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One new alkaloid, picrasine A, two new quassinoids, picralactones A-B, together with eleven known compounds were isolated from Picrasma chinensis P.Y. Chen. The structures of these compounds were determined using 1D and 2D NMR, HR-ESI-MS, and IR spectroscopic data, and by comparison with published data. Some compounds were tested for tyrosinase inhibiting activity, however, none of them exhibited strong inhibitory effects., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

Twenty-four new limonoids, toonaolides A-X (1-24), characterized with an α,β-unsaturated-γ-lactone A-ring were isolated from the twigs of Toona ciliata. Their structures and absolute configurations were elucidated by spectroscopic data, X-ray diffraction crystallography, and quantum chemistry calculations. Most of the isolated compounds (except 9, 18, and 24 which possessed the maleimide ring) featured the rare 21-hydroxybutenolide or 23-hydroxybutenolide moieties. In particular, compound 1 has an unprecedented limonoid architecture with 6/6 cis-fused A/B ring system and 2 has an unusual tetrahydrofuran ring B skeleton, featuring a 7/5/6/5 ring system. The biological evaluation showed that compounds 9, 11, 12, 14, and 18 exhibited significantly anti-NLRP3 inflammasome activity with IC 50 values ranging from 3.2 to 9.7 μM. Analysis of IL-1β and caspase-1 expression revealed that compounds 11 and 12 are selective inhibitors of NLRP3 inflammasome, which could ameliorate cell pyroptosis by blocking NLRP3 inflammasome activation., (Copyright © 2020 Elsevier Inc. All rights reserved.)

Objectives: Two labdane diterpenoids, leojapone B and heteronone B, were isolated from Leonurus japonicus Houtt., and their biological activity were evaluated in this study., Methods: Human and mouse cancer cells, human peripheral blood mononuclear cells (PBMCs) and mouse macrophages (RAW264.7 cells) were used to evaluate the activity of leojapone B and heteronone B, while the in vivo effects of leojapone B were further examined in Lewis Lung Cancer tumour-bearing mice., Key Findings: In vitro studies showed that leojapone B selectively inhibited the proliferation of lung cancer cells, and both leojapone B and heteronone B inhibited the production of pro-inflammatory cytokines in activated PBMCs. In tumour-bearing mice model, lung tumours were reduced in size in mice treated with intraperitoneal injections of leojapone B at 20 and 30 mg/kg for 14 days. The population ratio of CD4 + /CD8 + T cells in mouse spleens was found to be increased, while regulatory T cells were decreased after leojapone B treatment., Conclusions: The inhibitory effects of leojapone B in mouse lung tumours were demonstrated for the first time in this study. The immunomodulatory activity of heteronone B were also demonstrated. Our findings indicated that both leojapone B and heteronone B may act as active components in L. japonicus., (© 2020 Royal Pharmaceutical Society.)

Accumulating evidences have proved the protective role of traditional Chinese medicine in improving neurological damage induced by cerebral hypoxia-ischemia. Herein, we hypothesized that Dendrobium officinale aqueous extract exerted neuroprotection against brain damage. Initially, a model of hypoxic-ischemic brain damage (HIBD) was induced in neonatal rats, which were subsequently intragastrically administered with different doses of Dendrobium officinale aqueous extract. Next, the antioxidant capacity was examined by enzyme-linked immunosorbent assay. 2,3,5-Triphenyltetrazolium chloride and terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling staining assays were adopted to determine neuronal apoptosis in brain tissues. Furthermore, neurotrophic factors and hypoxia-inducible factor-1α (HIF-1α) expression was identified by Western blot analysis. The neonatal rat models of HIBD presented impaired neurobehaviors and antioxidant capacity, increased neuronal apoptosis and expression of HIF-1α and histone deacetylase 1 (HDAC1), as well as diminished expression of neurotrophic factors and K + -Cl - -cotransporter 2 (KCC2). Notably, in response to different doses of Dendrobium officinale aqueous extract, the impairment on neurobehaviors and antioxidant capacity was alleviated, accompanied by reduced levels of nitric oxide synthase, nitric oxide, and malondialdehyde, and increased superoxide dismutase activity. Besides, the neuronal apoptosis was inhibited as reflected by down-regulated cleaved caspase-3 and Bax and up-regulated Bcl-2. Moreover, we also found accelerated expression of neurotrophic factors and KCC2 and diminished expression of HIF-1α and HDAC1. Altogether, this present study highlights that the aqueous extract of Dendrobium officinale can suppress the neuronal apoptosis and enhance the expression of neurotrophic factors to protect neonatal rats against HIBD., (© 2019 The Authors. The Kaohsiung Journal of Medical Sciences published by John Wiley & Sons Australia on behalf of Kaohsiung Medical University.)

Phytochemical investigation of the leaves and twigs of Callicarpa cathayana led to the isolation of six new clerodane diterpenoids, cathayanalactones A-F (1-6), together with seven analogues (7-13). Their structures were established by extensive NMR analyses together with experimental and calculated ECD spectra analyses. Compounds 1, 2, 3, 7 and 11 showed inhibitory activities on lipopolysaccharide-induced nitric oxide production in RAW264.7 cells., (Copyright © 2019 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Amana edulis polysaccharides (AEPs) specifically HBSS, CHSS, DASS, and CASS were sequentially extracted with four different solvents. The present study characterized the AEPs with particular focus on their physicochemical and anti-oxidant based functional properties. Initially, monosaccharide analysis revealed arabinose (31.7%, 32.5%, 36.5%) as the main sugar in HBSS, CHSS, and DASS whereas, galactose (31.4%) in CASS besides their respective molecular weights of 6.29 × 10 2 , 1.5 × 10 2 , 8.1 × 10 2 , and 2.6 × 10 3  kD. HBSS showed the maximum solubility, while, CASS was observed for higher foam capacity and foam stability. Among all the fractions, DASS was observed with higher thermal stability. HBSS showed the highest ABTS + scavenging activity. HBSS and CASS had higher DPPH and OH - scavenging activities. DASS depicted the highest chelation and reducing ability. To summarize, these polysaccharides fractions may be further utilized for their enormous prospective in functional foods preparation., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Rhododendron molle G. Don, belonging to the Ericaceae family, is a traditional Chinese medicinal plant with a wide spectrum of pharmacological effects. This paper aimed to review the phytochemistry, pharmacology and toxicology of R. molle, and to discuss the tendency of future investigations on this plant. A systematic review of literature about R. molle was carried out using resources including classic books about Chinese herbal medicine, and scientific data bases including CNKI, Pubmed, SciFinder, Scopus, and Web of Science. Over 67 compounds, including diterpenes, triterpenes, flavonoids, and lignans, had been extracted and identified from R. molle. The extracts/monomers isolated from the root, flower and fruits of this plant were used as effective agents for treating pains, inflammatory diseases, hypertension, and pest, etc. In addition, diterpenes, such as rhodojaponin III, were considered as the toxic agents associated with the toxicities of this plant. These findings will be significant for the discovery of new drugs from this plant and full utilization of R. molle., (Copyright © 2018 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Three new prenylated flavonoids, macarindicins A-C (1-3), as well as seven known compounds (4-10) were isolated from the twigs of Macaranga indica. Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 2 and 3 enriched the diversity of prenyl moiety in genus Macaranga especially in the aspect of various lengths of prenyl chain. All the known compounds were isolated from M. indica for the first time and this plant was found to contain large number of ellagic acid. Compounds 1-10 were tested for their cytotoxicity against four cancer cell lines (MCF-7, Hep G2, Hela and P388) and showed IC50 values in the range of 2.61-20.35 μg/mL., (Copyright © 2015 Elsevier B.V. All rights reserved.)

Two acidic polysaccharides (GP-B1 and GP-C1) were obtained from Gynostemma pentaphyllum. The molecular weights (Mw) of the two fractions were 79 kDa for GP-B1 and 126 kDa for GP-C1. GP-B1 was composed of Gal, Ara, Man, Rha, Xyl, Glc, GalA and GlcA in a molar ration of 3.5:3.2:0.6:0.9:0.3:0.5:0.6:0.4. GP-C1 consisted of Gal, Ara, Man, Rha, Glc, and GlcA in the proportions of 2.1:1.0:0.3:0.5:0.4:0.9. Among them, GP-B1 treatment had a significant inhibitory effect on the growth of melanoma B16 in vivo and in vitro. Meanwhile GP-B1 could increase the relative spleen weight and stimulate the splenocyte proliferation alone or combined with ConA. Moreover, GP-B1 treatment induced an evident increase in the level of serum TNF-α, IFN-γ, and IL-12 and a reduction for IL-10 production. These results indicate that the antitumor effects of GP-B1 are associated with immunostimulation., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

O. horridus is used as a folk medicine by natives in the Northern Pacific coast of North America. This experiment studied the antiproliferative effects of the extract of O. horridus root bark and its fractions chromatographed from Dianion HP20 resin column with water, 30, 50, 70 and 100% ethanol on human breast cancer MCF-7 cells and non-small cell lung cancer (NSCLC) cells. The role of O. horridus in the cell cycle and apoptosis of MCF-7 cells was also investigated. The results showed that the 70% and 100% ethanol fractions demonstrated more potent antiproliferative effects than the total extract on both cell lines. The antiproliferative effects may result from the enrichment of active constituents detected by high performance liquid chromatography (HPLC). The IC(50) of the total extract, 50, 70, and 100% ethanol fractions for antiproliferation on MCF-7 cells were 248.4, 123.1, 44.0, and 31.5 microg/mL, respectively, and on NSCLC cells were 125.3, 271.1, 17.6, and 23.2 microg/mL, respectively. On the other hand, the water and 30% ethanol fractions significantly promoted cell proliferation on MCF-7 cells at concentrations > 100 microg/mL, suggesting that the hydrophilic fractions should be removed from the extract when used for cancer chemoprevention in order to achieve desirable activities. The effects of the total extract on cell cycle and apoptosis were similar to that of the 100% ethanol fraction because of the similarity of their chemical composition. At higher concentrations, the apoptotic effects of the 70% ethanol fraction are more significant. Data from this study suggested that the 70% and 100% ethanol fractions are active antiproliferative fractions and that induction of apoptosis is the mechanism involved in the antiproliferative effect observed., (Copyright (c) 2010 John Wiley & Sons, Ltd.)

Aim: In this study, we investigated the inhibitive effects of Oplopanax horridus extract (OhE) and its fractions (OhF1, OhF2, OhF3, OhF4 and OhF5) on the growth of human colorectal cancer cells and the possible mechanisms involved were investigated., Materials and Methods: The antiproliferative effects were evaluated by MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) cell proliferation assay. Apoptotic effects and cell cycle distribution were analyzed by flow cytometry after staining with Annexin V/PI or PI/RNase., Results: After treatment for 48 h, OhE, OhF4 and OhF5 (10-100 microg/ml) inhibited proliferation of HCT-116, SW-480 and HT-29 cell lines, and cell growth decreased most with the treatment of OhF4. On the other hand, OhF1, OhF2 and OhF3 were not observed to have obvious suppressive effects on these cell lines at concentrations of 10-100 microg/ml. OhE, OhF4 and OhF5 (1-10 microg/ml) noticeably induced apoptosis time- and concentration-dependently compared to the control at the same time point. Treatment with OhE, OhF4 or OhF5 (1-10 microg/ml) for 24 h distinctly induced a G(2)/M-phase arrest of the cell cycle in a dose-dependent manner. The trend of increasing cyclin A and cyclin B1 were similar to the increase of G(2)/M phase cells in all treated groups., Conclusion: These results showed that OhE had potential antiproliferative effects on human colorectal cancer cells, and the active components are enriched in the OhF4 and OhF5 fractions. The anticancer mechanism of OhE, OhF4 and OhF5 might be attributed to the induction of apoptosis and the regulation of cell cycle transition.

Based on our previous observation, the whole Scutellaria baicalensis extract (SbE) did not show significant breast cancer cell inhibitory effect. In this study, we isolated a baicalin-deprived-fraction (SbF1) of Scutellaria baicalensis, and baicalin-fraction (SbF3), and evaluated their anti-breast cancer properties using MCF-7 cells. The content of four flavonoids in extract/fractions were determined using high performance liquid chromatography. Analytical data showed that in SbF1, the major constituents are baicalein and wogonin, while SbF3 only contains baicalin. The antiproliferative effects of fractions and SbE were assayed using modified trichrome stain method. SbF1 showed significant antiproliferative effect. Treated with 100mug/ml of SbF1 for 72h inhibited MCF-7 cell growth by 81.6%, while in the same treatment concentration, SbF3 increased cell growth by 22.6%. SbF1 was recognized as an active fraction of SbE. The effects of four flavonoids in SbE, scutellarin, baicalin, baicalein and wogonin, were determined, and data showed that baicalein and wogonin significantly inhibited MCF-7 cell growth. In contrast, in certain concentrations, scutellarin and baicalin increased cancer cell growth. The effects of SbF1 on cell cycle and apoptosis were assayed using flow cytometry. SbF1 arrested MCF-7 cells in S- and G2/M-phases, and significantly increased induction of cell apoptosis. These combined phytochemical and biological data provide evidence for further chemopreventive studies of the baicalin-deprived SbE on breast cancer.

In this study, we investigated the possible synergistic chemopreventive effects of American ginseng berry extract (AGBE) and 5-fluorouracil (5-FU) on human colorectal cancer cell lines, SW-480, HCT-116 and HT-29. We used high-performance liquid chromatography to determine the contents of major ginsenosides, the active components of American ginseng, in AGBE. The anti-proliferative effects were evaluated by the cell counting method. AGBE (0.1-1.0 mg/ml) significantly inhibited SW-480, HCT-116 and HT-29 cell growth in a concentration-dependent manner. Cell growth decreased more with the combined treatment of 5-FU and AGBE than with 5-FU or AGBE applied alone, suggesting that AGBE can reduce the dose of 5-FU needed to achieve desired effects and thereby decrease the dose-related toxicity of the chemotherapy agent. Cell apoptosis assay showed that AGBE markedly reduced the number of viable SW-480 cells at 0.5 and 1.0 mg/ml, but did not increase cell apoptosis significantly. Neither 5-FU nor co-treatment with 5-FU and AGBE induced cell apoptosis markedly. Cell cycle assay showed that AGBE mainly arrested SW-480 cells in the G2/M phase. 5-FU increased the percentage of SW-480 cells at the S phase of the cell cycle. The assay of combined treatment groups indicated that AGBE can heighten the arrest of SW-480 cells in the S phase induced by 5-FU, and increase the cell distribution in G2/M phase compared with 5-FU applied alone. The trend of increasing cyclin A was similar to the increase of S and G2/M phase cells in all treated groups. The enhancement of S and G2/M phase arrest, rather than cell apoptosis, should be the mechanism of synergistic effects of AGBE on 5-FU. Further in vivo and clinical trials are needed to test AGBE as a valuable chemo-adjuvant.

Antioxidants have been considered as a useful remedy in diabetes therapeutics, and thus, herbal medicines with antioxidant properties may play major role in treating diabetes. In this report, we performed a comparative study using American ginseng and Scutellaria baicalensis to test whether the anti-diabetic effect of American ginseng is associated with its antioxidant activity. We used a simple water extraction procedure to prepare American ginseng root extract (AGE) and S. baicalensis extract (SbE), and utilized these two antioxidant herbs to evaluate their anti-diabetic effect in obese diabetic ob/ob mice. HPLC analysis was used to identify major constituents in the AGE and SbE. After 12 days of daily intraperitoneal injection, AGE at 300 mg/kg showed significant effects on fasting blood glucose levels (P<0.01) and glucose tolerance test (P<0.01) compared to vehicle-treated mice. Animal body weights also reduced significantly after 12-day treatment (P<0.01). However, SbE, a very strong antioxidant extract, administered at 5-50 mg/kg (based on our previous studies without adverse events) for 12 days did not show any significant effects on blood glucose and body weight changes. No effects were shown when baicalein, an effective antioxidant constituent in SbE, was administered at 1-5 mg/kg. It appears that the anti-diabetic effect of American ginseng may not be linked to its antioxidant actions. The mechanisms of American ginseng's effects on reducing high blood glucose levels and body weight remain to be investigated in future experiments.

Grape seed proanthocyanidin extracts (GSPEs) have been reported to be effective in treating arteriosclerosis, while little is known about therapeutic agents against diabetic macrovascular complications. We used streptozocin to induce diabetic rats. GSPEs (250 mg/kg of body weight) were administrated to diabetic rats for 24 weeks. Aortic blood pressure and pulse wave velocity (PWV) were determined in anesthetized rats. Serum glycated hemoglobin and advanced glycation end products (AGEs) were determined. An electronic microscope was used to observe the changes in aortic ultrastructure. Immunohistochemistry was used to evaluate the receptor of advanced glycation end product (RAGE) protein expression in aortic tissue. GSPEs significantly decreased aortic PWV, blood pressure, and aortic medial thickness (P<0.05), and inhibited the migration of vascular smooth muscle cells. GSPEs significantly reduced the AGEs (P<0.05) and the expression of RAGE in aortas of diabetic rats. GSPEs play an important role against diabetic macrovascular complications. This study may provide a new recognition of natural medicine for the treatment of diabetic macrovascular complications.

Reverse phase high-performance liquid chromatography (HPLC) coupled with a principal component analysis (PCA) method was used to distinguish the extract of notoginseng root from that of other species in the genus Panax . The content of 12 saponins in notoginseng root extracts from different sources was evaluated. Herbal extracts from different plant parts of notoginseng, Asian ginseng, and American ginseng were also evaluated. With an HPLC assay, however, it is difficult to determine whether notoginseng root extract has been adulterated with other plant parts or other Panax species before extraction. Therefore, PCA was introduced to identify adulteration in notoginseng root extract. PCA was performed on the data set obtained from the HPLC chromatogram. The HPLC-PCA assay distinguished notoginseng root extract not only from the extract of other plant parts of notoginseng but also from the extract of Asian or American ginseng plant parts.

Numerous effective anticancer drugs have been developed from botanical sources, and there remains a significant untapped resource in herbal medicines. In this study, we evaluated the chemical composition of extracts from American ginseng after steaming, the antiproliferative effects of the ginsenosides in the extracts on SW-480 human colorectal cancer cells, and their apoptotic mechanisms. American ginseng roots were steamed at 120 degrees C for 2 or 4 h. Representative ginsenosides in the unsteamed and steamed extracts were determined using HPLC. The antiproliferative effects of the ginsenosides Rb1, Rg3 and Rh2 on SW-480 cells were determined by the MTS method. The effect of extract steamed for 4 h on apoptosis of SW-480 cell was assayed by flow cytometry after staining with annexin V/PI. The expression of 84 apoptotic-related genes, including TNF, mitochondria and p53 pathways, was determined using real-time quantitative PCR array analysis. The mitochondrial membrane potential (Deltapsim) was analyzed after staining with FC-1. Steaming of American ginseng increased Rg3 and Rh2 content and antiproliferative activity significantly. The quantitative PCR array data demonstrated that multiple genes in mitochondrial pathway are involved in American ginseng-induced apoptosis of SW-480 cells and the expression profiling was validated by the cellular functional assay. The mitochondrial pathway may play a key role in American ginseng-mediated cancer cell apoptosis.

Background: Diabetic retinopathy (DR) is a leading cause of visual impairment and blindness among the people of occupational age. To prevent the progress of retina injury, effective therapies directed toward the key molecular target are required. Grape seed proanthocyanidin extracts (GSPE) have been reported to be effective in treating diabetic complications, while little is discussed about the functional protein changes., Methods: We used streptozotocin (STZ) to induce diabetes in rats. GSPE (250 mg/kg body weight per day) were administrated to diabetic rats for 24 weeks. Serum glucose, glycated hemoglobin and advanced glycation end products (AGEs) were determined. Consequently, 2-D difference gel electrophoresis and mass spectrometry were used to investigate retina protein profiles among control, STZ-induced diabetic rats, and GSPE treated diabetic rats., Results: GSPE significantly reduced the AGEs of diabetic rats (P < 0.05). Moreover, GSPE significantly suppressed the vascular lesions of central regions, decreased capillary enlargements and neovascularization, similar to those of the control rats under light microscope. Eighteen proteins were found either up-regulated or down-regulated in the retina of STZ-induced diabetic rats. And seven proteins in the retina of diabetic rats were found to be back-regulated to normal levels after GSPE therapy. These back-regulated proteins are involved in many important biological processes such as heat shock, ubiquitin-proteasome system, cell proliferation, cell growth and glucose metabolism., Conclusions: These findings might promote a better understanding for the mechanism of DR, and provide novel targets for evaluating the effects of GSPE therapy.

The aim of the study was to investigate the therapeutic effect and mechanism of proanthocyanidins from grape seeds (GSPE) in the treatment of ulcerative colitis (UC). Rats were intragastrically administered different doses of GSPE (100, 200, and 400 mg/kg) per day for 7 days after UC was twice-induced by intracolonic injection of 2,4,6-trinitrobenzene sulfonic acid (TNBS)dissolved in 50% ethanol. Sulfasalazine (SASP) at 200 mg/kg was used as a positive control drug. Macroscopic and microscopic damage scores and changes in weight/length ratio (mg/mm) of colon segments were analyzed. The levels of malonyldialdehyde (MDA), interleukin (IL)-1beta, IL-2, IL-4, and myeloperoxidase (MPO) activity in the colon tissues and MPO activity in the serum were all measured by biochemical methods or double antibody sandwich ELISA methods. Compared with the TNBS control group, GSPE treatment facilitated recovery of pathologic changes in the colon after insult with TNBS, as demonstrated by increased body weight (p < 0.01) and decreased colonic weight/length ratio (p < 0.01); GSPE also notably reduced the colonic macroscopic and microscopic damage scores (p < 0.01). The MPO activity in colon tissues and serum of rats treated with GSPE was significantly lower than that in the TNBS control group. The MDA and IL-1beta levels of colon tissues were also decreased in GSPE groups. The intestinal antiinflammatory effect of GSPE was accompanied by a significant improvement of IL-2 and IL-4 levels in the colon tissues of rats in the high-dose GSPE group (p < 0.05). Compared with the SASP group, GSPE groups had no significant difference in the therapeutic effect (p > 0.05). GSPE exerts a beneficial antiinflammatory effect in the acute phase of TNBS-induced colitis in rats by downregulating some of the mediators involved in the intestinal inflammatory response, inhibiting inflammatory cell infiltration and antioxidation damage, promoting damaged tissue repair to improve colonic oxidative stress, decreasing production of proinflammatory cytokines IL-1beta, and increasing production of antiinflammatory cytokines IL-2 and IL-4.

Diabetic nephropathy (DN) is a major cause of morbidity and mortality in diabetic patients. To prevent the development of this disease and to improve advanced kidney injury, effective therapies directed toward the key molecular target are required. Grape seed proanthocyanidin extracts (GSPE) have been reported to be effective in treating DN, while little is known about the functional protein changes. In this study, we used streptozotocin (STZ) to induce diabetic rats. GSPE (250 mg/kg body weight/day) were administrated to diabetic rats for 24 weeks. Serum glucose, glycated hemoglobin, and advanced glycation end products were determined. Consequently, 2-D difference gel electrophoresis and mass spectrometry were used to investigate kidney protein profiles among the control, untreated and GSPE treated diabetic rats. Twenty-five proteins were found either up-regulated or down-regulated in the kidneys of untreated diabetic rats. Only nine proteins in the kidneys of diabetic rats were found to be back-regulated to normal levels after GSPE therapy. These back-regulated proteins are involved in oxidative stress, glycosylation damage, and amino acids metabolism. Our findings might help to better understanding of the mechanism of DN, and provide novel targets for estimating the effects of GSPE therapy., (Copyright 2008 Wiley-Liss, Inc.)

Two new triterpenes mayteneri A (1), mayteneri B (2), and seven known compounds (3-9) were isolated from stems of Maytenus hookeri Loes. The chemical structures of compounds 1 and 2 were established by 1D, 2D NMR, HRESIMS analysis, and calculating electronic circular dichroism (ECD). The structures of known compounds 3-9 were determined by comparison of their spectral with those reported. Compounds 4-7 showed significant inhibitory activity for NLRP3 inflammasome, with the IC50 values of 2.36–3.44 μM. [ABSTRACT FROM AUTHOR]

Two new compounds verboncin A (1) and verboncin B (4) and 14 known compounds (2–3 and 5–16) were isolated from Verbena bonariensis, and these 14 compounds were first obtained from this plant. Their chemical structures were established by one and two-dimensional NMR and HRESIMS analysis and the results were compared with literature values. The absolute configuration of 1 was determined by calculating electronic circular dichroism (ECD). The cytotoxicity of some of the compounds against MCF-7, HCT-116, MDA-MB-231, and SW620 human cancer cell lines were evaluated, in which compound 4 showed negligible cytotoxic activity with an IC50 value of 68.08 ± 0.35 µM against the MCF-7 cell line. [ABSTRACT FROM AUTHOR]

One new ionone glycoside, named centrantheroside F (1), together with 9 known compounds (2-10), were isolated from the roots of Centranthera grandiflora. Their structures were determined by spectroscopic data analyses and comparing with the literature data. The absolute configuration of 1 was confirmed via 2 D NMR and electronic circular dichroism (ECD). All isolated compounds were evaluated for their inhibitory activity on lipopolysaccharide (LPS)-induced nitric oxide (NO) production. [ABSTRACT FROM AUTHOR]

In the present study, six new compounds namely, picralactones C H (1–6) along with nine known compounds (7–15) were isolated from the branches and leaves of Picrasma chinese P.Y. Chen. Their structures were determined with the help of spectroscopic techniques such as NMR, HR-ESI-MS, UV, IR and CD. Cytotoxicity of all compounds was evaluated against MDA-MB-231, SW-620 and HepG2 human cancer cell lines. Compound 4 showed cytotoxic activities. [Display omitted] • Six new quassinoids were isolated from the branches and leaves of Picrasma chinese P.Y. Chen. • Cytotoxicity of all compounds was evaluated against MDA-MB-231, SW-620 and HepG2 human cancer cell lines. • Compound 4 showed cytotoxic activities. [ABSTRACT FROM AUTHOR]

Four new diterpenoids (1–4) and four known diterpenoids (5–8) were purified from the whole plant of Euphorbia helioscopia L. Compounds 1 and 2 were jathophanes diterpenoids with a 5/12 polycyclic systems, compound 3 was rhamofolane diterpenoid with a 5/10 bicyclic skeleton and compound 4 was a rare class of euphorbia diterpenes featuring an unusual 5/10 fused ring system. Anti-inflammatory activity tests were conducted on the separated compounds, indicating that compound 4 had significant inhibitory effect on NLRP3 inflammasome with an IC 50 value of 7.75 μM. Further, the inhibitory effect of 4 was determined using immunofluorescence assays. [Display omitted] • Four new diterpenoids (1–4) and four known diterpenoids (5 - 8) were purified from the whole plant of Euphorbia helioscopia L. • Compound 3 was rhamofolane diterpenoid with a 5/10 bicyclic skeleton and 4 was a rare class of euphorbia diterpenes featuring an unusual 5/10 fused ring system • Compound 4 showed strong activity with IC 50 values of 7.75 μM. Frther, the inhibitory effects of 4 on protein levels were determined using immunofluorescence assays. [ABSTRACT FROM AUTHOR]

Nine previously undescribed clerodane-type diterpenoids (1–9), named caseabalanspenes A-I , along with six know compounds (10–15), were isolated from the twigs and leaves of Casearia velutina. Spectroscopic data (1D and 2D NMR) analysis permitted the definition of their structures and then determination of the molecular formula of the compound by high resolution mass spectrometry (HR-ESI-MS). It is worth noting that compound 7 contains N- heterocycle. Compounds 1–8 were tested the anti-inflammasome activity, and compound 3 exhibited potent activity and decreased LDH level in a dose-dependent manner, with IC 50 values of 2.90 μM. [Display omitted] • Nine undescribed clerodane diterpenoids were isolated from Casearia velutina. • Their structures were determined by 1D, 2D-NMR and HR-ESI-MS analyses. • The structure of compound 7 contains an N-heterocycle. • Compound 3 exhibited NLRP3-inflammasome inhibitory activity with IC 50 values of 2.90 μM. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • Chemical composition, antibacterial and insecticidal potential of seven plant derived essential oils were investigated. • The active components of oils were different, and terpenes and phenols were the main members of EOs. • Cinnamon EO and clove EO exhibited the highest antibacterial activity. • Cinnamon EO, clove EO, anise EO and their single compounds displayed appreciable fumigant toxicity against Sitophilus oryzae. Abstract The chemical composition, antibacterial and insecticidal potential of Anise, Peppermint, Clove, Cinnamon, Pepper, Citronella and Camphor essential oils (EOs) extracted by steam distillation from seven different plant species were investigated. GC–MS analysis revealed that terpenes and phenols were the main components of EOs. The different kinds of EOs exerted appreciable antibacterial action against Gram-positive (B. subtilis and S. aureus) as well as Gram-negative (E. coli and S. typhimurium) bacteria. Among EOs, cinnamon EO exhibited the highest antibacterial effect for all the bacterial strains with the lowest MIC ranging from 0.125 to 0.25 mg/mL, the largest inhibition zone and the strongest inhibition of bacterial growth, followed by clove EO. The moderate inhibitory effects were observed for remaining EOs. On the other hand, cinnamon EO, clove EO, and anise EO exhibited significant fumigant toxicity against Sitophilus oryzae at 7.69 μL/L air concentration after 24 and 48 h exposure. Furthermore, the single component analysis showed the LC 50 values of 2.90 for eugenol, 5.45 for cinnamaldehyde, and 5.42 μL/L air for estragole extracted from selected EOs (clove, cinnamon, anise), respectively. The results will pave a way for utilization of plant derived EOs as natural food preservatives to counteract food spoilage and pest's managements. [ABSTRACT FROM AUTHOR]

Four new diterpenoids (1–4) and sixteen known diterpenoids (5–20) were purified from the whole plant of Euphorbia helioscopia L. Compounds 1 and 2 were rhamofolane diterpenoids with a 5/7/6 tricyclic systems, compound 3 was a lathyranes diterpenoid, and compound 4 was a jathophanes diterpenoid. The isolated compounds were tested for their cytotoxicity and anti-Zika virus properties, and compounds 9 and 15 showed low cytotoxicity and strong anti-Zika virus properties with EC 50 2.63 and 5.94 μM, respectively. Further, the inhibitory effects of compounds on protein levels were determined using Western blotting and immunofluorescence assays. [Display omitted] • Twenty natural compounds were isolated from the Euphorbia helioscopia , of which four were new compounds. • Compounds 9 and 15 showed strong activity with EC 50 values of 2.63 and 5.94 μ M, respectively. In addition, the results of cytotoxicity tests showed that compounds 9 and 15 had relative cell activity of over 50% at 200 μ M. [ABSTRACT FROM AUTHOR]

Eleven undescribed 16,17-dinor-abietane diterpenoids, caseazins A-K (1 − 11), and ten known diterpenoids (12 − 21) were isolated from the twigs and leaves of Casearia kurzii (Flacourtiaceae). Caseazins A-K were the first abietane -type dinorditerpenoids to have been isolated from the plant of Casearia kurzii. Their chemical structures were elucidated using a combination of 1D and 2D NMR spectroscopy and mass spectrometry. The absolute configurations of 5 and 10 were established by electronic circular dichroism calculations. Moreover, compounds 2 , 3 , 13 , 14 , and 18 exhibited anti-inflammatory activity with IC 50 values of 0.17, 0.36, 6.55, 1.30, and 4.53 μM, respectively. IL-1β and caspase-1 analyses suggested that compound 14 inhibited NLRP3 inflammasome activation and blocked macrophage pyroptosis. Diterpenoids from Casearia kurzii with NLRP3 inflammasome inhibitory activity were reported in this research. [Display omitted] • Eleven undescribed dinorditerpenoids were isolated from Casearia kurzii. • The compound 14 showed potent inhibitory activity against pyroptosis by blocking NLRP3 inflammasome activation. Their structures were established by elucidated by NMR, HRESIMS and ECD analyses. [ABSTRACT FROM AUTHOR]

A phytochemical investigation to obtain bioactive substances as lead compounds or agents for anti-inflammatory led to the obtainment of eleven previously undescribed clerodane diterpenoids, named caseatardies A-K (1 − 11), and four known clerodane diterpenoids (12 – 15) from the twigs and leaves of Casearia tardieuae. The structural elucidation of these clerodane diterpenoids was based on 1D and 2D-NMR spectroscopy (COSY, HSQC, HMBC and ROESY) as well as high resolution mass spectrometry (HR-ESI-MS). The relative configurations were defined by ROESY correlations. The anti-inflammatory activity of all the isolated compounds was screened and compound 15 decreased LDH level in a dose-dependent manner, showing IC 50 value of 2.89 μM. [Display omitted] • Eleven new clerodane diterpenoids with conjugated diene side chain at C-9 were isolated from Casearia tardieuae. • The compound 15 showed potent inhibitory activity against pyroptosis by blocking NLRP3 inflammasome activation. • Their structures were established by elucidated by 1D, 2D-NMR and HR-ESI-MS analyses. [ABSTRACT FROM AUTHOR]

One rare flavonoid–diterpene heterodimer, denticulatain C ( 1 ), one modified geranyl-type side chain substituted flavonoid, denticulatain D ( 2 ) and one geranylated flavonoid, denticulatain E ( 3 ), as well as 11 known compounds ( 4 – 14 ) were isolated from the fronds of Macaranga denticulata . Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 4 and 8 inhibited the proliferation of A-549 cell line with IC 50 values of 48.6 and 20.2 μ g/mL, respectively. Compounds 3 , 6 , and 8 exhibited significant antiangiogenic activity on a zebrafish model with IC 50 values of 9.78, 0.34, and 2.55 μ g/mL, respectively. [ABSTRACT FROM AUTHOR]

Ten new prenylated flavonoids, named denticulains A-J (1−10), together with seven known prenylated flavonoids (11–17) were isolated from Macaranga denticulata. Their structures were elucidated on the basis of detailed spectroscopic analysis and by comparison with literature data. In addition, compounds 1 and 14 inhibited the proliferation of SW620 and HCT-116 cell lines with an IC 50 value of 46.08 μM and 56.83 μM, respectively. [Display omitted] • Ten new prenylated flavonoids were isolated from Macaranga denticulata. • Some compounds have week anticancer activities. [ABSTRACT FROM AUTHOR]

One unique prenylated bibenzyl, kurzphenol A ( 1 ), two new prenylated flavonoids, kurzphenols B and C ( 2 and 3 ), as well as fourteen known compounds ( 4 – 17 ) were isolated from the twigs of Macaranga kurzii . Compound 1 was the first example of prenylated bibenzyl which possesses a benzofuran ring. All the known compounds were isolated from M. kurzii for the first time. Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 1 – 17 were tested for their cytotoxicity against A-549 and Hep G2 cancer cell lines and showed IC 50 values in the range of 9.76–30.14 μ g/mL. [ABSTRACT FROM AUTHOR]

A phytochemical investigation was conducted on Euphorbia helioscopia , resulting in the isolation of thirteen compounds, including nine undescribed diterpenoids, Euphzycopias A − I (1 – 9), of which the skeletons of compounds 1 – 4 were found in E. helioscopia L. Compounds 1 – 3 had 5/7/6 cyclic systems, while compound 4 had a 4/11 polycyclic system with a 4,7-cyclic ether between C-4 and C-7. The anti-inflammasome test using the isolated compounds (1–6, 8–13) showed that the diterpenes from E. helioscopia L. had a strong inhibitory effect on NLRP3 inflammasomes with IC 50 values of 3.34–14.92 μM. [Display omitted] • Nine undescribed diterpenoids were isolated from Euphorbia helioscopia L. • The skeletons of the first four compounds first appeared in the genus Euphorbia L. • Some compounds had significant anti-inflammatory activity on NLRP3 inflammasome. [ABSTRACT FROM AUTHOR]