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Acquired resistance to cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) frequently emerges, and CDK4/6i-containing therapies in triple-negative breast cancer (TNBC) remain to be determined. RNA-sequencing, cell viability analysis, immunoblotting, siRNA transfection et al. were used to investigate and verify the resistance mechanism. BALB/c nude mice xenograft models and spontaneous MMTV-PyMT models were used to explore in vivo efficacy. The mTOR pathway was activated in acquired CDK4/6i-resistant cells and inhibition of mTORC1 restored the sensitivity. While fasting-mimicking diet (FMD) enhances the activity of anticancer agents by inhibiting the mTORC1 signaling, we assessed FMD and found that FMD restored the sensitivity of CDK4/6i-resistant cells to abemaciclib and potentiated the anti-tumor activity of CDK4/6i in TNBC. The anti-tumor effects of FMD and/or CDK4/6i were accompanied by the downregulation of S6 phosphorylation. FMD cooperated with CDK4/6i to suppress the levels of IGF1 and RAS. The combination of FMD and abemaciclib also led to a potent inhibition of tumor growth in spontaneous transgenic MMTV-PyMT mouse models. Our data demonstrate that FMD overcomes resistance and potentiates the anti-tumor effect of CDK4/6i by inhibiting mTORC1 signaling via lowering the levels of IGF1 and RAS, providing the rationale for clinical investigation of a potential FMD-CDK4/6i strategy in breast cancer. • mTORC1 activation is a key mechanism governing CDK4/6i-resistance in breast cancer. • FMD reversed CDK4/6i-resistance by suppressing the mTORC1 pathway. • CDK4/6i-resistance can be reversed by FMD through lowering the levels of IGF1 and RAS. • FMD cooperated with CDK4/6i in a transgenic MMTV-PyMT mouse model with favorable feasibility. [ABSTRACT FROM AUTHOR]

Eight previously undescribed diterpenoids, crolaevinoids A−H, including two halimanes, four clerodanes, and two laevinanes, along with six known analogues were isolated from the twigs of Croton laevigatus . The structures of the previously undescribed were elucidated by spectroscopic analysis, and their absolute configurations were determined by combination of a single crystal X-ray diffraction and CD analysis (exciton chirality and Rh 2 (OCOCF 3 ) 4 -induced methods). Crolaevinoids A and B represent the first halimane diterpenoids with a unique lactone bridge between C-12 and C-17. All compounds were evaluated for their inhibitory effects on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 macrophage cells. Furocrotinsulolide A and 3,4,15,16-diepoxy-cleroda-13(16),14-diene-12,17-olide exhibited pronounced inhibition of NO production with IC 50 values of 10.4 ± 0.8 and 6.0 ± 1.0 μ M, respectively, being more potent than the positive control, quercetin (IC 50 = 13.1 ± 1.9 μ M). [ABSTRACT FROM AUTHOR]

Norhypersampsone A ( 1 ), a novel degraded polycyclic polyprenylated acylphloroglucinol (PPAP) derivative, 3-(2-hydroxy-7-methyl-3-methyleneoct-6-enyl)-5-isoprenyl-2,4,6-trihydroxybenzophenone ( 2 ), a new polyprenylated benzophenone derivative, and nine known compounds ( 3 – 11 ) were isolated from Hypericum sampsonii . Their structures were elucidated by comprehensive spectroscopic techniques. Compound 1 represents a novel cyclohexenone monocyclic-PPAP formed by losing the fragment of C-2–C-4 and the side chains at C-3 and C-5 in the phloroglucinol ring. The results of the inhibitory effects of compounds 1 – 11 on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW 264.7 macrophages showed that compounds 1 , 6 – 8 , and 10 exhibited weak activities with IC 50 values in the range of 20.3–37.1 μM. [ABSTRACT FROM AUTHOR]

A finite element model of Boussinesq-type equations was set up, and a direct numerical method is proposed so that the full reflection boundary condition is exactly satisfied at a curved wall surface. The accuracy of the model was verified in tests. The present model was used to further examine cnoidal wave propagation and run-up around the cylinder. The results showed that the Ursell number is a nonlinear parameter that indicates the normalized profile of cnoidal waves and has a significant effect on the wave run-up. Cnoidal waves with the same Ursell number have the same normalized profile, but a difference in the relative wave height can still cause differences in the wave run-up between these waves. The maximum dimensionless run-up was predicted under various conditions. Cnoidal waves hold entirely distinct properties from Stokes waves under the influence of the water depth, and the nonlinearity of cnoidal waves enhances rather than weakens with increasing wavelength. Thus, the variations in the maximum run-up with the wavelength for cnoidal waves are completely different from those for Stokes waves, and there are even significant differences in the variation between different cnoidal waves. [ABSTRACT FROM AUTHOR]

One new halimane diterpenoid, marrubasch C ( 1 ), two new labdane diterpenoids, marrubaschs D and E ( 2 and 3 ), and three known labdane diterpenoids, marrubasch F ( 4 ), marrubiin ( 5 ), and marrubenol ( 6 ), were isolated from the ethanol extract of Marrubium aschersonii Magnus (Lamiaceae). Structures of these compounds were elucidated on the basis of spectroscopic analysis. The inhibitory effects of compounds 1 – 6 on nitric oxide (NO) production in RAW 264.7 macrophage cells activated by lipopolysaccharide (LPS) were investigated and all the compounds showed weak activity. [ABSTRACT FROM AUTHOR]

Eight undescribed triterpenoids (pterohoonoids A−H) including four oleananes, one nor-oleanane and three nor-ursanes, along with seven known analogues, were isolated from the whole plants of Pterocephalus hookeri (Dipsacaceae). The structures with relative stereochemistries of these molecules were elucidated mainly by spectroscopic analyses, and the absolute configurations of the undescribed ones were assigned by a variety of methods, including time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculation, Rh 2 (OCOCF 3) 4 -induced ECD experiment and chemical transformation. The inhibitory effects toward the diabetes target α -glucosidase of all the isolates were assessed, and four of them exhibited pronounced activity with IC 50 values ranging from 6.8 to 55.8 μ M. In addition, four compounds also showed inhibition against the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 macrophage cells (IC 50 = 12.4–63.7 μ M). Further assays demonstrated that the most active compound pterohoonoid A inhibited the release of two key pro-inflammatory cytokines TNF- α and IL-6 in a dose-dependent manner. [Display omitted] • Eight undescribed triterpenoids were isolated from Pterocephalus hookeri. • The absolute configurations of the compounds were determined by extensive methods. • Four compounds exhibited pronounced inhibitory activity against α-glucosidase. • Four compounds exhibited inhibition against the nitric oxide production. • The inhibitory effects on pro-inflammatory factors TNF-α and IL-6 were investigated. [ABSTRACT FROM AUTHOR]

Chemical investigation of the traditional Chinese medicine Amomum kravanh led to the isolation of a new secolignan (1), two flavonoids (2 and 3), four monoterpenoids (4 – 7) and six steroids (8 – 13). Compounds 1 , 5 – 8 and 12 – 13 were isolated from the family Zingiberaceae for the first time. Compound 1 is the first lignan reported in the genus Amomum and compound 8 is firstly described as a natural product, which could be of chemotaxonomic importance for the genus Amomum and family Zingiberaceae. • A phytochemical investigation on the fruits of Amomum kravanh was conducted. • Thirteen compounds including a new secolignan were isolated and structurally characterized. • The chemotaxonomic significance of the isolated compounds was discussed. [ABSTRACT FROM AUTHOR]

Seven new diarylheptanoids, kravanhols C−I (1 – 7), along with two known analogues (8 and 9), were isolated from the fruits of Amomum kravanh. The structures of compounds 1 – 7 were elucidated by analysis of spectroscopic data, and the absolute configurations of selective ones were determined by time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculations. All compounds were evaluated for their inhibitory effects on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells. Compounds 2 , 5 , 6 and 9 exhibited moderate inhibitory activity with IC 50 values in the range of 17.4–26.5 μM, being more potent than the positive control dexamethasone (IC 50 = 32.5 μM). [ABSTRACT FROM AUTHOR]

Three new sesquiterpenoids (1 – 3) and two new sesquiterpenoid glucosides (4 & 5), along with 24 known analogues (6 – 29), were obtained from the flowers of Inula japonica. Structures of the new compounds were determined by interpretation of spectroscopic data, and their absolute configurations were established via comparison of experimental with computed ECD curves. All the isolates were tested in an in vitro cytotoxic assay against human A549, MCF-7 and MDA-MB-231 cancer cell lines, and selective ones displayed significant activity close to the positive control adriamycin. The new molecules 1 – 5 were also evaluated for their nitric oxide (NO) release inhibitory effect in murine macrophage RAW264.7 cells, with compound 1 showing comparable activity (IC 50 16.2 ± 0.8 μM) to the positive control dexamethasome. A preliminary mechanistic study of the effect of 8 toward A549 cells revealed that it could arrest cell cycle at G 2 /M phase and induce cell apoptosis in a dose-dependent manner. Unlabelled Image [ABSTRACT FROM AUTHOR]

Seven previously undescribed polycyclic diterpenoids, euphonoids A−G, including four ent -abietanes, two ent -atisanes, and one ent -kaurene, along with 26 known analogues were isolated from the roots of Euphorbia fischeriana. The structures of the undescribed compounds were elucidated by spectroscopic analysis, ECD calculations, and single crystal X-ray diffraction. Besides, the structure of a previously reported ent -abietane diterpenoid, fischeriabietane A, was revised. All the isolates were screened for the cytotoxicities against five cancer cell lines. Euphonoid A, fischeriabietane A, 11-oxo-ebracteolatanolide B, caudicifolin, jolkinolide B, and methyl-8,11-3-dihydroxy-12-oxo- ent -abietadi-13,15(17)-ene-16-oate showed significant inhibitory activities against human prostate cancer C4-2B and C4-2B/ENZR cell lines, with IC 50 values being less than 10 μ M. The brief structure-activity relationships (SARs) of these diterpenoids were also discussed. Seven previously undescribed polycyclic diterpenoids along with 26 known analogues were isolated from the roots of Euphorbia fischeriana. Six compounds showed significant inhibitory activity against C4-2B and C4-2B/ENZR cell lines, with IC 50 values being less than 10 μ M. Image 1 • Seven previously undescribed diterpenoids were isolated from Euphorbia fischeriana. • Six compounds showed significant cytotoxicity against a panel of cancer cell lines. • The brief structure-activity relationships of these diterpenoids were discussed. [ABSTRACT FROM AUTHOR]

Under the guidance of MS/MS-based molecular networking, five new clerodane diterpenoid glucosides, tinosinesides R-V (1 – 5), along with 15 known diterpenoids (6–20), were isolated from the stems of Tinospora sinensis. Compound 1 represents the first example of diterpenoid bearing a thio sugar and compound 5 is the first 18,19-dinor-clerodane with cis -fused A/B ring. The structures of the new compounds were elucidated by spectroscopic means, and their absolute configurations were established on the basis of time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculation and chemical methods. Selected compounds were evaluated for their immunomodulatory effect and several compounds could enhance the proliferation of B lymphocytes. Preliminary mechanistic studies disclosed that 3 could promote B cell generation and inhibit B cell differentiation. [Display omitted] [ABSTRACT FROM AUTHOR]

Chemical investigation of the Tinospora sinensis led to the isolation of a new cadinane sesquiterpene (1) and twelve known sesquiterpenes (2 − 13). The structures of these compounds were deduced using a suite of comprehensive spectroscopic techniques including NMR, MS etc. , and the absolute configuration of 1 was established through a combination of TDDFT calculations and chemical methods. Compound 1 demonstrated mild cytotoxicity against MDA-MB-231 cell line, with an inhibition rate of 46.8% and 54.2% at 50 μmol/L and 100 μmol/L, respectively. Compounds 1 , 5 − 13 were reported to exist in the Menispermaceae family for the first time. Furthermore, the chemotaxonomic significance of the isolates is also discussed. • Thirteen sesquiterpenes were isolated from the Tinospora sinensis. • A new cadinane sesquiterpene was isolated from the Tinospora sinensis. • Compounds 1 , 5–13 were isolated from Menispermaceae for the first time. • The chemotaxonomic significance of the isolates is discussed. [ABSTRACT FROM AUTHOR]

Inunicosides A−K (1–11), eleven unusual polyacylated ent -kaurane diterpenoid glycosides, were isolated from the flowers of a traditional Chinese herbal plant Inula japonica. Their structures with absolute configurations were determined on the basis of comprehensive spectroscopic analyses, chemical degradation, enzymatic hydrolysis and ECD experiments. Among these isolates, inunicoside K (11) showed mild antibacterial activity against Staphylococcus aureus ATCC 25923. Diterpene constituents have been rarely reported in the Inula species, and thus the discovery of this panel of compounds greatly enriches the chemical diversity of metabolites from the genus Inula. Image 1 • Eleven unusual 18-norditerpenoid glycosides were isolated from the flowers of Inula japonica. • The absolute configurations were determined via chemical derivatization, enzymatic hydrolysis and ECD analysis. • An intact diterpenoid glycoside with 4-geminal carboxyl groups showed moderate antibacterial activity. • The discovery of these compounds enriches the chemical diversity of metabolites from Inula species. [ABSTRACT FROM AUTHOR]

Abstract Seven new pentacyclic triterpenoids including six ursane-type, marinoids A–F (1 – 6), and one oleanane-type, marinoid G (7), along with five known analogues (8 – 12), were separated from the roots of Morinda officinalis var. officinalis. Their structures were assigned by spectroscopic means especially analysis of 2D NMR data, with the absolute configurations of 1 and 2 being determined via comparison of their experimental ECD spectra with the computed ones. Selective compounds displayed cytotoxic activity against two human osteosarcoma cell lines and also antibacterial effects against one Gram positive and one Gram negative strains. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Twenty-seven monoterpene indole alkaloids (MIAs) including three new ones were isolated from the plant of Rhazya stricta . Their structures were elucidated by analyses of HRMS and NMR data. Secopleiocarpamine A ( 1 ) represents a novel 2,3- seco pleiocarpamine type MIA possessing a cyano group. A possible biosynthetic pathway for 1 was postulated. All compounds were evaluated for their inhibitory activities against six Candida strains, and the results showed that 2 , 5 , 12 , 21 , 23 , and 27 exhibited moderate inhibitory activities with MIC values ranging from 3.125 to 50 μg/mL. [ABSTRACT FROM AUTHOR]

A pair of undescribed bicoumarin enantiomers, ( P )/( M )-corinepalensin A, two undescribed prenylated coumarins, corinepalensins B and C, along with ten known coumarins were isolated from the twigs of Coriaria nepalensis . ( P )/( M )-corinepalensin A feature a rare C-5 C-5′ axially chiral linkage between two prenylated coumarin monomers. Their structures were determined by a combination of spectroscopic methods, single crystal X-ray diffraction, and ECD calculations. All isolates were evaluated for the inhibitory activity against phosphodiesterase-4 (PDE4), which is a drug target for the treatment of asthma and chronic obstructive pulmonary disease. Compounds ( P )-corinepalensin A, ( M )-corinepalensin A, corinepalensin B, norbraylin, braylin, and nepalin C exhibited significant inhibition with IC 50 values ranging from 0.43 to 7.15  μ M. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Salvia plebeia R. Brown, a traditional Chinese medicinal herb, has been used to treat inflammatory diseases such as cough, hepatitis, and diarrhea for a long history. Aim of the study The aim of the present study was to isolate and identify potential anti-inflammatory agents from the herb of S. plebeia , which may have contributed to its folk pharmacological use in the treatment of inflammatory diseases. Material and methods The aerial parts of S. plebeia were extracted with 95% ethanol and separated by silica gel, RP-C 18 , Sephadex LH-20, and HPLC. The structures of the isolated compounds were elucidated by extensive spectroscopic analysis (MS, NMR, and X-ray). Anti-inflammatory activities of all compounds were evaluated by the model of LPS-induced up-regulated of NO in Raw264.7 macrophages. The expression levels of cytokine (TNF-α) and proteins (iNOS and COX-2) were assessed by ELISA kit and Western blotting analysis, respectively. Furthermore, the influences of salviplenoid A ( 1 ) on NF-κB and MAPK signaling pathways were determined by Western blotting analysis and immunofluorescence assay. Results Six new ( 1 − 6 , salviplenoids A–F) and ten known ( 7 – 16 ) sesquiterpenoids were isolated from the herb of S. plebeia . The absolute configurations of compounds 1 , 2 , and 7 were determined by X-ray diffraction. The new eudesmane-type sesquiterpenoid, salviplenoid A ( 1 ), significantly decreased the release of NO and TNF-α and the expression of proteins iNOS and COX-2. In addition, the biochemical mechanistic study indicated that 1 regulated the NF-κB dependent transcriptional activity through inhibiting the nuclear translocation of p50/p65 dimer and decreasing the phosphorylation of IκB and Erk1/2. Conclusions Among all sesquiterpenoids isolated from S. plebeian , the new salviplenoid A ( 1 ) exhibited the most potent anti-inflammatory activity in LPS-induced Raw264.7 cells via inhibition of NF-κB and Erk1/2 signaling pathways. [ABSTRACT FROM AUTHOR]

Twenty-two labdane-type diterpenoids, including ten pairs of 15-epimers and a pair of 13,15-epimers, were obtained from the aerial parts of a well-known medicinal plant Leonurus japonicus Houtt. While these epimers were separated by chiral HPLC, their structures were established mainly via spectroscopic methods especially NMR, X-ray crystallography and ECD techniques. Among them, seventeen compounds, encompassing three pairs of solvolysis artefacts likely due to the use of ethanol as extracting solvent, were reported for the first time in the current work. Our preliminary anti-inflammatory screening demonstrated that seven diterpenoids displayed noteworthy inhibitory effect on the NO production in LPS-induced RAW264.7 cells. In addition, the release of pro-inflammatory factors TNF-α, IL-1β and IL-6, as well as the expression of iNOS and COX-2 proteins, was also suppressed by the unreported 15,16-epoxy-6β-hydroxy-15α-methoxy-7,16-dioxolabd-8,13-diene. Further investigation into the preliminary anti-inflammatory mechanism of this compound indicated that it could block the activation of NF-κB signaling pathway. Twenty-two labdane-type diterpenoids including 17 previously unreported ones were obtained from Leonurus japonicus , with selective ones showing noteworthy anti-inflammatory effects. [Display omitted] • Seventeen unreported labdane-type diterpenoids were obtained from Leonurus japonicus. • The structures were elucidated by analyses of spectroscopic data and X-ray crystallography. • Selective compounds showed noteworthy inhibitory effect on the NO production. • Compound 1 could block the activation of NF-κB signaling pathway. [ABSTRACT FROM AUTHOR]

Five new lanostane-type triterpenoids, ganoderenses A − E ( 1 − 5 ), two new lanostane nor-triterpenoids, ganoderenses F and G ( 6 and 7 ), along with 13 known analogues ( 8 − 20 ) were isolated from the fruiting body of Ganoderma hainanense . Their structures were determined by combined chemical and spectral methods, and the absolute configurations of compounds 1 and 13 were confirmed by single crystal X-ray diffraction. All compounds were evaluated for inhibitory activity against thioredoxin reductase (TrxR), a potential target for cancer chemotherapy with redox balance and antioxidant functions, but were inactive. [ABSTRACT FROM AUTHOR]

Chemical fractionation of the EtOH extract of the roots of a traditional Chinese herb, Morinda officinalis , afforded an array of methyl 2-naphthoate derivatives (1 – 9) including four pairs of enantiomers (1 – 4), two pimarane diterpenes and two ursane triterpenoids. Among them, eight compounds (1a / 1b - 3a / 3b , 11 and 13) were reported in the current work for the first time. The structures of the new compounds, including their absolute configurations, were defined by spectroscopic analyses in combination with quantum chemical electronic circular dichroism (ECD) and gauge-independent atomic orbital (GIAO) NMR calculations. All the isolates were evaluated for their inhibitory effect on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells, and the enantiomers 1a and 3b exhibited moderate activity with IC 50 values of 41.9 and 26.2 μM. Meanwhile, compound 3b also dose-dependently inhibited the secretion of two pro-inflammatory cytokines TNF-α and IL-6 in the same cell model. [Display omitted] • Three pairs of new methyl 2-naphthoate enantiomers were isolated from Morinda officinalis. • One new pimarane diterpenoid and one new unstable ursane triterpenoid were also identified. • Two new enantiomers 1a and 3b showed mild inhibition against the release of NO in RAW264.7 cells. • Compound 3b could dose-dependently block the secretion of pro-inflammatory factors TNF-α and IL-6. [ABSTRACT FROM AUTHOR]

Chemical investigation of the South China Sea soft coral Sarcophyton solidum has led to the isolation of one new ( 1 ) and seven known ( 2 – 8 ) diterpenoids, including three sarsolenanes ( 1 – 3 ), two capnosanes ( 4 and 5 ), and three cembranes ( 6 – 8 ). Sarsolilide B ( 4 ) was firstly confirmed by single-crystal X-ray diffraction. Compounds 1 , 3 , 4 , and 6 – 8 were isolated from S . solidum for the first time, and 1 , 2 , and 4 – 7 were considered as the chemotaxonomic markers for the species S . solidum . [ABSTRACT FROM AUTHOR]

Abstract: Background: Thionamide antithyroid drugs (ATDs) have certain disadvantages and are associated with some adverse events (AEs). To overcome the problems associated with ATDs, a compound antithyroid ointment (CATO) containing methimazole (MMI) and hydrocortisone has been developed for use as a local thyroid treatment (LTT). Objective: The aim of this study was to assess the clinical effectiveness and tolerability of CATO LTT in patients with Graves disease (GD). Methods: This was a prospective, randomized, open-label, parallel-group clinical trial conducted at the Provincial Hospital Affiliated to Shandong University (Jinan, China). Patients with GD aged 19 to 65 years were randomized to receive either CATO LTT 0.3 g/d or oral MMI 37.5 mg/d (control group) treatment for 18 months, with a 4-year follow-up period. Hyperthyroid symptoms, thyroid function, granulocyte count, liver function, and AEs were assessed at baseline and every 2 weeks until serum thyroid hormone (TH) concentration normalized, at which point patients were assessed monthly. The primary efficacy end points were the duration of treatment required for serum TH concentration to normalize and the remission rate after completing the 18-month treatment regimen. Results: A total of 154 patients (133 women, 21 men; mean [SD] age, 39.6 [11.8] years; all Han Chinese) participated in the study; all patients completed the 18-month treatment period. Compared with the MMI group (n 76), the CATO- treated group (n 78) had a significantly shorter median (range) time to restoration of normal serum thyroid hormone concentration (43 [12–150] vs 22 [7–60] days; P < 0.001), a significantly lower rate of recurrence of hyperthyroidism (309/1520 [20.3%] vs 193/1368 [14.1%] person-time; P < 0.001), a significantly lower drug hypothyroidism rate (185/1520 [12.2%] vs 54/1368 [3.9%] person-time; P < 0.001), and a higher remission rate (year 1:46/69 [66.7%] vs 65/72 [90.3%] patients, P 0.001; year 2:40/69 [58.0%] vs 60/72 [83.3%] patients, P - 0.001; year 3:34/69 [49.3%] vs 57/72 [79.2%] patients, P < 0.001; and year 4:30/69 [43.5%] vs 55/72 [76.4%] patients, P < 0.001). Systemic AEs occurred in 6 patients (7.9%) in the MMI group (drug neutropenia, 2 patients [2.6%]; epistaxis, 1 [1.3%]; hepatopathy, 1 [1.3%]; and other systemic AEs, 2 [2.6%]), while no systemic AEs were observed/reported in the CATO group. Conclusion: This study suggests that CATO LTT was well tolerated and more effective than oral MMI treatment in controlling thyrotoxicosis and promoting remission of GD in these Han Chinese patients. [Copyright &y& Elsevier]

Chemical fractionation of the EtOH extract of a medicinal macro fungus, Inonotus obliquus , afforded an array of lanostane-type triterpenoids (1 − 11) including two new ones (1 and 8). The structures of these compounds were determined on the basis of spectroscopic analyses, single crystal X-ray crystallography of 3 – 6 and biosynthetic considerations. With the confirmatory structural information provided by X-ray diffraction analysis in hand, several previously reported 21,24-cyclolanostanes, such as inonotsutriols A–C and (20 R ,21 S ,24 S)-21,24-cyclopenta-3 β ,21,25-trihydroxylanosta-8-ene, were structurally corrected. In addition, the NMR data of other types of 21,24-cyclo triterpenoids were also re-examined and structural revisions were thus suggested. Compounds 2 , 6 and 8 showed significant cytostatic effects against a panel of tumor cell lines with IC 50 values ranging from 7.80 to 18.5 μM. Further assays established that compound 2 exerted promising in vitro anti-breast cancer potential by inhibiting the proliferation and migration of 4T1 cells. [Display omitted] • Two new lanostane-type triterpenoids were isolated from fungus Inonotus obliquus. • The absolute configurations were characterized by single-crystal X-ray diffraction. • The structures of several previously reported 21,24-cyclolanostanes were corrected. • Selective compounds showed cytotoxicity against lung, breast & gastric tumor cells. • Compound 2 dose-dependently inhibited the proliferation and migration of 4 T1 cells. [ABSTRACT FROM AUTHOR]

Six undescribed low-polarity compounds including three rare 14-methylergostane steroids (1 – 3), one euphane triterpenoid (4) and two octadecanoic acid ethyl esters (5 and 6), along with ten previously reported terpenyl cometabolites (7 – 16), were isolated from the stems of Tinospora sagittata. Their structures were determined by detailed spectroscopic analyses and comparison with structurally related known compounds, and all of them have been reported from T. sagittata for the first time. Compounds 4 – 6 and 16 showed potent in vitro inhibitory activity against the diabetes target α -glucosidase, while compounds 10 and 14 displayed promising antibacterial effect toward Staphylococcus aureus ATCC 25923. [Display omitted] • New 14-methylergostane steroids, euphane triterpenoid and octadecanoid derivatives were separated from Tinospora sagittata. • All the compounds have been reported from Tinospora sagittata for the first time. • Compounds 4 – 6 and 16 showed potent α-glucosidase inhibitory activity. • Compounds 10 and 14 exerted promising antibacterial effect toward Staphylococcus aureus. [ABSTRACT FROM AUTHOR]

Six new compounds including four prenylated indole alkaloids (1 – 4) and two lignans (5 – 6), along with eight known cometabolites (7 – 14), were isolated from the flower buds of Tussilago farfara. Structures of the new compounds were elucidated by comparison with structurally related known analogues and also by comprehensive spectroscopic analyses. Their absolute configurations were determined by a variety of means including Mosher's method, Marfey's analysis, electronic circular dichroism (ECD) exciton chirality method and ECD calculations. Our bioassays have established that compounds 1 and 2 showed potent α -glucosidase inhibitory activity with IC 50 values of 105 ± 4.7 and 35.2 ± 3.2 μM, respectively, while the known 13 and 14 exerted moderate DPPH radical scavenging activity with IC 50 values of 45.2 ± 2.9 and 29.2 ± 2.0 μM, respectively. Unlabelled Image • Four new prenylated indole alkaloids and two new lignans were isolated from Tussilago farfara. • Structures with absolute configurations of the new compounds were fully characterized. • The new indole alkaloids 1 and 2 showed potent α -glucosidase inhibitory activity. • Two known lignans 13 and 14 exerted moderate antiradical effect. [ABSTRACT FROM AUTHOR]

Three new thiophene derivatives, ecliprostins A–C (1 – 3), have been isolated from the aerial parts of a Compositae medicinal plant Eclipta prostrata , and structures of them have been elucidated by comprehensive spectroscopic analyses. Both ecliprostins A (1) and B (2) feature an acetylenic bithiophenyl backbone and also incorporate an isovalerate moiety, while ecliprostin C (3) is a symmetrical dimer of compound 1 and represents the first example bonded via an ether bridge among the very limited natural dimers. All three compounds show antibacterial activity against Staphylococcus aureus. Three new antibacterial thiophene derivatives, including an unusual dimer with an ether bridge, were isolated and identified from the aerial parts of Eclipta prostrata. Unlabelled Image • Three new acetylenic thiophenes were isolated from the aerial parts of Eclipta prostrata. • The first example linked via an ether bond of natural acetylenic thiophene dimers was reported. • All the isolates showed antibacterial activity against Staphylococcus aureus. [ABSTRACT FROM AUTHOR]

Chemical fractionation of the ethanolic extract of Eclipta prostrata yielded a series of unreported terpenoid constituents, including a rare 6/6/6/6-fused tetracyclic triterpenoid, a pentacyclic triterpenoid, two pentacyclic triterpenoid saponins, a diterpenoid and a sesquiterpenoid. Structures were assigned to these compounds on the basis of comprehensive spectroscopic analyses, with the absolute configurations of the tetracyclic triterpenoid, the diterpenoid and the sesquiterpenoid being determined via explanation of electronic circular dichroism data. Screening of these isolates in an array of bioassays revealed antibacterial, cytotoxic and α -glucosidase inhibitory activities for selective compounds. Of particular interest, the tetracyclic triterpenoid showed very strong inhibition against α -glucosidase with an IC 50 of 0.82 ± 0.18 μM, being 103-fold as active as the positive control acarbose. Six unreported terpenoids including a rare 6/6/6/6 tetracyclic triterpenoid were isolated from Eclipta prostrata. Their antibacterial, cytotoxic and α -glucosidase inhibitory activities were evaluated. Image 1 • Six unreported terpenoid constituents were obtained from the aerial parts of Eclipta prostrata. • Experimental and calculated ECD data were compared to establish absolute configurations. • An oleanane-type triterpenoid saponin showed mild antibacterial activity against S. aureus. • Two 28-noroleanane-type triterpenoid saponins showed cytotoxicity against two cancer cells. • A rare lemmaphyllane-type triterpenoid displayed strong inhibition against α -glucosidase. [ABSTRACT FROM AUTHOR]