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Nine new diterpenoids, Rubellacrns A − I (1–9), including five isopimaranes (1–4, 9), four pimaranes (5–8), together with five known isopimarane analogues (10–14), were isolated from Callicarpa rubella. The structures of these compounds were unambiguously established by HR-ESIMS and NMR spectroscopic data, the absolute configurations of compounds 5 and 9 were determined by ECD. All the isolated compounds were tested for their anti-inflammatory effects and compounds 2 and 11–14 showed NLRP3-inflammasome inhibitory activity with IC 50 values ranging from 7.02 to 14.38 μM. Unlabelled Image • Nine new diterpenoids were isolated from Callicarpa rubella. • The absolute configuration of 5 and 9 was deduced by ECD. • The new compound 2 showed potent inhibition of inflammasome activation. [ABSTRACT FROM AUTHOR]

Citrisorbicillinol (1), along with six other known compounds (2 – 7), was isolated from an endphyte Penicillium citrinum ZY-2 of Plantago asiatica L. Citrisorbicillinol (1) was characterized as a skeletally unprecedented hybrid sorbicillinoid, and its unique framework is likely formed by intermolecular [4 + 2] cycloaddition between intermediates derived from citrinin and sorbicillinoid biosynthetic gene clusters. Compounds 1 and 2 demonstrated to promote osteoblastic differentiation in MC3T3-E1 cells, and to be osteogenic in the prednisolone induced osteoporotic zebrafish. Compounds 3–7 exhibited moderate cytotoxicity against four human cancer cell lines. [Display omitted] • An undescribed polyketide citrisorbicillinol was isolated from endphyte Penicillium citrinum ZY-2. • The unique citrisorbicillinol framework is likely formed by an intermolecular [4 + 2] cycloaddition. • Citrisorbicillinol was demonstrated to be osteogenic in the prednisolone induced osteoporotic zebrafish. [ABSTRACT FROM AUTHOR]

Abstract Ethnopharmacology relevance Rhizome of Ligusticum chuanxiong Hort. (Abbreviated as LC) is a frequently prescribed component in plenty of traditional Chinese medicine (TCM) formulas which are used to treat diabetic nephropathy (DN). The aims of the present study are to investigate the protective effect of the ethanol extract of LC rhizome (EEL) against DN in vivo , evaluate its potential mechanism, and find the evidence supporting its enthopharmacological use as an anti-DN agent. Materials and methods Hepa 1c1c7 murine hepatoma cells, human breast carcinoma MDA-MB-231 cells, human renal glomerular endothelial cells (HRGEC), and RAW 264.7 murine macrophages were adopted to test the effects of EEL and its active constituents on inhibitions of oxidative stress and inflammation in vitro. A streptozotocin (STZ) -induced DN C57BL/6 mice model was established and used to investigate the preventive effect of EEL against DN in vivo. Results EEL demonstrated potential inhibitory effects against oxidative stress and inflammation in vitro. Using a STZ-induced DN mice model, it has been found that EEL treatment significantly prevented STZ-induced increases of urine production, urinary albumin excretion (UAE) and urine albumin-to-creatinine ratio (UACR), and markedly attenuated STZ-induced renal damages (e.g. glomerulosclerosis and fibrosis). The predominant bioactive constituents, Z -ligustilide (LGT), ferulic acid (FA), and tetramethylpyrazine (TMP), were inhibitors of oxidative stress and inflammation through acting with Nrf2 and NF-κB pathways. Conclusions EEL attenuates structural and functional damages of kidney in STZ-induced DN model in vivo , which might be related to the functions of EEL on inhibitions of oxidative stress and inflammation. These finding definitely supports the ethnopharmacological use of LC as an anti-DN agent. Graphical abstract fx1 [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]

Myocardial fibrosis (MF) is a common pathological manifestation of many cardiovascular diseases at a certain stage, with excessive accumulation of collagen fibers, excessive increase in collagen content, and a significant increase in collagen volume as the main pathological changes. There are currently no effective drugs for the treatment of myocardial fibrosis. Traditional Chinese medicine (TCM), the main component of the medical practice used for more than 5000 years, especially in China, often exerts a wider action spectrum than previously attempted options in treating human diseases. In recent times, the great potential of TCM in the treatment of MF has received much attention. Especially many experimental studies on the treatment of MF by Astragalus mongholicus Bunge have been conducted, and the effect is remarkable, which may provide more comprehensive database and theoretical support for the application of Astragalus mongholicus Bunge in the treatment of MF and could be considered a promising candidate drug for preventing MF. This review summarizes the chemical components of Astragalus mongholicus Bunge, Astragalus mongholicus Bunge extrac t, Astragalus mongholicus Bunge single prescription, and Astragalus mongholicus Bunge compound preparation in the treatment of MF, and provides comprehensive information and a reliable basis for the exploration of new treatment strategies of botanical drugs in the therapy of MF. The literature information was obtained from the scientific databases on ethnobotany and ethnomedicines (up to August 2022), mainly from the PubMed, Web of Science, and CNKI databases. The experimental studies on the anti-myocardial fibrosis role of the effective active components of Astragalus mongholicus Bunge and the utility of its compound preparation and the involved mechanisms were identified. The search keywords for such work included: "myocardial fibrosis" or "Cardiac fibrosis ", and " Astragalus mongholicus Bunge", "extract," or "herb". Several studies have shown that the effective active components of Astragalus mongholicus Bunge and its formulas, particularly Astragaloside IV, Astragalus polysaccharide, total saponins of Astragalus mongholicus Bunge, triterpenoid saponins of Astragalus mongholicus Bunge, and cycloastragenol, exhibit potential benefits against MF, the mechanisms of which appear to involve the regulation of inflammation, oxidant stress, and pro-fibrotic signaling pathways, etc. Conclusion : These research works have shown the therapeutic benefits of Astragalus mongholicus Bunge in the treatment of MF. However, further research should be undertaken to clarify the unconfirmed chemical composition and regulatory mechanisms, conduct standard clinical trials, and evaluate the possible side effects. The insights in the present review provided rich ideas for developing new anti-MF drugs. Myocardial fibrosis (MF) with excessive accumulation of collagen fibers, excessive increase in collagen content, and a significant increase in collagen volume as the main pathological changes is a common pathological manifestation of many cardiovascular diseases at a certain stage, which seriously affects cardiac function. At present, there is still a lack of effective drugs for the treatment of MF. Traditional Chinese medicine (TCM), the main component of the medical practice used for more than 5000 years especially in China, often exerts wider action spectrum than previously attempted options in treating human diseases. In recent times, the great potential of TCM in the treatment of MF has received much attention. Especially many experimental studies on the treatment of MF by Astragalus mongholicus Bunge have been conducted, and the effect is remarkable, which may provide more comprehensive data base and theoretical support for the application of Astragalus mongholicus Bunge in the treatment of MF and could be considered a promising candidate drug for preventing MF. [Display omitted] [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]

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]

Abstract: Regulation of signal transducer and activator of transcription (STAT) 1 signaling is being explored as a new approach to the treatment of inflammatory bowel diseases. However, few chemicals have been reported to inhibit IFN-γ/STAT1 signaling for Crohn''s disease therapy. In the present study, we found that cirsilineol, a small natural compound isolated from Artemisia vestita, significantly ameliorated trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice, which was closely associated with reduced autoreactive T-cell proliferation and activation. Moreover, the regulatory action of pro-inflammatory and anti-inflammatory cytokine by cirsilineol treatment was found to decrease the activity of effector Th1 cells but increase the activity of regulatory T cells as characterized by down-regulation of IFN-γ and corresponding up-regulation of IL-10 and TGF-β. The therapeutic effect of cirsilineol was attributable to a novel regulatory mechanism with selective inhibiting IFN-γ signaling in colonic lamina propria CD4+ T cells, which was mediated through down-regulating STAT1 activation and T-bet expression. Furthermore, cirsilineol was found to down-regulate the activation of JAK2, a critical kinase for IFN-γ/STAT1 signaling, and abrogate the expression of T-bet, resulting in markedly decreased proliferation and activation of T cells in vitro. Importantly, the inhibition of IFN-γ/STAT1 signaling by cirsilineol was reversible in the presence of high level of IFN-γ. These results strongly suggest that cirsilineol might be potentially useful for treating T-cell-mediated human inflammatory bowel diseases. [Copyright &y& Elsevier]

A new isoiphionane sesquiterpene, named (3 S , 5 S , 7 S , 10 R)-3, 11-dihydroxyisoiphion-4-one (1), two new phloroglucinol glycosides, named eucalglobuside A (2) and eucalglobuside B (3), along with 15 known compounds were isolated from the leaves of Eucalyptus globulus. Their structures were elucidated based on extensive spectroscopic analysis and in comparison with literature data. The absolute configuration of compound 1 was determined by ECD calculation. All isolates were evaluated their inhibitory activities against the mushroom tyrosinase. As a result, three sesquiterpenoids, 1 , 5 β , 11-dihydroxy-iphionan-4-one (5), and (−)-globulol (8), exhibited the most potent activities with IC 50 values of 14.17 μM, 10.08 μM and 9.79 μM, respectively. Unlabelled Image • One new isoiphionane sesquiterpene and two new phloroglucinol glycosides were isolated from Eucalyptus globulus. • The absolute configuration of compound 1 was determined by ECD calculation. • Compounds 1 , 5 , and 8 exhibited more potent activities against the tyrosinase than the positive control kojic acid. [ABSTRACT FROM AUTHOR]