 1 , 2 , 3, 4 & 9 ) were designated from the species S. binhchauensis . Furthermore, the furancoumarin, chromone and flavanoid classes were notified for the first time from the genus Stereospermum.

The antidepressant activity of Spathodea campanulata flowers was evaluated in mice and in silico. When tested at doses of 200 and 400 mg/kg, the methanol extract of S. campanulata (MESC) showed dose-dependent antidepressant activity in the force swim test (FST), tail suspension test (TST), lithium chloride-induced twitches test and the open field test. In FST and TST, animals treated with MESC demonstrated a significant decrease in the immobility period compared to the control group. The lithium chloride-induced head twitches were significantly reduced following administration of MESC. The latter, at the dose of 400 mg/kg, also significantly reduced locomotor activity. Following administration of MESC, changes in the levels of serum corticosterone, and of norepinephrine, dopamine, serotonin, 4-hydroxy-3-methoxyphenylglycol (MHPG), 4-dihydroxyphenylacetic acid (DOPAC), and 5-hydroxyindoleacetic acid (5-HIAA) were measured in different brain regions using HPLC. The presence of spatheoside A (m/z 541) and spatheoside B (m/z 559) in MESC was detected using HPLC/ESI-MS. These two iridoids demonstrated a high predictive binding affinity for the active site of the type A monoamine oxidase (MAO-A) enzyme with scores of 99.40 and 93.54, respectively.  These data suggest that S. campanulata flowers warrants further investigation as a source of novel templates for antidepressive drugs.

Ethnopharmacological Relevance: Tecoma stans (L.) Juss. ex Kunth (Bignoniaceae) is an attractive evergreen plant known as kusi urakame, koyawari, Palo amarillo, tronadora, yellow-elder, yellow trumpet bush, trumpet-flower, yellow-bells, trumpet bush, ginger-Thomas, esperanza, and timboco. It is widely used in traditional Mexican medicine, to treat hyperglycemia, gastrointestinal and urinary tract disorders, jaundice, toothaches, headaches, colds, skin infections, and scorpion, snake, and rat bites. Current research focusses on evaluating its bioactive components and therapeutic potential., Aim of the Study: The current article reviewed the information available on Tecoma stans ethnopharmacology, geographical distribution, chemical composition, phytochemistry, therapeutic effects, and toxicology., Material and Methods: Information of botanical description, distribution, traditional uses, chemical composition, bioactive components, and therapeutic investigations was gathered from a comprehensive literature search of electronic databases such as Science Direct, PubMed, Web of Science, Wiley, ACS, Springer, Taylor and Francis, Google Scholar, and SCOPUS until 2020 for publications (peer-reviewed articles, eBooks, short communications, reports from international organizations, and case letters). Information was also included from books, conference proceedings, and thesis. Primary keywords for data collection were "Tecoma stans," and "Ethnopharmacology," followed by secondary keywords such as "Constituents," "Therapeutic effect," and "Toxicity.", Results: An exhaustive comparative study of the accessible sources of Tecoma stans confirmed its origin, ethnopharmacological and therapeutic uses. More than 120 chemical compounds have been isolated, and the main active principles are alkaloids, phenolic acids, flavonoids, and fatty acids. The plant possesses vast therapeutic benefits, such as lowering elevated blood sugar levels, anti-inflammatory, anti-cancer, anti-bacterial, anti-fungal, anti-oxidant, hepatoprotective, and wound healing actions., Conclusions: Comprehensive literature analysis exhibits that many populations have utilized Tecoma stans around the globe with specific reference to different parts of Mexico. The above information shows that the plant holds many hidden potentials and can, therefore, be studied extensively for its phytoconstituents and therapeutic effects. However, while going through the literature, it was observed that incomplete data is reported on in vivo trials, especially concerning its dosage, positive and negative control groups, intervention time, and toxicity studies. Additionally, there is a lack of information on its complete nutritional and phytochemical profiling. We trust that this review will help lay the groundwork for encouraging pharmacological and pharmaceutical studies. It will also direct us to understand the clinical relevance and applications of bioactive compounds from Tecoma stans in the prevention and treatment of diseases., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Catalpa pod has been used in traditional medicine for the treatment of diabetes mellitus in South America. Studies on the constituents of Catalpa species have shown that it is rich in iridoids. In the present study, three previously undescribed compounds ( 2 - 4 ), including two secoiridoid derivatives along with twelve known compounds, were isolated from the fruits of Catalpa bignonioides Walt. In addition, fully assigned 13 C-NMR of 5,6-dihydroxy-7,4'-dimethoxyflavone-6- O -sophoroside ( 1 ) is reported for the first time in the present study. The structures of compounds were determined on the basis of extensive spectroscopic methods, including UV, IR, 1D, and 2D NMR, mass spectroscopy, and CD spectroscopic data. All the isolated compounds were evaluated for α-glucosidase inhibitory activity. Among the tested compounds, compounds 2 , 3 , and 9 exhibited significant inhibitory activity against α-glucosidase enzyme assay. Meanwhile, the effect of compounds 2 , 3 , and 9 on glucose-stimulated insulin secretion (GSIS) was measured using pancreatic β-cells. Compounds 2 , 3 , and 9 exhibited non-cytotoxicity-stimulated insulin secretion in INS-1 cells. The expression levels of proteins associated with β-cell function and insulin secretion such as phosphorylation of total insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), Akt, activated pancreatic duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) were increased in INS-1 cells after treatment with compounds 2 , 3 , and 9 . The findings of the present study could provide a scientific warrant for their application as a potential antidiabetic agent.

Natural products are rich sources of interesting scaffolds possessing a plethora of biological activity. With the isolation of the martinella alkaloids in 1995, namely martinelline and martinellic acid, the pyrrolo[3,2-c]quinoline scaffold was discovered. Since then, this scaffold has been found in two additional natural products, viz. incargranine B and seneciobipyrrolidine. These natural products have attracted attention from synthetic chemists both due to the interesting scaffold they contain, but also due to the biological activity they possess. This review highlights the synthetic efforts made for the preparation of these alkaloids and formation of analogues with interesting biological activity.

Fusarium verticillioides is an important fungal pathogen of maize, causing stalk rot and severely affecting crop production. The aim of this study was to characterize the protective effects of formulations based on Jacaranda mimosifolia leaf extracts against F. verticillioides in maize. We compared different seed treatments comprising J. mimosifolia extracts, chemical fungicide (mefenoxam) and salicylic acid to modulate the defense system of maize host plants. Both aqueous and methanolic leaf extracts of J. mimosifolia (1.2% w/v) resulted in 96-97% inhibition of mycelial growth of F. verticillioides. While a full-dose (1.2%) extract of J. mimosifolia provided significant protective effects on maize plants compared to the inoculated control, a half-dose (0.6% w/v) application of J. mimosifolia in combination with half-strength mefenoxam was the most effective treatment in reducing stalk rot disease in pot and field experiments. The same seed treatment significantly upregulated the expression of genes in the leaves encoding chitinase, glucanase, lipid transfer protein, and pathogenesis-related proteins PR-1, PR-5 and PR-10, 72 h after inoculation. This treatment also induced the activities of peroxidase, polyphenol oxidase, protease, acid invertase, chitinase and phenylalanine ammonia lyase. We conclude that seed pre-treatment with J. mimosifolia extract with half-strength chemical mefenoxam is a promising approach for the management of stalk rot in maize.

In Southeast Asia, traditional medicine has a longestablished history and plays an important role in the health care system. Various traditional medicinal plants have been used to treat diseases since ancient times and much of this traditional knowledge remains preserved today. Oroxylum indicum (beko plant) is one of the medicinal herb plants that is widely distributed throughout Asia. It is a versatile plant and almost every part of the plant is reported to possess a wide range of pharmacological activities. Many of the important bioactivities of this medicinal plant is related to the most abundant bioactive constituent found in this plant-the baicalein. Nonetheless, there is still no systematic review to report and vindicate the biological activities and therapeutic potential of baicalein extracted from O. indicum to treat human diseases. In this review, we aimed to systematically present in vivo and in vitro studies searched from PubMed, ScienceDirect, Scopus and Google Scholar database up to 31 March 2020 based on keywords " Oroxylum indicum " and "baicalein". After an initial screening of titles and abstracts, followed by a full-text analysis and validation, 20 articles that fulfilled all the inclusion and exclusion criteria were included in this systematic review. The searched data comprehensively reported the biological activities and therapeutic potential of baicalein originating from the O. indicum plant for anti-cancer, antibacterial, anti-hyperglycemia, neurogenesis, cardioprotective, anti-adipogenesis, anti-inflammatory and wound healing effects. Nonetheless, we noticed that there was a scarcity of evidence on the efficacy of this natural active compound in human clinical studies. In conclusion, this systematic review article provides new insight into O. indicum and its active constituent baicalein as a prospective complementary therapy from the perspective of modern and scientific aspect. We indicate the potential of this natural product to be developed into more conscientious and judicious evidencebased medicine in the future. However, we also recommend more clinical research to confirm the efficacy and safety of baicalein as therapeutic medicine for patients.