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The review introduced chemical diversity in structures, biological activities, biosynthesis and chemical synthesis of unusual cyclized triterpenoids.

Chemical investigation of the aerial parts of Astragalus lehmannianus Bunge (Leguminosae) led to the isolation and identification of a new cycloartane triterpene glycoside – lehmanniaside (2'-O-ace...

Astragalus genus has been recorded as yielding a wide range of flavonoids, triterpenes, triterpene saponins, and polysaccharides. Cycloartane- and oleanane-type triterpenes are widely distributed in this genus with intriguing biological effects. Combining liquid chromatography (LC) with high-resolution mass spectrometry (HR.MS) has provided a valuable tool in the analysis of these triterpenes in plants. In this chapter, we summarized the main triterpenes studied by liquid chromatography high.resolution mass spectrometry (LC-HR-MS) associated with mass analysers, molecular weight information and mass fragmentation, presenting an interesting overview of increasing interest for cycloartane- and oleanane-type triterpenes.Astragalus genus has been recorded as yielding a wide range of flavonoids, triterpenes, triterpene saponins, and polysaccharides. Cycloartane- and oleanane-type triterpenes are widely distributed in this genus with intriguing biological effects. Combining liquid chromatography (LC) with high-resolution mass spectrometry (HR.MS) has provided a valuable tool in the analysis of these triterpenes in plants. In this chapter, we summarized the main triterpenes studied by liquid chromatography high.resolution mass spectrometry (LC-HR-MS) associated with mass analysers, molecular weight information and mass fragmentation, presenting an interesting overview of increasing interest for cycloartane- and oleanane-type triterpenes.

Shikimic acid-derived polyoxygenated cyclohexene natural products commonly occurring in several species of the

Soot particles emitted from the burning of solid fuel sources in the households carry important environmental and public health implications. In this study, the indoor soot particles released from firewood, cow dung, and bagasse burning at households of selected rural areas of Khyber Pakhtunkhwa province of Pakistan were investigated by characterization analyses to study its morphological and elemental compositions. Results demonstrated diverse compositions of soot particles from each fuel source. The surface areas of soot particles emitted by the firewood, cow dung, and bagasse were about 0.3, 0.4, and 8.64 m2 g-1 , respectively. For the soot particles emitted by the firewood burning, the major functional groups for aromatic compounds were C═C at the 1,431-1,599 at 1,000-2,000 cm-1 . The absorbance rate of alkanes was about 1,599-1,431 at 1,000-2,000 cm-1 . However, silicon band vibration was more prominent in bagasse soot particles as compared to other samples. The emission of soot particles with high surface area in the atmosphere could provide an elevated adsorption sites for atmospheric pollution and trap more energy resulting in increased atmospheric temperature. Findings from the present study suggest that current households' fuel combustion practices significantly contribute to increase the particulate matter in the atmosphere and possible enhance climate change phenomenon and related disasters in northern Pakistan.

Background Natural products acquire vast and intriguing structural diversity and have been recognized as a tremendously diverse source of new lead compounds. Numerous bioactive secondary metabolites are present in the form of glycosylated molecules in which the sugar parts are normally associated with the interaction along with molecular recognition of the cellular target. Scope and approach The presence of sugar entities are crucial as well as in some cases necessary, for therapeutic effects. Establishing novel and potent glycosylated secondary metabolites has formed a main goal in the natural product field from fungi and bacteria. These compounds possess a diverse range of sugar units. Key findings and conclusions Fungi is considered one of the important sources for approved drugs with a diverse range of mode of action. The sugar part in numerous pharmacologically active natural products enhances bioavailability, biological potential, reduce toxicity, and improve stability. The vast majority of glyocosides showed antimicrobial effects, cytotoxic, antiviral and antiinflammatory effects. Notably, numerous fungal glycosides presented in this review illustrate significant antimicrobial effects towards various microorganisms especially against plant pathogens. The antimicrobial effects of these fungal glycosides indicate that these metabolites could be employed as natural preservatives in food in order to abolish or control the growth of pathogenic and spoilage microorganisms.

Introduction: Cancer has been identified to be the second major cause of death internationally as exemplified by ca. 9.6 million deaths in 2018 along with ca. 18 million new patients in 2018 that have been recorded. Natural boswellic acids (BAs) and their source, frankincense, have been reported to possess in vitro and in vivo anticancer effects toward various cancer cells.Areas covered: This comprehensive review focuses on the importance of boswellic acids (BAs) for the establishment of future treatments of cancer. Moreover, potent semisynthetic derivatives of BAs have been described along with their mode of action. In addition, important structural features of the semisynthetic BAs required for cytotoxic effects are also discussed.Expert opinion: Numerous semisynthetic BAs illustrate excellent cytotoxic effects. Of note, compounds bearing cyanoenone moieties in ring A, endoperoxides and hybrids display increased and more potent cytotoxic effects compared with other semisynthetic BAs. Moreover, BAs have the potential to conjugate or couple with other anticancer compounds to synergistically increase their combined anticancer effects. In addition, to get derived BAs to become lead anticancer compounds, future research should focus on the preparation of ring A cyanoenones, endoperoxides, and C-24 amide analogs.

In the last decade the prevalence of diabetes has escalated globally and it is estimated that the number of diabetic people will increase to 642 million by 2040. Although numerous classes of pharmaceutical drugs are available to treat Type ll diabetes, they manifest certain side effects. PTP1B has attracted significant interest as an important therapeutic agent and has been validated to target diabetes and obesity. Fungi, in general, produce secondary metabolites with some amazing chemical and structural diversity and are recognized to be a valuable source for therapeutic molecules. In this review, the focus is on describing the PTP1B effects and their potential as anti-diabetic agents for the various metabolites isolated from fungi.

Yu Zhang,1– 3,* Li Cui,2,* Yizeng Lu,4 Jixiang He,5 Hidayat Hussain,6 Lei Xie,4 Xuan Sun,2 Zhaoqing Meng,7 Guiyun Cao,7 Dawei Qin,1 Daijie Wang2,3 1School of Chemistry and Chemical Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250353, People’s Republic of China; 2School of Pharmaceutical Sciences and Key Laboratory for Applied Technology of Sophisticated Analytical Instruments of Shandong Province, Shandong Analysis and Test Center, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250014, People’s Republic of China; 3Biological Engineering Technology Innovation Center of Shandong Province, Heze Branch of Qilu University of Technology (Shandong Academy of Sciences), Heze, 274000, People’s Republic of China; 4Shandong Provincial Center of Forest and Grass Germplasm Resources, Jinan, 250102, People’s Republic of China; 5School of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, 250353, People’s Republic of China; 6Department of Bioorganic Chemistry, Leibniz Institute of Plant BioChemistry, Halle, D-06120, Germany; 7Shandong Hongjitang Pharmaceutical Group Co., Ltd., Jinan, 250103, People’s Republic of China*These authors contributed equally to this workCorrespondence: Dawei Qin, School of Chemistry and Chemical Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250353, People’s Republic of China, Tel/Fax +86 53189631208, Email qdw@qlu.edu.cn Daijie Wang, Biological Engineering Technology Innovation Center of Shandong Province, Heze Branch of Qilu University of Technology (Shandong Academy of Sciences), Heze, 274000, People’s Republic of China, Tel +86 53182605319, Fax +86 53182964889, Email wangdaijie@qlu.edu.cnBackground: The leaves of L. japonica (LLJ) are widely used as medicine in China. It is rich in caffeoylquinic acids, flavonoids and iridoid glycosides and has strong reducing capacities. Therefore, it can be used as a green material to synthesize silver nanoparticles.Methods: LLJ was used as a reducing agent to produce the LLJ-mediated silver nanoparticles (LLJ-AgNPs). The structure and physicochemical properties of LLJ-AgNPs were characterized by ultraviolet spectroscopy (UV-Vis), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and x-ray powder diffraction (XRD). Antioxidant activity of LLJ-AgNPs was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging. Antibacterial activity was determined by 96 well plates (AGAR) gradient dilution, while the anticancer potential was determined by MTT assay.Results: The results showed LLJ-AgNPs had a spherical structure with the maximum UV-Vis absorption at 400 nm. In addition, LLJ-AgNPs exhibited excellent antioxidant properties, where the free radical scavenging rate of LLJ-AgNPs was increased from 39% to 92% at concentrations from 0.25 to 1.0 mg/mL. Moreover, LLJ-AgNPs displayed excellent antibacterial properties against E. coli and Salmonella at room temperature, with minimum inhibitory values of 10− 6 and 10− 5 g/L, respectively. In addition, the synthetic LLJ-AgNPs exhibited a better inhibition effect in the proliferation of cancer cells (HepG2, MDA-MB − 231, and Hela cells).Conclusion: The present study provides a green approach to synthesize LLJ-AgNPs. All those findings illustrated that the produced LLJ-AgNPs can be used as an economical and efficient functional material for further applications in food and pharmaceutical fields.Keywords: leaves of Lonicera japonica Thunb, LLJ-AgNO3-NPs, green approach, antioxidant, antibacterial, anticancer

Frankincense (This inclusive review focuses on the significance of frankincense diterpenoids, and in particular, incensole derivatives for establishment future treatments of depression, neurological disorders, and cancer. The authors survey the available literature and furnish an overview of future perspectives of these intriguing molecules.Numerous diterpenoids including cembrane, prenylaromadendrane, and the verticillane-type have been isolated from various

Activating mutations in FLT3 receptor tyrosine kinase are found in a third of acute myeloid leukemia (AML) patients and are associated with disease relapse and a poor prognosis. The majority of these mutations are internal tandem duplications (ITDs) in the juxtamembrane domain of FLT3, which have been validated as a therapeutic target. The clinical success of selective inhibitors targeting oncogenic FLT3, however, has been limited due to the acquisition of drug resistance. Herein the identification of a dual FLT3/microtubule polymerization inhibitor, chalcone 4 (2'-allyloxy-4,4'-dimethoxychalcone), is reported through screening of 15 related chalcones for differential antiproliferative activity in leukemia cell lines dependent on FLT3-ITD (MV-4-11) or BCR-ABL (K562) oncogenes and by subsequent screening for mitotic inducers in the HCT116 cell line. Three natural chalcones (1-3) were found to be differentially more potent toward the MV-4-11 (FLT3-ITD) cell line compared to the K562 (BCR-ABL) cell line. Notably, the new semisynthetic chalcone 4, which is a 2'-O-allyl analogue of the natural chalcone 3, was found to be more potent toward the FLT3-ITD+ cell line and inhibited FLT3 signaling in FLT3-dependent cells. An in vitro kinase assay confirmed that chalcone 4 directly inhibited FLT3. Moreover, chalcone 4 induced mitotic arrest in these cells and inhibited tubulin polymerization in both cellular and biochemical assays. Treatment of MV-4-11 cells with this inhibitor for 24 and 48 h resulted in apoptotic cell death. Finally, chalcone 4 was able to overcome TKD mutation-mediated acquired resistance to FLT3 inhibitors in a MOLM-13 cell line expressing FLT3-ITD with the D835Y mutation. Chalcone 4 is, therefore, a promising lead for the discovery of dual-target FLT3 inhibitors.

A new a bisflavan-3-ol, boerhavianane (1), was isolated from Boerhavia elegans L. The structure of the flavanol dimer was elucidated by detailed spectroscopic analysis including 1H, 13C NMR, COSY, HMQC, HMBC, and ESI-MS. Boerhavianane (1) was evaluated for its anticancer activity and demonstrated a significant reduction in the viability of breast cancer cells in a concentration-dependent manner with an IC50 value of 38.48 μg/mL. Moreover, boerhavianane (1) was also screened for DPPH antioxidant activity and acetyl cholinesterase, xanthine oxidase, urease, and α-glucosidase enzyme inhibition activities. Preliminary results showed that it exhibited significant inhibition (81.0 ± 2.0%) against urease enzyme, whereas for DPPH radical scavenging it showed moderate activity (75.0 ± 1.5%).

This mini review describes the research between 1962 and 2019 on ethnobotany, chemistry and pharmacology of Harungana madagascariensis (Hypericaceae), the unique plant species in the genus Harungana. The plant is mainly distributed in Africa and Europe, where it has been used in the traditional medicine to cure several diseases. The first chemical investigation of H. madagascariensis genus took place earlier in 1962 with the isolation of harunganin whose the structure was characterized by X-ray. Several works have been done over the last 57 years on leaves, bark, roots and branches of the plant and as result, 42 secondary metabolites belonging to numerous classes of compounds including anthranoids, anthraquinones, xanthones, triterpenoids, flavonoids, steroids and alkaloids have been isolated and are presented herein together with some derivatives obtained from chemical transformations including thermal rearrangement and allylation. The anthranoids reported from natural sources represent almost 49 % of the total secondary metabolites obtained from the genus and display the most potent biological activities. Along with anthraquinones, they constitute the chemo markers of Harungana. The extracts and compounds from the plant have been evaluated for their potencies in antimicrobial, anti-protozoan, anti-sickling, anti-inflammatory, antioxidant, enzyme inhibition or cytotoxic activities. The results support the uses of H. madagascariensis in folk medicine and provide further evidence in new drugs discovery.

Understanding the impacts and constraints of climate change on Ziziphus nummularia′s geographical distribution is crucial for its future sustainability. In this study, we analyze information obtained from the field investigation, the distribution and response of climatic changes of Ziziphus nummularia by the use of ArcGIS analysis. The genetic diversity of 180 genotypes from three populations was studied by morphological attributes and simple sequence repeat (SSR). The results showed that the significant bioclimatic variable limiting the distribution of Z. nummularia was the mean temperature (bio 10_18.tif and bio19). Under the current climatic change, the suitable growth region of Z. nummularia is Swat (35.22° N, 72.42° E), while the future distribution would be Buner (34.39° N, 72.61° E), respectively. A total of 11 phenotypic traits were noted and had significant phenotypic variation among the traits. A total of 120 alleles were amplified. The alleles per locus ranged from 2 to 6, averaging 4.42, whereas PIC ranged from 0.33 to 0.79. Within a mean value of 0.67 per locus, expected heterozygosity was 0.57, observed heterozygosity was 0.661, and average gene diversity was 0.49. Flow estimates (6.41) indicated frequent gene flow within genotypes. The clustering, STRUCTURE, and PCoA analysis indicated Swat and Buner migration routes and evolution as well. The results indicated the prevalence of genetic variability and relationships among Z. nummularia across geographical boundaries had retained unique alleles. This may facilitate the development of agronomically desirable cultivars. However, climate change has impacted species distributions, requiring strategies to conserve genetic resources in different areas.

Green synthesis of silver nanoparticles (AgNPs) employing an aqueous plant extract has emerged as a viable eco-friendly method. The aim of the study was to synthesize AgNPs by using plant extract of Sanvitalia procumbens (creeping zinnia) in which the phytochemicals present in plant extract act as a stabilizing and reducing agent. For the stability of the synthesized AgNPs, different parameters like AgNO3 concentration, volume ratios of AgNO3, temperature, pH, and contact time were studied. Further, AgNPs were characterized by UV–visible spectroscopy, FT-IR (Fourier Transform Infrared Spectroscopy), XRD (X-ray Diffraction), SEM (Scanning Electron Microscopy), and EDX (Energy Dispersive X-ray Spectrometer) analysis. FT-IR analysis showed that the plant extract contained essential functional groups like O–H stretching of carboxylic acid, N–H stretching of secondary amides, and C–N stretching of aromatic amines, and C–O indicates the vibration of alcohol, ester, and carboxylic acid that facilitated in the green synthesis of AgNPs. The crystalline nature of synthesized AgNPs was confirmed by XRD, while the elemental composition of AgNPs was detected by energy dispersive X-ray analysis (EDX). SEM studies showed the mean particle diameter of silver nanoparticles. The synthesized AgNPs were used for photocatalytic degradation of Orange G and Direct blue-15 (OG and DB-15), which were analyzed by UV-visible spectroscopy. Maximum degradation percentage of OG and DB-15 azo dyes was observed, without any significant silver leaching, thereby signifying notable photocatalytic properties of AgNPs.

The antioxidant and enzyme inhibitory potential of fifteen cycloartane-type triterpenes’ potentials were investigated using different assays. In the phosphomolybdenum method, cycloalpioside D (6) (4.05 mmol TEs/g) showed the highest activity. In 1,1-diphenyl-2-picrylhydrazyl (DPPH*) radical and 2,2′-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS) cation radical scavenging assays, cycloorbicoside A-7-monoacetate (2) (5.03 mg TE/g) and cycloorbicoside B (10) (10.60 mg TE/g) displayed the highest activities, respectively. Oleanolic acid (14) (51.45 mg TE/g) and 3-О-β-d -xylopyranoside-(23R,24S)-16β,23, 16α,24-diepoxycycloart-25(26)-en-3β,7β-diol 7-monoacetate (4) (13.25 mg TE/g) revealed the highest reducing power in cupric ion-reducing activity (CUPRAC) and ferric-reducing antioxidant power (FRAP) assays, respectively. In metal-chelating activity on ferrous ions, compound 2 displayed the highest activity estimated by 41.00 mg EDTAE/g (EDTA equivalents/g). The tested triterpenes showed promising AChE and BChE inhibitory potential with 3-О-β-d-xylopyranoside-(23R,24S)-16β,23, 16α,24-diepoxycycloart-25(26)-en-3β,7β-diol 2′,3′,4′,7-tetraacetate (3), exhibiting the highest inhibitory activity as estimated from 5.64 and 5.19 mg GALAE/g (galantamine equivalent/g), respectively. Compound 2 displayed the most potent tyrosinase inhibitory activity (113.24 mg KAE/g (mg kojic acid equivalent/g)). Regarding α-amylase and α-glucosidase inhibition, 3-О-β-d-xylopyranoside-(23R,24S)-16β,23, 16α,24-diepoxycycloart-25(26)-en-3β,7β-diol (5) (0.55 mmol ACAE/g) and compound 3 (25.18 mmol ACAE/g) exerted the highest activities, respectively. In silico studies focused on compounds 2, 6, and 7 as inhibitors of tyrosinase revealed that compound 2 displayed a good ranking score (−7.069 kcal/mole) and also that the ΔG free-binding energy was the highest among the three selected compounds. From the ADMET/TOPKAT prediction, it can be concluded that compounds 4 and 5 displayed the best pharmacokinetic and pharmacodynamic behavior, with considerable activity in most of the examined assays.

A silver ion high-speed counter-current chromatography ([Ag+]-HSCCC) was developed to separate and purify five sesquiterpenoids from germacrene A fermentation broth. The solvent system was consisted of n-hexane-methanol-silver nitrate (3 mol/L) solution (10:9.5:0.5, v/v). By employing this chromatographic protocol, five sesquiterpenoids named β-elemene (1, 54.1 mg), germacrene A (2, 28.5 mg), γ-selinene (3, 4.6 mg), β-selinene (4, 3.4 mg), and α-selinene (5, 1.3 mg) were obtained successfully from 500 mg extracted crude sample with purities of 97.1%, 95.2%, 98.2%, 96.3% and 98.5%, respectively, combined with preparative HPLC. The results reveal that the addition of metal ion in biphasic solvent system significantly improved the HSCCC separation factor of sesquiterpenoids. Meanwhile, our study also provided an alternate approach to separate the compounds with less polarity, also geometrical isomers and various natural product classes.

Lectins are unique glycoproteins that react with specific sugar residues on cell surfaces resulting in agglutination. They offer enormous applications in therapeutics, diagnostics, medicine, and agriculture. Rice lectins are naturally expressed during biotic and abiotic stresses suggesting their importance in stress resistance physiology. The objective of this study was to determine the presence and relative concentration of lectins in different accessions of rice obtained from IABGR/NARC Islamabad mainly originated from Pakistan. About 210 rice accessions including 02 local varieties and 05 transgenic seeds were screened for seed lectins using a hemagglutination (HA) assay with 5% Californian bred rabbits’ erythrocytes. A protein concentration of 3–8 mg/100 mg of seed flour was measured for all the rice accessions, the highest was 8.03mg for accession 7600, while the lowest noted was 3.05 mg for accession 7753.Out of 210 accessions, 106 showed the highest HA activity. These 106 genotypes were further screened for titer analysis and specific activity. The highest titer and specific activity were observed for accession 7271 as 1024 and 236 hemagglutination unit (HAU), respectively. The selected accessions’ relative affinity and HA capability were evaluated using blood from four different sources: human, broiler chicken, local rabbit, and Californian-breed rabbit. The highest HA activity was observed with Californian-breed rabbit RBCs. The lectin assay was stable for about 1–2 h. After the required investigations, the accessions with higher lectin concentration and HA capability could be used as a readily available source of lectins for further characterization and utilization in crop improvement programs.

Chemical investigation of the aerial parts of

Multi-walled carbon nanotubes (MWCNTs) and graphene oxide (GO) reinforced carbon foam (CF) composite were prepared by direct pyrolysis of MWCNTs, GO and mesophase coal tar pitch. The effect of additive amount of the mixture of MWCNTs and GO on the microstruture and properties of carbon foam was analzyed by transmission electron miscroscopy (TEM), scanning electron microscopy (SEM), X-ray diffraction (XRD), Four-probe resistance meter, universal testing machine, and laser thermal conductivity tester respectively. The result shows that MWCNTs and GO had significant impact on the microstructure of carbon foam. Futhermore, the electrical, mechanical and thermal properties of carbon foam composites were significantly enhanced by increasing the additive amount. Maximum compressive strenght of 19.2 MPa and Young’s modulus of 56.8 MPa of CF composite were observed. Similarly, Highest thermal conductivity of 30.91 W/m.K and electrical conductivity of 27.2 ×103 S/m were observed at 2 wt. % of MWCNTs-GO additive loading.

Introduction Oleanane-type pentacyclic triterpenes named glycyrrhetinic acids (GAs) featuring a C-30 carboxylic acid group, are extracted from the licorice (Glycyrrhiza uralensis). Numerous biological properties of GA have been reported and have attracted researchers from all over the world in recent years due to the peculiar GA scaffold-based semisynthetic cytotoxic effects. Areas covered This review represents the applications of semisynthetic derivatives of GA for the development of future cancer treatments. Included in the review are important structural features of the semisynthetic GAs crucial for cytotoxic effects. Expert opinion Numerous semisynthetic GA derivatives illustrated excellent cytotoxic effects toward various cancer cells. Notably the C-3(OH) at ring A along with C30-CO2H at ring E as vital structural features, make GA very appealing as a lead scaffold for medicinal chemistry, since these two groups permit the creation of further chemical diversity geared toward improved cytotoxic effects. Furthermore, numerous GA derivatives have been synthesized and indicate that compounds featuring cyanoenone moieties in ring A, or compounds having the amino group or nitrogen comprising heterocycles and hybrids thereof, illustrate more potent cytotoxicity. Furthermore, GA has a great capability to be conjugated with other anticancer molecules to synergistically enhance their combined cytotoxicity.

Investigation on medicinal plants' therapeutic potential has gained substantial importance in the discovery of novel effective and safe therapeutic agents. The present study is aimed at investigating the hepatoprotective potential of Seriphidium kurramense methanolic extract (SKM) against carbon tetrachloride- (CCl4-) induced hepatotoxicity in rats. S. kurramense is one of the most imperative plants for its various pharmacological activities. Therefore, this study was aimed at evaluating the hepatoprotective potential against CCl4-induced liver toxicity. The serum samples were analyzed for alanine aminotransferase (ALT) and aspartate aminotransferase (AST) together with the oxidative stress mediator levels as nitric oxide (NO), malondialdehyde (MDA), glutathione (GSH), reduced glutathione (GSH), and superoxide dismutase (SOD) as well as peroxidation and H2O2 activity. CCl4 administration resulted in an elevated free radical generation, altered liver marker (AST and ALT) enzymes, reduced antioxidant enzyme, and increased DNA damage. Methanolic extract of S. kurramense decreased CCl4-induced hepatotoxicity by increasing the antioxidant status and reducing H2O2 and nitrate content generation as well as reducing DNA damage. Additionally, SKM reversed the morphological alterations induced by CCl4 in the SKM-treated groups. These results demonstrated that SKM displayed hepatoprotective activity against CCl4-induced hepatic damage in experimental rats.

The foraging and consumption of wild food plants is a long-standing tradition in many parts of the world and their importance in promoting food security has become more widely debated in recent years. The current study aimed to document, analyze, and interpret the traditional knowledge of non-cultivated vegetables among four Pathan tribes (Alisher Khel, Hadarzai, Haji Khel, and Umarzai) living in the Gadoon Valley, Swabi District, Khyber Pakhtunkhwa, NW Pakistan, and to evaluate how these practices vary among the considered tribal communities. A total of 104 informants were interviewed via a semi-structured, open-ended questionnaire and group discussions. The field survey was conducted from October 2018 to November 2020. Information about local names, growth habit, used plant parts, food/cooking details, medicinal perceptions, availability season, and market prices were collected. The field survey recorded 51 non-cultivated vegetables belonging to 24 botanical families, for which the frequently used plant parts included young leaves, stems, and flowers. The greatest number of use reports was recorded for Colocasia and the highest cultural index value was recorded for Rumex dentatus, the dominant botanical families were Asteraceae and Fabaceae (six species each). Seven species were found to be sold at local and regional markets. Cross-cultural analysis among the four considered tribes showed that the largest number of species was reported by members of the Hadarzai and Umarzai tribes, although most of the quoted wild vegetables were homogenously gathered among all considered communities, with some more idiosyncratic plant uses among the Umarzai group, who have likely been less affected by the erosion of traditional knowledge or possibly have had less access to traded cultivated vegetables. The novelty of the data was assessed by comparing it with the previously published wild food ethnobotanical literature of Pakistan, which showed fifteen new wild vegetables not yet reported in the NW of the country. The recorded food biocultural heritage should be seriously considered in future local development projects aimed at fostering environmental sustainability and food security.

Multicomponent reactions, especially the Ugi-four component reaction (U-4CR), provide powerful protocols to efficiently access compounds having potent biological and pharmacological effects. Thus, a diverse library of betulinic acid (BA), fusidic acid (FA), cholic acid (CA) conjugates with TEMPO (nitroxide) have been prepared using this approach, which also makes them applicable in electron paramagnetic resonance (EPR) spectroscopy. Moreover, convertible amide modified spin-labelled fusidic acid derivatives were selected for post-Ugi modification utilizing a wide range of reaction conditions which kept the paramagnetic center intact. The nitroxide labelled betulinic acid analogue 6 possesses cytotoxic effects towards two investigated cell lines: prostate cancer PC3 (IC50 7.4 ± 0.7 μM) and colon cancer HT29 (IC50 9.0 ± 0.4 μM). Notably, spin-labelled fusidic acid derivative 8 acts strongly against these two cancer cell lines (PC3: IC50 6.0 ± 1.1 μM; HT29: IC50 7.4 ± 0.6 μM). Additionally, another fusidic acid analogue 9 was also found to be active towards HT29 with IC50 7.0 ± 0.3 μM (CV). Studies on the mode of action revealed that compound 8 increased the level of caspase-3 significantly which clearly indicates induction of apoptosis by activation of the caspase pathway. Furthermore, the exclusive mitochondria targeting of compound 18 was successfully achieved, since mitochondria are the major source of ROS generation.

Background: Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects. Objective: his review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products. Methods: The date about the published patents was downloaded via online open access patent databases. Results: Cucurbitacins display significant cytotoxic properties, in particular cucurbitacins B and D which possess very potent effects towards a number of cancer cells. Numerous cucurbitacins isolated from natural sources have been derivatized through chemical modification at the C(2)-OH and C(25)- OH groups. Most importantly, an acyl ester of the C(25)-OH and, iso-propyl, n-propyl and ethyl ether groups of the C(2)-OH demonstrated the most increased cytotoxic activity. Conclusion: The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.

Oxidative stress is often considered detrimental for cellular processes and damaging for the lipid bi-layer. Counteracting such stresses with the aid of nature-based chemical constituents can be an ideal therapeutic approach. The current study aimed to investigate the chemical constituents of resins derived from the well-known Aloe vera and less known Commiphora mukul trees and their effect in mitigating the lipid peroxidation (LPO) process. The bio-guided isolation of bio-active fractions from both resins afforded 20 chemical constituents (17 from A. vera and 3 from C. mukul). These compounds belonged to anthraquinones, anthraquinone glycosides, quinones, coumarins, polypodane-type terpenoids and benzene derivatives. Major chemical constituents of the resins of A. vera and C. mukul were from the classes of quinones and terpenoids. Feroxidin (4, from A. vera) showed slightly higher inhibition (IC 50 = 201.7 ± 0.9 µmol L−1) than myrrhanone C (18, from C. mukul: IC 50 = 210.7 ± 0.0 µmol L−1) and methyl 3-(4-hydroxyphenyl) propionate from A. vera (13, IC 50 = 232.9 ± 0.2 µmol L−1) compared to the other compounds. Structure-activity relationship showed that the existence of hydroxyl, methoxy and ether groups might play a major role in countering oxidative stress. To the best of our knowledge, anti-LPO activities of compounds 1–4, 14, 18 and 20 are reported for the first time. Such chemical constituents with high anti-lipid peroxidation activity could be helpful in synthesizing candidate drugs.

Diabetes mellitus is a chronic metabolic disorder which is rapidly spreading worldwide. It is characterized by persistent elevated blood glucose level above normal values (hyperglycemia) due to defect in either insulin secretion or in insulin action or both of them. Currently approved oral synthetic antidiabetic drugs such as biguanides, thiazolidinediones, sulfonylureas, and meglitinides have shown undesirable side effects. Therefore, newer approaches and targets for the management of diabetes mellitus are highly desirable. Dipeptidyl peptidase-4 enzyme, α-glucosidase enzyme and sodium-dependent glucose co-transporter 2 (SGLT2) have been recognized as effective therapeutic targets for the management of diabetes mellitus while natural products are alternatives to oral synthetic hypoglycemic agents. During the last two decades, many researchers were working on the identification and the validation of plant-derived products for curing various diseases. Natural products do not only provide useful drugs in their own right but also provide templates for the development of more effective compounds for enhanced therapeutic potential. Herein, we advocated the vital role of natural products as source of new drugs by presenting promising inhibitors of dipeptidyle peptidase-4 enzyme, α-glucosidase enzyme and (SGLT2) obtained from different medicinal plants as potential candidates for drug development against diabetes mellitus. The structure-activity relationship (SAR) of these various inhibitors is also discussed.

Nanomaterials have been shown to possess exclusive properties in heterogeneous catalysis as evidenced by studies dedicated to the synthesis of transition-metal-containing nanomaterials. However, the series of nanomaterials which have been synthesized are mostly oxides. A ligand, 1-(2-chloro-4-nitrophenyl)-3,3-chlorobenzoyl (Tu), has been created through which MnS nanoparticles (NPs) and nanosheets (NSs) have been successfully synthesized, initially from a single-source precursor (SS) and then from multi-source precursors, respectively. The main objective of this article was to identify the differences in the morphologies of the materials synthesized from the two different sources, with photodegradation and battery applications performed just with MnS NPs (synthesized by the SS method). A preliminary study has been carried out on the photocatalytic properties and battery applications of the recently synthesized MnS employing the SS method. MnS NPs demonstrated higher activity than their bulk sheet for the photocatalytic degradation of four different dyes, methyl violet, methylene green, methylene blue, and rhodamine B, under visible-light irradiation. More significantly, the preparation method in the present work might be applied to other metal chalcogenide nanomaterials for various new applications. More notably, battery applications have been evaluated for MnS NPs (synthesized by the SS method) by testing their electrochemical discharge/charge at voltage limits of − 0.2 to 3.2 V versus Li/Li+.

Gold is considered as an inert metal and ranks as one of the noblest among all the metals. Progressive importance associated with nanotechnology offers potential development of new methods and cont...

A new flavonoid glycoside, named desmiflavanoside (1), was isolated from the MeOH extract of Desmidorchis flava (N.E.Br.) Meve & Liede, and its structure was elucidated based on 1D and 2D NMR spectroscopic techniques as well as mass spectrometry. Preliminary studies demonstrated that although compound 1 is moderately cytotoxic at lower concentrations, its activity plateaus at higher concentrations. Notably, compound 1 demonstrated a significant dose-dependent response to lipid peroxidation and that its antilipid peroxidation was similar (89.6 ± 0.81%) to the known standard (BHT; 91.3 ± 0.49%; p < 0.051). On the other hand, the flavone glycoside 1 did not show inhibitory effects against urease and acetylcholinesterase enzymes.

CdS nanoparticles (CdS NPs) and CdS nanoslabs (CdS NSs) were synthesized from the single source (SS) and multi-source (MS) precursors, respectively. Our target was to observe any change in morphology by altering the synthetic route. CdS NPs with spherical morphology (0.2–0.5 µm in diameter) were obtained by using the SS precursor route via the formation of a Cd-complex. CdS NSs (100–200 nm in length, 50–100 nm wide and 25–50 nm in thickness) were obtained by using the MS precursors, by direct addition of the ligand to metal salt. Both NPs and NSs were used for the degradation of four different cationic organic dyes viz., malachite green (MG), methylene blue (MB), rhodamine B (RhB) and methyl violet (MV) under visible light. CdS NPs synthesized from SS precursor exhibited higher photocatalytic activity than CdS NSs fabricated via MS precursor due to spherical morphologies (small size of particles increases the surface area) and higher band gap. On the other hand, CdS NSs show sheet or cube like morphologies. The kinetic study proved that the rate constants for the MG, MB, MV, and RhB degradation by CdS NPs (1.65 × 10–2, 1.25 × 10–2, 1.2 × 10–2, and 1.24 × 10–2 min–1, respectively) are higher than those for CdS NSs (1.45 × 10–2, 1.13 × 10–2, 1.05 × 10–2, 1.14 × 10–2 min–1, respectively). The precursors were characterized by 1H and 13C nuclear magnetic resonance. Phase pattern and composition of CdS were confirmed by X-ray diffraction and energy dispersive X-ray spectroscopy. Morphology and size were confirmed by transmission electron microscopy and scanning electron microscopy.

Nepeta adenophyta Hedge (Lamiaceae) is an endemic therapeutic herb from Astore, Gilgit (Pakistan). This plant species has been reported among the local communities, especially for treating abdominal pain, kidney pain, menstrual pain, headache, and controlling bleeding disorders. Therefore, the scientific basis is provided for the relief of pain as it is used in various pain management among the natives, especially as ethnogynecological herbal remedy.The present study investigates the analgesic and anti-inflammatory effects of the ethanolic extract of N. adenophyta in animal models. Furthermore, the extract was also studied to determine their valuable phytoconstituents.The biological effects were determined via tail-flick, hot plate, and acetic-acid-induced abdominal writhing methods. At the same time, anti-inflammatory activity was assesed via oxidative burst and antioxidant DPPH assay. Gas chromatography-mass spectrometry (GC-MS), and liquid chromatography-mass spectrometry (LC-MS) techniques were employed to understand the phytochemicals present in the crude ethanolic extract of Nepeta adenophyta.In the current study, Nepeta adenophyta extract exhibited potent analgesic and anti-inflammatory effects on different pain models and indicated that the analgesic effect of N. adenophyta extract is mediated both in central and peripheral ways. Dose-dependent and significant (P 0.05) increases were shown in pain threshold, at 45 min post-treatment, with 20 and 40 mg/kg of the extract in the tail-flick model. The effects of the extract were similar to aspirin but lower to those by morphine (2.5 mg/kg) in the same tests. The extract (20-40 mg/kg) showed dose-dependent inhibition of writhing with a significant (P 0.001) increase protection against thermal stimuli in hot plate test as compared to control and similar to aspirin and morphine. Further, the anti-inflammatory activity of the crude in oxidative burst and DPPH assays showed significant inhibitory activity. The chemical profile analysis showed major phytochemicals, including long chain derivatives of alkane and alcohol, phenolics, naphthalene, naphthopyran, androsten phenanthrenone, nepetalactones, flavonoids etc. CONCLUSIONS: Nepeta adenophyta Hedge is suggested as a natural alternative for mild pain relief. Our findings endorse the folklore use of N. adenophyta in different pain managements which can be attributed to the presence of polyphenolic compounds, naphthalene derivatives, flavanoids and nepetalactones etc.

Pleurospermum (Apiaceae) species possess a wide range of biological properties viz. analgesic, anti-inflammatory, and antimalarial etc. Pleurospermum candollei (DC.) Benth. Ex C. B. Clark. is reported to cure diarrhea, gastric, respiratory, stomach, abdominal, joint and back pain problems. In addition, it is also used for both male and female infertility. The present study deals with an efficient technique using high-speed counter-current chromatography for separation of chemical components from the methanol extract of P. candollei. Notably, nine main compounds namely luteolin 7-O-glucoside (1), oxypeucedanin hydrate (2), pabulenol (3), bergapten (4), heptadecanoic acid (5), (E)-isoelemicin (6), trans-asarone (7), α-linolenic acid (8), and isoimperatorin (9) were very efficiently separated and isolated in pure form. Multiple injections were applied followed by two off-line recycling high-speed counter-current chromatography. The inhibitory effect of nitric oxide production of all compounds was tested in the presence of 200 ng/mL lipopolysaccharide in RAW264.7 mice macrophage cells. The results demonstrated that compounds 7 and 8 effectively inhibited nitric oxide production, with IC50 values of 28.44 and 53.18 μM, respectively. This study thus validates the traditional claim of using P. candollei. Taken together, these findings will be useful in future research to find a potential candidate with anti-inflammatory properties. This article is protected by copyright. All rights reserved.

In the present work, carbon foam (CF) coupled multi-wall carbon nanotubes (MWCNTs) and CF/MWCNTs coupled nanodiamond (NDs) hybrid composites were prepared by the direct treatment of MWCNTs and NDs with pretreatment pitches through foaming, graphitization, and carbonization process. Both series of CF composites were compared and explored by Fourier-transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy and energy dispersive X-ray spectroscopy techniques. It was investigated that the structural morphology, pore size and pore uniformity upgraded with the increment of MWCNTs content, however, the effect of ND particles in this aspect was more influential. Furthermore, the effect of additive loading of MWCNTs and NDs on the mechanical, electrical and thermal properties of CF composites were checked. The results revealed that maximum compressive strength 15.8 MPa and electrical conductivity 30.2×103 S/m of CFs were obtained at 4 wt.% MWCNTs and ND loadings respectively. While the maximum thermal conductivity value of 32.2 Wm-1k-1 was revealed by CFs having 2 wt.% MWCNTs and NDs loadings.

In this study, nano-TiO2 sulfonated (STiO2) with 1,3-propanesultone was incorporated into the chitosan matrix for the fabrication of chitosan/STiO2 (C/STiO2) nanocomposite membranes. The grafting of sulfonic acid (–SO3H) groups was confirmed with Fourier transform infrared spectroscopy, thermos-gravimetric analysis and energy-dispersive X-ray spectroscopy. The physicochemical properties such as water uptake, swelling ratio, thermal and mechanical stability, ion exchange capacity and proton conductivity of the as prepared membranes were measured. The proton groups on the surface of TiO2 can form continuous proton conducting pathways along the C/STiO2 interface resulting in the improvement of proton conductivity of C/STiO2 nanocomposite membranes. The nanocomposite membrane with 5 % sulfonated TiO2 showed higher proton conductivity (0.035 S·cm-1) than commercial Nafion-117 membrane (0.033 S·cm-1) due to the strong interfacial interactions between -SO3H group of acid and hydroxyl group of TiO2. Further, the –NH2 groups of chitosan restrict the mobility of chitosan chains to enhance the thermal and mechanical stability of the nanocomposite membranes. These C/STiO2 nanocomposite membranes have promising applications in proton exchange membrane fuel cells.

Phytochemical investigation of the methanolic extract obtained from the aerial parts of Lagochilus setulosus (Lamiaceae) afforded the new compound 1-methoxy-3-O-β-glucopyranosyl-α-l-oliose (1) together with five known glycosides, namely sitosterol-3-O-β-glucoside (2), stigmasterol-3-O-β-glucoside (3), pinitol (4), 6β-hydroxyl-7-epi-loganin (5), and chlorotuberoside (6). The structures of these compounds were elucidated by extensive spectroscopic analyses, especially HR-MS, 1D and 2D NMR spectroscopy. The in vitro cytotoxic activity of the methanolic extract and the isolated compounds was assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and crystal violet (CV) staining assays. In addition, the antifungal activities of the components were evaluated against Botrytis cinerea, Septoria tritici, and Phytophthora infestans. The anthelmintic potential was determined against Caenorhabditis elegans nematodes. Neither the extract nor the isolated compounds showed promising activity in all the bioassays.

Investigation on medicinal plants’ therapeutic potential has gained substantial importance in the discovery of novel effective and safe therapeutic agents. The present study is aimed at investigating the hepatoprotective potential of Seriphidium kurramense methanolic extract (SKM) against carbon tetrachloride- (CCl4-) induced hepatotoxicity in rats. S. kurramense is one of the most imperative plants for its various pharmacological activities. Therefore, this study was aimed at evaluating the hepatoprotective potential against CCl4-induced liver toxicity. The serum samples were analyzed for alanine aminotransferase (ALT) and aspartate aminotransferase (AST) together with the oxidative stress mediator levels as nitric oxide (NO), malondialdehyde (MDA), glutathione (GSH), reduced glutathione (GSH), and superoxide dismutase (SOD) as well as peroxidation and H2O2 activity. CCl4 administration resulted in an elevated free radical generation, altered liver marker (AST and ALT) enzymes, reduced antioxidant enzyme, and increased DNA damage. Methanolic extract of S. kurramense decreased CCl4-induced hepatotoxicity by increasing the antioxidant status and reducing H2O2 and nitrate content generation as well as reducing DNA damage. Additionally, SKM reversed the morphological alterations induced by CCl4 in the SKM-treated groups. These results demonstrated that SKM displayed hepatoprotective activity against CCl4-induced hepatic damage in experimental rats.

International audience; Breast cancer is known as the most devastating cancer in the global female community and is considered as one of the severe health care burdens in both developed and developing countries. In many cases, breast cancer has shown resistance to chemotherapy, radiotherapy and hormonal therapy. Keeping in view these limitations, there is an urgent need to develop safe, readily available and effective breast anticancer treatments. Therefore, the scientists are keen in the extraction of plant-based phytochemicals (organosulfur compounds, betalains, capsaicinoids, terpenes, terpenoids, polyphenols, and flavonoids) and using them as breast anticancer agents. Results of numerous epidemiological investigations have revealed the promising role of phytochemicals in the prevention and treatment of breast cancer. The diverse classes of plant bioactive metabolites regulate different metabolic and molecular processes, which can delay the proliferation of cancers. These phytochemicals possess chemo-preventive properties as they down-regulate the expression of estrogen receptor-a, inhibit the proliferation of cancer cells, and cause cell cycle arrest by inducing apoptotic conditions in tumor cells. This review article discusses the potent role of various plant-based phytochemicals as potential therapeutic agents in the treatment or prevention of breast cancer along with the proposed mechanisms of action.

The genus Lagochilus (Lamiaceae) is native to Central, South-Central, and Eastern Asia. It comprises 44 species, which have been commonly used as herbal medicines for the treatments of various ailments for thousands of years, especially in Asian countries. This review aims to summarize the chemical constituents and pharmacological activities of species from the genus Lagochilus to unveil opportunities for future research. In addition, we provide some information about their traditional uses, botany, and diversity. More than 150 secondary metabolites have been reported from Lagochilus, including diterpenes, flavonoids, phenolic compounds, triterpenoids, iridoid glycosides, lignans, steroids, alkaloids, polysaccharides, volatile, non-volatile and aromatic compounds, lipids, carbohydrates, minerals, vitamins, and other secondary metabolites. In vitro and in vivo pharmacological studies on the crude extracts, fractions, and isolated compounds from Lagochilus species showed hemostatic, antibacterial, anti-inflammatory, anti-allergic, cytotoxic, enzyme inhibitory, antispasmodic, hypotensive, sedative, psychoactive, and other activities.

Diabetes, a metabolic disorder, is caused by a high blood sugar level. Diabetes is an increasing health issue and search for potent antidiabetic agents is desirable. Owing to its ethnomedicinal value, the Himalayan perennial herb Bergenia stracheyi (Hook. f. & Thoms.) Engl. (Saxifragaceae Juss) is used to treat diabetes. Herein, an efficient high-speed countercurrent chromatography with elution mode is reported for separation of active compounds from B. stracheyi. In current investigation, six main compounds including β-arbutin (1), bergenin (2), 6-O-galloylarbutin (3), gallic acid (4), 11-O-galloylbergenin (5), and (-)-epicatechin 3-O-gallate (6) with above 95% purity were efficiently separated in a single run using biphasic tert-butyl methyl ether/n-butanol/methanol/water (1:3:1:5, v/v/v/v) solvent system. The structures of these compounds were characterized using spectral techniques and compared with the literature. Antidiabetic and antioxidant activities evaluation of the study samples showed that β-arbutin (1) and 6-O-galloylarbutin (3) have a significant protective effect, especially at high dose against hydrogen peroxide induced oxidative injury. Our results might help further in-depth phytochemical and biological evaluation studies in search of potent antidiabetic compounds from B. stracheyi.

The Azadirachta indica, which is commonly known as the neem tree, has gained prominence thanks to its wide spectrum of medicinal properties and its great potential to treat various diseases. In 1992 the US National Academy of Sciences recognized the importance of this plant and declared neem as a tree for solving global problems. The A. indica belongs to the family Meliaceae. It is a fast growing tropical evergreen tree indigenous to the Indo-Pakistan subcontinent since antiquity. The A. indica is also known as a wonder tree due to its richness in bioactive components in all parts of the tree such as the leaves, the bark, the flowers, the fruits, the seeds, the roots, and the gum oil and therefore it is highly exploitable. Over the years, a large number of diverse types of chemical constituents belonging to the various classes of compounds such as flavonoids, alkaloids, triterpenoids, steroids, carotenoids, and ketones, as well as phenolic compounds, have been extracted from the neem plant. The ultimate goal is to promote plant-derived products with the least side effects as modern drugs. In the last few decades, apart from the chemical analysis of the neem compounds, many researchers have investigated the potential of natural products as candidate medications for the treatment of various diseases. As a summary, substantial progress has been made in identifying neem-derived bioactive compounds for the development of medications for the treatment of a wide range of diseases. In this chapter, the major bioactive components of A. indica are presented along with their applications for the cure of many life-threatening diseases.