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Diterpenoids occupy an important slot of the natural products diversity space with wide ranges of bioactivities and complex structures, providing potential applications for the development of therapeutics. In this study, we reported four new abietane-type diterpenoids viroxocin B-E (1–4), a new totarane-type diterpenoid viroxocin F (5), and a new sempervirane-type diterpenoid viroxocin G (6) along with four known compounds (7 – 10), isolated and identified from a widely used Traditional Chinese Medicine, Isodon serra (I. serra). Their structures were established by spectroscopic data analysis, experimental and calculated electronic circular dichroism (ECD) data, as well as X-ray diffraction analysis. Compounds 2 , 5 , 7 , 8 and 10 exhibited promising anti-inflammatory activities in lipopolysaccharide (LPS)-induced RAW 267.4 cells, and their inhibition rates on NO production were more than 60% at 10 μM. Compound 7 showed cytotoxicity against human renal cell carcinoma 769P at 20 μM, the inhibition rate was 52.66%. [Display omitted] [ABSTRACT FROM AUTHOR]

Three undescribed sesquiterpenes, designed as pichinenoid A-C (1 – 3), along with nine known ones (4 – 12) were isolated from the stems and leaves of Picrasma chinensis. The new isolates including their absolute configurations were elucidated based on extensive spectroscopic methods, single crystal X-ray diffraction, and electronic circular dichroism (ECD) experiments, as well as comparison with literature data. Structurally, compounds 1 and 2 are descending sesquiterpenes, while pichinenoid C (3) is a rare sesquiterpene bearing a 2-methylenebut-3-enoic acid moiety at the C-6 side chain. All the isolated compounds were tested for their neuroprotective effects against the H 2 O 2 -induced damage on human neuroblastoma SH-SY5Y cells, and most of them showed moderate neuroprotective activity. Especially, compounds 1 , 3 – 5 , and 7 showed a potent neuroprotective effect at 25 or 50 μM. Moreover, the neuroprotective effects of compounds 1 and 4 were tested on a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinson's disease (PD) mouse model. Results of western blot and immunofluorescence indicated that compound 4 significantly counteract the toxicity of MPTP, and reversed the expression of tyrosine hydroxylase (TH) in substantia nigra (SN) and striatum (ST) of the mouse brain. Interestingly, western blot data suggested compound 4 also enhanced B-cell lymphoma-2 (Bcl-2) and heme oxygenase 1 (HO-1) expressions in the brain tissues from MPTP damaged mouse. [Display omitted] [ABSTRACT FROM AUTHOR]

Seven new triterpenoids, named Adeterpenoids A-G (1 – 7) and eight known compounds (8 – 15), were isolated from 70% ethanol extract of the roots of Adenophora tetraphylla (Thub.) Fisch. The compounds from it were separated by column chromatography techniques such as silica gel, ODS, and preparative liquid chromatography. Their structures were clarified based on extensive spectral analysis (1D, 2D-NMR, HR-ESI-MS, IR, UV, and CD) and comparison with the literature. At the same time, all compounds were evaluated for their cytotoxic activity against the LN229 (human glioma cell line). The results showed that compounds 2 , 5 , 6 , 13, and 14 had a significant inhibitory effect on LN229 cells. [Display omitted] [ABSTRACT FROM AUTHOR]

Nine polyacetylenes, including five new compounds named sadivaethynes E -I (1 – 5), were isolated from the roots of Saposhnikovia divaricata. Structural elucidation of compounds 1 – 5 was established by extensive spectroscopic analysis, quantum chemical calculations and DP4+ probability analysis. Among them, the absolute configuration of compound 1 – 2 , 4 – 5 was unambiguous determined by ECD. Also, all compounds were evaluated for cytotoxicity against two human cancer cell lines (A549, HEPG2) in vitro, compound 9 showed moderate inhibitory effect with an IC 50 value of 11.66 μM against HEPG2. [Display omitted] • Five undescribed compounds were isolated from the roots of Saposhnikovia divaricata. • The structures were characterized chemically by NMR, quantum chemical calculations and CD data analysis. • Compound 9 showed moderate inhibitory effect with an IC 50 value of 11.66 μM against HEPG2. [ABSTRACT FROM AUTHOR]

Diabetes mellitus stands as a metabolic ailment marked by heightened blood glucose levels due to inadequate insulin secretion. The primary aims of this investigative inquiry encompassed the isolation of phytochemical components from the bark of Kopsia teoi , followed by the assessment of their α-amylase inhibition. The phytochemical composition of the K. teoi culminated in the discovery of a pair of new indole alkaloids; which are 16- epi -deacetylakuammiline N (4)-methylene chloride (akuammiline) (1), and N (1)-methoxycarbonyl-11-methoxy-12-hydroxy-Δ14–17-kopsinine (aspidofractinine) (2), together with five known compounds i.e. kopsiloscine G (aspidofractinine) (3), akuammidine (sarpagine) (4), leuconolam (aspidosperma) (5), N -methoxycarbonyl-12-methoxy-Δ16, 17-kopsinine (aspidofractinine) (6), and kopsininate (aspidofractinine) (7). All compounds were determined via spectroscopic analyses. The in vitro evaluation against α-amylase showed good inhibitory activities for compounds 5 – 7 with the inhibitory concentration (IC 50) values of 21.7 ± 1.2, 34.1 ± 0.1, and 30.0 ± 0.8 μM, respectively compared with the reference acarbose (IC 50 = 34.4 ± 0.1 μM). The molecular docking outputs underscored the binding interactions of compounds 5 – 7 ranging from −8.1 to −8.8 kcal/mol with the binding sites of α-amylase. Consequently, the outcomes highlighted the anti-hyperglycemic attributes of isolates from K. teoi. [Display omitted] [ABSTRACT FROM AUTHOR]

Angiotensin I-converting enzyme (ACE) inhibition is currently a common method for the treatment and control of hypertension. In this study, four new (1–4) and one known (5) cycloartane triterpenoids were isolated from the leaves of Swietenia macrophylla by chromatographic techniques and identified by their spectroscopic data and a comprehensive comparison of published data. The triterpenoids were evaluated for their ACE inhibitory potential using in vitro inhibition assays and in silico methods. The inhibition assay and enzyme kinetics results showed that the most active triterpenoid, compound 4 , inhibited ACE in a mixed-type manner with an IC 50 value of 57.7 ± 6.07 μM. Computer simulations revealed that compound 4 reduces the catalytic efficiency of ACE by competitive insertion into the active pocket blocking the substrate, and the binding activity occurs mainly through hydrogen bonds and hydrophobic interactions. The study showed that S. macrophylla can be a source of bioactive material and the ACE inhibitory triterpenoid could be a potential antihypertensive agent. [Display omitted] • Four new cycloartane triterpenoids were isolated from Swietenia macrophylla. • 3β,16β-dihydroxy-29-norcycloartan-24-one (4) inhibited ACE in a mixed-type manner. • Hydrogenation at C-16 and substitution by the carbonyl group at C-24 enhanced the ACE inhibitory activity of the triterpenoids. • Computational simulation analyses showed that hydrogen bonds were the major binding forces. [ABSTRACT FROM AUTHOR]

Six anthraquinones were isolated from Morinda scabrida Craib, an unexplored species of Morinda found in the tropical forest of Thailand. All six anthraquinones showed cytotoxicity against A549 lung cancer cells, with the most active compound, nordamnacanthal (MS01), exhibiting the IC 50 value of 16.3 ± 2.5 μM. The cytotoxic effect was dose-dependent and led to cell morphological changes characteristic of apoptosis. In addition, flow cytometric analysis showed dose-dependent apoptosis induction and the G2/M phase cell cycle arrest, which was in agreement with the tubulin polymerization inhibitory activity of MS01. Molecular docking analysis illustrated the binding between MS01 and the α/β-tubulin heterodimer at the colchicine binding site, and UV–visible absorption spectroscopy revealed the DNA binding capacity of MS01. [Display omitted] • Six anthraquinones were isolated from Morinda scabrida Craib, an unexplored species. • Nordamnacanthal exhibited the IC 50 value of 16.3 ± 2.5 μM against A549 lung cancer cells. • Apoptosis and the G2/M phase cell cycle arrest were induced by nordamnacanthal. • Antitubulin activity supported the cell cycle arrest activity of nordamnacanthal. [ABSTRACT FROM AUTHOR]

Eight undescribed alkaloids named corydalisine D-K (1 – 7), including one isoquinoline benzopyranone alkaloid (1), one benzocyclopentanone alkaloid (2), four benzofuranone alkaloids (3 , 4 , and 5a / 5b) and two protoberberine alkaloids (6 and 7), along with fourteen known ones, were isolated from the Corydalis saxicola. Their structures, including absolute configurations, were unambiguously identified using spectroscopic techniques, single-crystal X-ray diffraction and electron circular dichroism calculation. Compounds 2 , 14 and 21 exhibit antiproliferative activity against five cancer cell lines. The aporphine alkaloid demethylsonodione (compound 14), which exhibited the best activity (IC 50 = 3.68 ± 0.25 μM), was subjected to further investigation to determine its mechanism of action against the T24 cell line. The molecular mechanism was related to the arrest of cell cycle S-phase, inhibition of CDK2 expression, accumulation of reactive oxygen species (ROS), induction of cell apoptosis, inhibition of cell migration, and activation of p38 MAPK signaling pathway. The results indicated that 14 could be used as a potential candidate agent for further development of anti-bladder transitional cell carcinoma. [Display omitted] • Eight new alkaloids were characterized from the DCM extract of Corydalis saxicola Bunting. • Compound 14 as a CDK2 inhibitor further accelerated apoptotic rate of T24 cells and induced apoptosis by activating the p38 MAPK signaling pathway dependent on the ROS levels. [ABSTRACT FROM AUTHOR]

Four undescribed neolignan analogs, together with eight known compounds, were isolated from the twigs of Pinus koraiensis (Korean pine). The chemical structure of the isolated compounds was determined through extensive spectroscopic analysis and chemical method. Their relative and absolute configurations were assigned through a well-established empirical rule and electronic circular dichroism (ECD) analysis, respectively. Four compounds (3 and 9 – 11) at 20 μM concentration showed significant neurotrophic effect by inducing nerve growth factor (NGF) secretion in C6 cells with the stimulation levels a range of 140.82 ± 4.62% to 160.04 ± 11.04%. Additionally, the result indicated that the glycosylation of neolignan led to an improvement in neurotrophic activity compared to their aglycone form. A compound (7) inhibited nitric oxide production with an IC 50 value of 31.74 μM in LPS-activated BV2 cells. Twelve neolignans, including four undescribed compounds, were isolated from the twigs of Pinus koraiensis and their neurotrophic and anti-inflammatory activities were assessed. [Display omitted] • Four undescribed neolignans were isolated from the twigs of Pinus koraiensis. • The chemical structures established by spectroscopic analysis. • The stereochemistry was elucidated through an empirical rule and ECD analysis. • Some isolates showed neurotrophic activity by inducing NGF secretion in C6 cells. [ABSTRACT FROM AUTHOR]

Crude extracts prepared from aerial parts and nut galls of Quercus floribunda Lindl. Ex. A. Camus were evaluated for phytochemical screening, in vitro antioxidant, and in vivo analgesic, anti-inflammatory and antipyretic activities. Various solvents including methanol (M), acetone (A), distilled water (DW), distilled water + methanol (DWM) were used for extraction. Highest total phenolic (66.9 ± 0.05 μg GAE/mgE) and flavonoid content (38.4 ± 0.72 μg QE/mgE) were measured in QFAA extract by colorimetric methods. Cumulative maximum concentrations of polyphenols were quantified in QFMG, QFAA, and QFMA extracts i.e. 19.036, 15. 574 and 11.647 μg/mg of extract by RP-HPLC analysis. From aerial parts extracts, apentacyclic tritepenoid, glutinol was isolated using column chromatography techniques and structure was elucidated using spectroscopic techniques. QFDWMA (205.5 ± 0.56 μg AAE/mg of extract) showed highest total reducing power while highest total antioxidant capacity (207.1 ± 0.49 AAE/mg of extract) and free radical scavenging potential (96.1 ± 0.42%) were observed in QFAA extract. QFAA extract showed significant (p ≤ 0.001) analgesic potential in different pain models i.e. hot plate method, cold plate method, Haffner's tail clip method and acetic acid induced writhing assay having 50.20%, 62.07%, 57.26% and 70.49% analgesia respectively at 300 mg/kg. QFAA extract showed maximum anti-inflammatory activity in croton oil induced edema (68.83%) and in carrageenan induced paw edema models (72.32%) at 300 mg/kg concentration. QFAA extract markedly reduced the rectal temperature at 300 mg/kg concentration, in brewer's yeast induced pyrexia model. Detailed investigations can be executed in future to determine the molecular mechanisms of these pharmacological attributes. [Display omitted] [ABSTRACT FROM AUTHOR]

Five new compounds including two stilbenes, designated thujasutchins A (1) and B (2), two phenolic compounds namely thujasutchins C (3) and D (4), as well as one sesquiterpene thujasutchin E (5), were isolated from the 95% ethanolic extract from the trunks and roots of Thuja sutchuenensis. Their structures were determined by means of extensively spectroscopic analysis including UV, IR, HRESIMS, 1H and 13C NMR (COSY, HSQC, HMBC). Moreover, compounds 1 , 3 – 5 were evaluated for in vitro cytotoxic activities against SF-268, MCF-7, HepG-2, and A549 tumor cell lines. Unlabelled Image [ABSTRACT FROM AUTHOR]

Two kinds of biologically active compounds were isolated from the MeOH extract of the Early Cretaceous Burmese amber [99 million years ago (Ma)], which is older than the K-Pg boundary (65 Ma). These compounds had inhibitory activity against the hypersensitive mutant yeast strain (zds1 ∆ erg3 ∆ pdr1 ∆ pdr3∆) with respect to Ca2+ signal transduction. They were identified as 16,17-bisnordehydroabietic acid (1) and 16,17-bisnorcallitrisic acid (2), respectively, on the basis of spectral analyses including HREIMS, 1D, and 2D NMR. Both have faint growth restoring activities around the clear inhibition zone against the mutant yeast on the 0.31–0.16 μg/spot. This is the first report of direct structural elucidation of 1 and 2 and the biologically active compounds derived from Burmese amber. Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Six previously undescribed naturally occurring meroterpenoids (2, 5–9) together with seven known meroterpenoids (1, 3, 4, 10–13) were isolated from the root plant of Arnebia euchroma. Their structures and absolute configurations were determined by extensive 1D (1H NMR, 13C NMR) and 2D NMR (1H 1H COSY, DEPT, HMQC, HMBC, NOESY) spectroscopic methods, spectroscopy high resolution mass spectrometry, as well as DFT and MM2 force-field calculations. Meroterpenoids 1–13 were evaluated for their cytotoxicities against human liver cancer cell lines SMMC-7721, HepG2, QGY-7703 and HepG2/ADM. Meroterpenoid 5 exhibited the most potent activity with IC 50 values of 6.40 ± 0.51, 3.86 ± 0.28, 3.43 ± 0.27 and 11.31 ± 0.67 μM, respectively. Meroterpenoid 4 exhibited significant growth inhibitory effects against HepG2/ADM with IC 50 at 18.77 ± 1.23 μM, and meroterpenoid 8 with IC 50 at 5.41 ± 0.51 and 6.18 ± 0.47 μM against HepG2 and QGY-7703, respectively. These were more potent than the positive drug, Cisplatin. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Four meroterpenoids, applanatumols F (1), H (3), I (2), and lingzhiol (4) were isolated from the 95% EtOH extract of the fruiting bodies of Ganoderma sinense. Their structures were established on the basis of NMR spectroscopic analyses, optical rotatory dispersion data, ECD spectra, and X-ray crystallography. Compounds 1 , 2 , 4 existed as racemic mixtures ((+) 1a , 2a , 4a ; (−) 1b , 2b , 4b), while 3 as a single enantiomer. Base on the seperated enantiomers, we sought to explicit possible effects of compounds 1 – 4 on hydrogen peroxide (H 2 O 2)-induced cell death and to determine their underlying molecular mechanisms in human normal liver LO2 cells. Among them, compound 2a treatment effectively protected LO2 cells against H 2 O 2 -induced cell damage and apoptosis. H 2 O 2 exposure increased ROS, which was inhibited by 2a treatment. Mitochondrial membrane potential decrease, nuclear fragments, caspase-3 activation and PARP cleavage were also arrested by 2a. Further, increased levels of Nrf2, HO-1, phosphorylation Akt and up-regulation of antioxidant enzymes were detected in 2a treated cells, indicating that the anti-oxidative effects of 2a might protect LO2 cells against oxidative damage via PI3K/Akt-mediated activation of Nrf2/HO-1 pathway. In addition, compound 2a showed potential protective role of cardiomyocyte from ischemia/reperfusion injury, and pretreatment with 2a could decrease CK and LDH levels and increase GSH level. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Stilbene derivatives, the principal constituent of Rheum undulatum L., are known to have a wide range of biological activities, such as anti-allergic, anti-diabetic, antioxidant, and anti-inflammatory activities. A phytochemical study on the methanol extract of Korean rhubarb (R. undulatum L.) led to the isolation of nine stilbene derivatives (1 – 9) and one flavonoid (10). All structures were elucidated based on a comprehensive analysis of spectroscopic data. Compound 1 (5-methoxy- cis -rhapontigenin) was elucidated as a new compound, while compound 2 (5-methoxy- trans -rhapontigenin) was isolated from a natural source for the first time. Among the isolated compounds, stilbene derivatives (7 – 9) showed a strong inhibitory effect on protein tyrosine phosphatase 1B (PTP1B) with IC 50 values ranging from 4.25 to 6.78 μM, which was significantly higher than that of the positive control, ursolic acid (IC 50 = 11.34 μM). Furthermore, for the first time, kinetic analysis and molecular docking simulations were performed in order to understand the inhibition type as well as the interaction and binding mode of the active stilbenes (7 – 9) with PTP1B. Our results showed that the types of PTP1B inhibition were noncompetitive for ɛ-viniferin (8) and mixed for piceatannol (7) and δ-viniferin (9). Docking simulations of these stilbenes demonstrated negative binding energies and close proximity to residues in the binding pocket of PTP1B. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Gracilistones A (1) and B (2), two new eudesmane-type sesquiterpenoids with an unusual tetrahydrofuran-fused 6/6/5 tricyclic ring system, were obtained from Acanthopanax gracilistylus under the guidance of LC-MS investigation. Their structures and absolute configurations were assigned by extensive spectroscopic analyses and quantum calculation methods. Compounds 1 and 2 showed potent inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages, compared with the positive control L-NMMA. In addition, compounds 1 and 2 were also evaluated for their antioxidant (DPPH• and ABTS•+) and xanthine oxidase (XO) inhibitory activities, and they exhibited weak inhibitory effects at 100 μM. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Two new compounds, odoratisol E (1) and decurrenal A (2), together with 12 known compounds were isolated from the twig and leaf extracts of Mitrephora wangii HU (Annonaceae). All structures were elucidated by spectroscopic methods. The structure of compound (+)- 6 was also confirmed by X-ray diffraction analysis. The absolute configurations of odoratisol E and decurrenal A were determined by comparison of their electronic circular dichroism (ECD) spectra with those of related known compounds. Most of the isolated compounds were evaluated for their antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. Compounds 4 and (+)- 6 displayed potent ABTS radical scavenging activity with IC 50 values of 11.9 ± 1.8 and 10.8 ± 1.7 μM, respectively, which is better than that of standard compound, ascorbic acid, (IC 50 = 19.3 ± 0.1 μM). Compound 9 showed moderate DPPH radical scavenging activity with an IC 50 value of 38.7 ± 0.8 μM. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract β -Carboline alkaloids in Picrasma quassioides (D. Don) Benn. have been proven to possess inhibitory activity against various cancer cells. However, their effect on hepatocellular carcinoma and structure-activity relationships (SAR) have not been systematically reported. In this work, bioactivity-directed fractionation of P. quassioides led to the separation of active fraction A2–2. A total of 39 β -carbolines, including 4 new ones (1–4), were obtained from the active fraction. Moreover, all the isolated compounds were identified in the active fraction A2–2 by LC-MS. The cytotoxicity on HepG2 and Hep3B cells of all compounds was screened by MTT assay, and the SAR were established. The SAR were also supported by the apoptosis ratio of HepG2 cells using flow cytometry analysis after treatment with potential compounds 1 , 2 , 9 , 10 , 12 , 29 , 36 and 38. It suggested that these active compounds caused death of hepatoma cells through apoptosis induction. In addition, further study revealed that compounds 12, 29, 36 significantly activated caspase-3 in HepG2 cells. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

A new bakuchiol compound Δ 11 -12-hydroxy-12-dimethyl bakuchiol ( 1 ), a new flavanone compound 2( S )-6-methoxy-7- hydroxymethylene-4′-hydroxyl-flavanone ( 8 ), and two new isoflavanone compounds 4′,7-dihydroxy-3′-(6”β-hydroxy-3″,7″-dimethyl-,2″,7″-dibutenyl)-geranylisoflavone ( 9 ) and 4′,7-dihydroxy-3′-(7″-hydroxy-7″-methyl-2″,5″-dibutenyl)-geranylisoflavone ( 10 ) together with eight known compounds ( 2–7 , 11 , 12 ) were isolated from the P. corylifolia . Their structures were elucidated on the basis of spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1/2. Among them, compounds 3 , 9 and 10 were found to exhibit selective inhibitory activity on DGAT1 with IC 50 values ranging from 93.7 ± 1.3 to 96.2 ± 1.1 μM. Compound 1 showed inhibition activity on DGAT1 with IC 50 values 73.4 ± 1.3 μM and inhibition of DGAT2 with IC 50 value 121.1 ± 1.3 μM. [ABSTRACT FROM AUTHOR]

Seven new N -acylanthranilic acid derivatives ( 1–3 , 4a/4b , 5a/5b ) including two pairs of enantiomers ( 4a/4b and 5a/5b ) were isolated from the leaves of Isatis indigotica Fortune. Their chemical structures were elucidated by extensive spectroscopic data analyses. The absolute configurations of compounds 4a/4b and 5a/5b were determined by comparison of the experimental and calculated ECD spectra. All compounds were tested for their anti-A β 1–42 aggregation activity. As a result, compounds 1 (72.1%), 2 (79.8%) and 5a (81.8%) showed stronger inhibitory activity than the positive control curcumin (67.0%). By the comparison between 5a (81.8%) and 5b (63.1%), it was found that stereochemical configurations may affect A β 1–42 aggregation activity, which was discussed through the molecular docking results of compounds 5a and 5b . [ABSTRACT FROM AUTHOR]

Phytochemical investigation of the fruits from Trichilia connaroides led to the isolation of four rare 1,2- seco phragmalin-type limonoids ( 1 – 4 ) with C-7/28 δ -lactone ring along with two known triterpenoids ( 5 – 6 ). An oxygen bridge between C-1 and C-2 formed an rare 9- oxa -tricyclo[3.3.2.1 7,10 ]undecane-2-ene moiety in structure of 1 and 2 , and 3 – 4 possessed a bicyclo[5.2.1 4,10 ]decane skeleton. Their structures were established based on extensive spectroscopic methods and their absolute configurations of 1 were confirmed by TDDFT/ECD calculation and comparative analysis. Compounds 5–6 showed moderate inhibitory effects on Hela tumor cell lines with inhibition ratio values of 83.8% and 87.1% at concentration 40 μM, respectively. [ABSTRACT FROM AUTHOR]

Chemical investigation of Euphorbia helioscopia resulted in the identification of seven new triterpenes named euphorbatrine A-G ( 1 – 7 ), including two (19 α H)-lupane ( 1 – 2 ) and three (9 β H)-lanostane ( 4 – 6 ), which are very rare metabolites from plants. Their structures were elucidated by extensive spectroscopic analysis, X-ray crystallography and chemical methods. Compounds 5 and 6 triggered apoptosis of Hela −/− cell with EC 50 values of 1.59 ± 0.25 and 26.48 ± 0.78 μM, respectively. [ABSTRACT FROM AUTHOR]

The three new metabolites: thiotagetin B ( 2 ) [( Z )-1″-([2,2′-bithiophen]-5-yl)-8″-chloro-6″,11″-dimethylundeca-6″,10″-dien-2″-yn-9″-one], tagetannin A ( 9 ) [3,4-bis-(galloyl-3,5-dimethyl ether)-( α / β )- d -glucopyranose], and tagetannin B ( 10 ) [2,3-bis-(galloyl-3,5-dimethyl ether)-( α / β )- d -glucopyranose], along with ecliptal (5-formyl- α -terthiophene) ( 1 ), 5-(4-hydroxybut-1-ynyl)-2,2′-bithiophene ( 3 ), scopoletin ( 4 ), p -hydroxybenzoic acid ( 5 ), protocatechuic acid methyl ester ( 6 ), gallic acid ( 7 ), and patuletin 7-O- β - d -glucoside ( 8 ) were isolated from the aerial parts of Tagetes minuta L. (Asteraceae). Their structures were verified by extensive spectroscopic analyses as well as by comparison with literature data. The isolated compounds were evaluated for their antioxidant and anti-inflammatory activities using DPPH and enzyme-linked immunosorbent assays, respectively. Compounds 5 – 10 possessed the highest antioxidant potential with a scavenging activity (SCA) ≈ 74 to 93% of DPPH radicals. Moreover, 5 – 10 displayed significant anti-inflammatory potential, while 4 showed moderate activity. Compounds 5 – 10 exhibited significant decreases in NFκB p65, TNF-α, and IL-6 levels at all tested concentrations. [ABSTRACT FROM AUTHOR]

Twenty natural stilbenoids ( 1 − 20 ), including seven new stilbenoids ( 2 , 4 – 7 , 19 , 20 ) and thirteen known stilbenoids ( 1 , 3, 8 – 18 ), were isolated from the stem barks of Acanthopanax leucorrhizus , and six modified stilbenoid derivatives ( 1a , 2a , 4a , 4b , 7a and 17a ) were obtained via methylation, demethylation and isopentenylation of the corresponding isolates ( 1 , 2 , 4 , 7 and 17 ). These stilbenoids were structurally characterized by comprehensive analysis of their spectroscopic data and comparison with literature information, and evaluated for their cytotoxic activities against three human tumor cell lines (leukemia HL-60, hepatoma SMMC-7721 and breast carcinoma MCF-7) in vitro by MTT assay. The results showed that compounds 1a , 4a and 4b showed potent selective cytotoxicity against SMMC-7721 ( IC 50 = 10.16 ± 1.95 μM and 9.76 ± 1.32 μM) and MCF-7 ( IC 50 = 10.72 ± 2.78 μM) cell lines. The cytotoxic evaluation of these structurally modified stilbenoid derivatives have led to the establishment of a structure-activity relationship. [ABSTRACT FROM AUTHOR]

Four new naphthoquinones ( 1 – 4 ), named rhinacanthins S ( 1 ), T ( 2 ), U ( 3 ) and V ( 4 ), together with 13 known naphthoquinones were isolated from the leaf extract of Rhinacanthus nasutus . The structures of isolated compounds were elucidated by spectroscopic methods, especially 1D and 2D NMR spectroscopy and mass spectrometry. Rhinacanthin S ( 1 ) exhibited acetylcholinesterase inhibition activity with a % inhibition value of 48.04 ± 3.25. The known rhinacanthin A ( 5 ) showed cytotoxicity against a MCF-7 cell line with an IC 50 value of 8.79 μM, while rhinacanthin N ( 15 ) was active against the NCI-H187 cell line with an IC 50 = 2.24 μM and Vero cells (IC 50 = 3.00 μM) [ABSTRACT FROM AUTHOR]

Four new labdane diterpenoids, 12 β -hydroxy-15-norlabda-8(17),13(14)-dien-16-oic acid ( 1 ), ( E )-15-ethoxy-15-methoxylabda-8(17),12-dien-16-al ( 2 ), ( E )-15 α -ethoxy-14 α -hydroxylabda-8(17),12-dien-16-olide ( 3 ), and 15-ethoxy-12 β -hydroxylabda-8(17),13(14)-dien-16,15-olide ( 4 ) were isolated from the methanol extract of Curcuma amada rhizomes collected in Myanmar, together with 13 known analogs. Their structures were elucidated by extensive spectroscopic techniques. All of the isolates were evaluated for their antiproliferative activities against a small panel of five different human cancer cell lines (A549, human lung cancer; HeLa, human cervical cancer; MCF7, human breast cancer; PANC-1 and PSN-1, human pancreatic cancer). Among the isolates, compounds 2 − 4 , 7 , 8 , 12 , and 17 showed mild antiproliferative activities with IC 50 values ranging from 19.7 to 96.1 μM. ( E )-14-Hydroxy-15-norlabda-8(17),12-dien-16-al ( 11 ) exhibited strong antiproliferative activities selectively against HeLa, PANC-1, and PSN-1 cells, with IC 50 values of 5.88, 1.00, and 3.98 μM, respectively. These potencies were comparable to those of the positive control, 5-fluorouracil. [ABSTRACT FROM AUTHOR]

Five new isocoumarin derivatives, pestalactone A–C ( 1–3 ) and pestapyrone D–E ( 4–5 ), together with two known compounds ( 6–7 ) were isolated from the solid cultures of the endophytic fungus Pestalotiopsis sp. obtained from Photinia frasery . Their structures were mainly determined by extensive spectroscopic analysis, Mo 2 (OCOCH 3 ) 4 -induced electronic circular dichroism (ECD), and ECD calculation. Compounds 1 and 2 were rare isocoumarin derivatives and derived from distinctive polyketide pathways. Compound 3 exhibited potent antifungal activity against Candida glabrata (ATCC 90030) with an MIC 50 value of 3.49 ± 0.21 μg/mL. [ABSTRACT FROM AUTHOR]

Two new polyketides versicolorones A-B (1 – 2), one new diketopiperazine derivative aspergiamide B methyl ester (3), along with twenty known compounds 4 – 23 , were obtained from the EtOAc extract of the Cordyceps -colonizing fungus Aspergillus versicolor ZJUTE2. The structures of 1 – 3 were established by detailed interpretation of the spectroscopic data and their absolute configurations were established by comparative analyses of the calculated and experimental ECD spectra. In the in-vitro bioassay, compounds 8 and 21 exhibited significant inhibitory activity against the Escherichia coli β -glucuronidase (EcGUS) with IC 50 values of 54.73 ± 2.69 and 56.59 ± 1.77 μM, respectively. [Display omitted] [ABSTRACT FROM AUTHOR]

Three new 2-phenylnaphthalene derivatives, cherrevenaphthalenes A–C ( 1–3 ), and a new polyoxygenated cyclohexene derivative, (−)-uvaribonol F ( 4 ) together with six known compounds, 5–10 , were isolated from the stem and root extracts of Uvaria cherrevensis (Annonaceae). The structures of all isolated compounds were elucidated by spectroscopic analysis. The structures of 3 and 4 were further confirmed by single crystal X-ray diffraction methods. Compound 2 exhibited modest antiplasmodial activity against the P. falciparum stains TM4/8.2 and K1CB1 with IC 50 values of 18.8 ± 3.63 and 23.4 ± 4.08 μM, respectively, and weak cytotoxicity to a Vero cell line. Furthermore, compound 4 displayed cytotoxic activity against a KB cell line with an IC 50 value of 22.1 ± 0.42 μM but was non-cytotoxic to the Vero cell line. Compound 5 revealed stronger cytotoxicity towards the KB cell line, with an IC 50 value of 5.05 ± 0.86 μM and was nearly equally cytotoxic to the Vero cell line. [ABSTRACT FROM AUTHOR]

Six undescribed monoterpenoids, together with twelve known compounds were isolated and identified from Hyssopus cuspidatus Boriss. Their structures were established by spectroscopic analysis, and the absolute configurations were established by ECD calculations and single-crystal X-ray diffraction crystallography. The isolated compounds were tested for their anti-inflammatory, antibacterial and antitumor activities. Most of the compounds showed potent anti-inflammatory activities. Among them, 3 β -hydroxy-7,8-dihydro- β -ionone (8), oleanolic acid (17) and acetylpleamolic acid (18) showed strong anti-inflammatory activity against IL-6 and TNF- α in lipopolysaccharide (LPS) stimulated RAW 264.7 cells. Several compounds showed moderate inhibitory activities against Staphylococcus aureus , Candida albicans , and Escherichia coli. And (4 S)- p -menth-l-ene-7,8-diol 8- O - β -D-glucopyranoside (16) showed antitumor activities against MCF-8 and HT-29 cell lines with IC 50 values of 93.39 ± 3.69 and 71.89 ± 2.94 μ M, respectively. Oleanolic acid (17) showed moderate antitumor activity against HT-29 cell lines with an IC 50 value of 52.62 ± 1.63 μ M. In this study, the discovery of anti-inflammatory, antibacterial and antitumor components from H. cuspidatus could benefit further development and utilization of this plant. [Display omitted] • Eighteen terpenoids including six new ones were isolated from Hyssopus cuspidatus. • Most of the compounds showed potent anti-inflammatory activities. • Compound 8 showed strong anti-inflammatory activity against IL-6 and TNF-α. • Several compounds showed good activities against MCF-8, HT-29 and HT-29 cell lines. • Several compounds showed moderate antimicrobial activities. [ABSTRACT FROM AUTHOR]

Four new 2-(2-phenethyl)chromone dimers (1–4) were isolated from EtOAc extract of agarwood originating from Aquilaria filaria from Philippines. Their structures were elucidated by spectroscopic analysis (1D and 2D NMR, and HRESIMS) and comparison of the experimental and computed ECD curves. Compounds 1–4 exhibited inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW264.7 cells with IC 50 values in the range from 33.94 to 57.53 μM. [Display omitted] • Four new 2-(2-phenethyl)chromone dimers were isolated from agarwood of Aquilaria filaria from Philippines. • Compound 4 , whose unites A and B were linked via C5-O-C7″-ether bond, was a relative unusual 2-(2-phenethyl)chromone dimer. • Compounds 1–4 exhibited inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW264.7 cells. [ABSTRACT FROM AUTHOR]

Three new isoquinoline alkaloids including a morphine derivative (1), two aporphine alkaloids (2 – 3), together with five known alkaloids (4 – 8) were obtained from the extract of Dactylicapnos scandens (D.Don) Hutch. (D. scandens). Their structures and absolute configurations were elucidated by extensive spectroscopic data analysis including HRESIMS, NMR and electronic circular dichroism (ECD) and ECD calculation. Compounds 1 – 8 were evaluated for ATP Citrate Lyase (ACLY) inhibitory activity through an enzymatic assay. Among them, 2 and 3 showed the high ACLY inhibitory activity with an IC 50 value of 10.48 ± 1.59 and 10.89 ± 4.89 μM. [Display omitted] • Three new alkaloids were obtained from Dactylicapnos scandens. • Their structures were evaluated by the analysis of extensive spectroscopic data. • Compound 2 and 3 exhibited significant ACLY inhibitory activity. [ABSTRACT FROM AUTHOR]

Croton kongensis Gagnepain. belongs to the genus Croton , the Euphorbiaceae family, mainly distributed in Hainan and southern Yunnan, China. The aim of present study was to acquire secondary metabolites of the ethanol extract obtained from the leaves and twigs of C. kongensis. Three new abietane-type diterpenoids, crokongenolides A-C (1 – 3), together with seven known diterpenoids (4 – 10), were isolated from the leaves and twigs of C. kongensis. The structures of the new compounds were determined by extensive spectroscopic methods (1D and 2D NMR, IR, and HRESIMS), and their absolute configurations were confirmed by single-crystal X-ray diffraction analysis or electronic circular dichroism (ECD) calculations. The absolute configuration of 4 was determined for the first time by single-crystal X-ray diffraction analysis with Cu-Kα irradiation. Some compounds were evaluated for their antimicrobial properties by assessing their inhibitory effects on Staphylococcus aureus , Candida albicans , and Escherichia coli. Compound 10 showed significant antimicrobial activity against S. aureus with MIC value of 1.56 μg/ml. [Display omitted] • Three new abietane-type diterpenoids were isolated from the leaves and twigs of Croton kongensis. • The structures of three new compounds were elucidated by extensive analysis of spectroscopic data. • Some compounds showed significant antimicrobial activity against Staphylococcus aureus. [ABSTRACT FROM AUTHOR]

One new 1,4-bis-phenyl-1,4-butanedione glycoside (14), one new eudesmane-type sesquiterpenoid (16), and 16 known compounds were isolated from the leaves and stems of Nelumbo nucifera Gaertn. The structures of the isolated compounds were elucidated by interpretation of their 1D and 2D NMR spectroscopic and HRESIMS data. Time-dependent density functional theory calculations and Electronic Circular Dichroism (ECD) spectroscopy was used to determine absolute configurations of the new eudesmane-type sesquiterpenoid (16). All the isolated compounds were examined for their antiosteoclastogenic activity. Preliminarily results of the TRAP staining on RAW 264.7 cells indicated that compounds 1 and 11 possess potential inhibitory effects on RANKL-induced osteoclast formation. Further bioassay investigation was carried out to reveal that compounds 1 and 11 suppressed RANKL-induced osteoclast formation in a concentration-dependent manner with the inhibition up to 55% and 78% at the concentration of 10 μM, respectively. In addition, the structure-activity relationship analysis showed that the 1,3-dioxole substitute and the double bond at C-6a/C-7 in the aporphine skeleton may be responsible for the antiosteoclastogenic activity. The findings provided valuable insights for the discovery and structural modification of aporphine alkaloids as the antiosteoclastogenic lead compounds. [Display omitted] • A phytochemical investigation of Nelumbo nucifera leaves and stems was conducted. • One new 1,4-bis-phenyl-1,4-butanedione glycoside and one new eudesmane-type sesquiterpenoid were identified. • The absolute configurations were determined by experimental ECD and ECD calculations. • Two compounds showed a strong, dose-dependent antiosteoclastogenic activity. [ABSTRACT FROM AUTHOR]

The main objective of our present research work was to explore molecular insight for potentially active new acetylcholinesterase inhibitor from the aerial parts of Delphinium uncinatum. New norditerpenoid alkaloids, uncinatine-A, was isolated from the basic alkaloidal fraction of D. uncinatum, based on bioactivity guided isolation. The structure of uncinatine-A was determined through latest spectroscopic techniques including single X-Ray diffraction technique. The structural data and electronic properties of uncinatine-A was also calculated by Density Functional Theory (DFT) using B3LYP/6-31þ G (p) basis set. The isolated natural product was evaluated for their acetyl cholinesterase inhibitory potential in dose dependent protocol (62.5–1000 μg/mL), followed by molecular docking studies. Significant competitive type inhibition activity (IC 50 = 207.73 ± 0.3) was shown by isolated natural norditerpenoid against cholinesterase targets in comparison with standard drugs available in the market such as galanthamine. The molecular docking results showed that isolated natural product was well accommodated by AChE in the active site with docking scores −11.0326. This is the first report indicating uncinatine-A as a potent acetylcholinesterase inhibitor and can be used as a target drug in cerebral dementia and Alzheimer diseases. [Display omitted] • Uncinatine-A, a new acetylcholinesterase inhibitor has been isolated from D. uncinatum. • Structures of the isolated compound was deduced on the basis of spectroscopic and single X-ray ray technique. • The compound uncinatine-A was evaluated for their acetylcholinesterase inhibitory potential both in vitro and ins ilico. • The isolated compound showed promising acetylcholinesterase inhibition activity. • DFT analysis of uncinatine-A was also conducted. [ABSTRACT FROM AUTHOR]

Five new compounds ( 1 – 5 ), including three limonoids, one diterpenoid, and one phytosterol, along with four known limonoids ( 6 – 9 ), were isolated from the ethanolic extracts of whole plants of Munronia henryi . Their structures were elucidated by extensive spectroscopic analysis. In addition, the anti-tobacco mosaic virus (TMV) activities of all the isolated compounds were evaluated by the conventional half-leaf and leaf-disk methods along with Western blot analysis. Most of the tested compounds showed strong antiviral activities, with IC 50 values in the range of 14.8–34.0 μg/mL, compared with ningnanmycin as a positive control (IC 50 = 44.6 μg/mL), and their preliminary structure-activity relationships were also discussed. [ABSTRACT FROM AUTHOR]

Five new hexacyclic monoterpenoid indole alkaloids, rauvovertine A ( 1 ), 17- epi -rauvovertine A ( 2 ), rauvovertine B ( 3 ), 17- epi -rauvovertine B ( 4 ), and rauvovertine C ( 5 ) together with 17 known analogues were isolated from the stems of Rauvolfia verticillata . Compounds 1 / 2 and 3 / 4 were obtained as C-17 epimeric mixtures due to rapid hemiacetal tautomerism in solution. The structures of 1 – 5 were established by spectroscopic analysis and with the aid of molecular modeling. The new alkaloids were evaluated for their cytotoxicity in vitro against human tumor HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cell lines. [ABSTRACT FROM AUTHOR]

A chemical investigation of callus cultures of Dysosma versipellis led to the isolation of five new flavonol dimers, dysoverines A − E ( 1 − 5 ), together with 12 known compounds ( 6 − 17 ). The structures of new compounds were determined by the extensive spectroscopic data analyses. The biosynthetic pathway of the new compounds was proposed to involve O -methylation, prenylation, and Diels–Alder cycloaddition, which successively occurred in cultured plant cells. Compounds 1 − 17 exhibited in vitro neuraminidase inhibitory activities with the IC 50 values of 31.0 − 93.9 μM. [ABSTRACT FROM AUTHOR]

One new 9,10- seco -abietane derivative, crotontomentosin A ( 1 ), four new abietane-type diterpenoids, crotontomentosins B–E ( 2 – 5 ), one new ent -halimane-type diterpenoid, crotontomentosin F ( 6 ), along with five known diterpenoids ( 7 – 11 ) and one known sesquiterpenoid ( 12 ) were obtained from the twigs and leaves of Croton caudatus Geisel. var. tomentosus Hook. The structures of the compounds were established on the basis of extensive spectroscopic data. Compounds 1 – 4 and 11 exhibited moderate to weak inhibitory activity against the proliferation of the Hela, Hep G2, MDA-MB-231, or A549 cell lines selectively. [ABSTRACT FROM AUTHOR]

Three new cyanogenetic triglycosides linustatins A–C ( 1 – 3 ), and two new simple glycosides linustatins D and E ( 4 and 5 ) were isolated from the 70% ethanol extract of flaxseed meal ( Linum usitatissimum L.). Their structures were elucidated on the basis of spectroscopic analysis and chemical evidence. All of the isolates showed moderate activities against aldose reductase and weak activities against α -glucosidase, DPP-IV, and FBPase at the same concentrations as the positive control drugs. [ABSTRACT FROM AUTHOR]

Nine new sesquiterpenes ( 1 – 9 ), together with seventeen known ones ( 10 – 26 ), were isolated from Chinese eaglewood. Their structures were established by extensive spectroscopic analysis, and the absolute configuration of 6 was determined by the modified Mosher's method. Compounds 7 , 10 , 14 , 15 , and 21 exhibited significant inhibition of nitric oxide production in lipopolysaccharide-stimulated BV-2 microglial cells with IC 50 values in the range 7.1–53.8 μM. [ABSTRACT FROM AUTHOR]

A pair of new diastereoisomers neolignans (1–2) and a new alkaloid (7) were isolated from the stems of Nauclea officinalis : naucleaoxyneolignoside A (1) , naucleaoxyneolignoside B (2) , (2 S ,3 S)-javaniside (7) , together with nine known compounds, 2 S -3,3-di-(4-hydroxy-3-methoxyphenyl)-propane-1,2-diol (3) , threo -1,2-bis-(4-hydroxy-3-methoxyphenyl)-propane-1,3-diol (4) , nauclefine (5) , angustidine (6) , naucleoxoside A (8) , naucleoxoside B (9), angustoline (10), (3 S ,19 S)-3,14-dihydroangustoline (11) , and (3 S ,19 R)-3,14-dihydroangustoline (12).The structures of 1 , 2 and 7 were elucidated by extensive spectroscopic methods and the known compounds were identified by comparison of their data with those reported in the literature. The absolution configurations of 1 , 2 , 7 , 11 and 12 were confirmed by the quantum chemical CD calculation method. Compounds 1 – 9 showed weak to moderate inhibitory activity on nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro with IC 50 values comparable to that of dexamethasone. In addition, compounds 1 – 9 were evaluated for the antibacterial and cytotoxic effects, and the results revealed that these compounds showed no anti-bacterial activity, and compounds 3 – 6 showed modest cytotoxic activity. [Display omitted] [ABSTRACT FROM AUTHOR]

Four new phenolic acids, clerodens A–D ( 1 – 4 ) possessing an unusual bicycle [2.2.2] octane moiety were isolated from the whole plants of Clerodendranthus spicatus . Their structures were elucidated by extensive spectroscopic methods, including NMR, MS, and ECD data. All isolates were evaluated for their anti-inflammatory activities on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7, and compound 4 showed significant inhibitory activities with IC 50 value of 6.8 μM. [ABSTRACT FROM AUTHOR]

Chromatographic separation of an aqueous acetone extract of the galls from Tamarix aphylla using gels resulted in isolation of an ellagitannin, phyllagallin M1 ( 13 ), a gallo-ellagitannin, phyllagallin D1 ( 14 ), and four gallotannins, phyllagallin M2 ( 15 ) and phyllagallins D2–D4 ( 16 – 18 ), in addition to four known ellagitannins and three phenolics of lower molecular weight structurally related to hydrolyzable tannins. The structures of the six new tannins were elucidated based on spectroscopic and chemical data. Among the phenolics, flavogallonic acid dilactone ( 8 ), which is presumed to be biogenetically produced by C–C oxidative coupling of an ellagic acid unit with a galloyl residue, shows an exceptional oxidative pattern of gallic acid residues in plants of the family Tamaricaceae. Although the ellagitannin tamarixellagic acid ( 4 ) was reported to be a constituent of the galls of T. aphylla , such compounds with anomalous location of the DHDG moiety at O-3 on the glucopyranose core have not been observed among the tannins of tamaricaceous plants. [ABSTRACT FROM AUTHOR]

One new 19-norbufadienolide ( 1 ) and one new bufogargarizin ( 2 ), together with twelve known bufadienolides ( 3–14 , resp.) were isolated from Chan Su, a traditional Chinese medicine that is used in the treatment of cancer. Their structures were elucidated on the basis of detailed spectroscopic analysis and comparison of corresponding data that is previously reported. The cytotoxic activities of the isolated compounds were evaluated on HeLa and A549 cell lines. Though 1 and 2 showed weak cytotoxic activities on both cell lines, compounds 4 and 5 showed lower IC 50 values than bufalin, the most widely studied bufadienolide in Chan Su. Furthermore, four 3-ester derivatives ( 15–18 ) of compound 4 were synthesized and their cytotoxic activities were also evaluated. Analysis of the structure–activity relationship indicated that bufadienolides with aldehyde group at C-10 or α -hydroxyl group at C-11 exhibit stronger cytotoxic activities on both cell lines. The cytotoxic activity of arenobufagin-3-ester derivative 17 was 4-fold higher than compound 4 . [ABSTRACT FROM AUTHOR]

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 IC 50 values in the range of 2.61–20.35 μ g/mL. [ABSTRACT FROM AUTHOR]

Inhibitors of protein tyrosine phosphatase 1B (PTP1B) are promising agents for the treatment of type 2 diabetes and obesity. The bioactivity-guided isolation led to the separation of two new compounds, (±)-tradescantin ( 13 ) and tradescantoside ( 16 ), along with fourteen known compounds ( 1 – 12 , 14 , and 15 ) from the aerial parts of Tradescantia spathacea Sw. (Commelinaceae). Their chemical structures were elucidated by spectroscopic methods as well as by comparing with those reported in the literature. The isolated compounds ( 1 – 16 ) were then examined for their inhibitory activity toward PTP1B. The results indicated that compounds 2 , 6 , 8 , and 12 possessed potent inhibition with IC 50 values of 7.82 ± 0.79, 6.80 ± 0.89, 4.55 ± 0.92, and 6.38 ± 0.14 μM, respectively. Kinetic study of compounds 2 , 6 , 8 , 12 , 13 , and 16 was conducted and the structure–activity relationships of the isolated compounds ( 1 – 16 ) were also discussed herein. To the best of our knowledge, all the isolates were separated for the first time from this plant. [ABSTRACT FROM AUTHOR]

Ten flavonoid glycosides, apetalumosides A ( 1 ), B 1 –B 7 ( 2 – 8 ), and C ( 9 ), quercetin 3- O -(2,6-di- O - β - d -glucopyranosyl)- β - d -glucopyranoside ( 10 ), were obtained from the seeds of Lepidium apetalum Willd. Their structures were elucidated by chemical and spectroscopic methods (UV, IR, NMR, and HRESI-TOF-MS). 1 – 9 were new isolates. The NMR data for 10 was reported here for the first time. On the other hand, activity screening results showed that 1 – 3 and 10 had triglyceride accumulation inhibitory effects in HepG2 cells. Preliminary structure–activity relationship study revealed that 7-hydroxyl group is an essential moiety. [ABSTRACT FROM AUTHOR]

Five new benzylphenanthrenes, cremaphenanthrenes L–P ( 1 – 5 ) were isolated from the EtOAc-soluble extract of the tubers of Cremastra appendiculata . Their structures were elucidated based on the spectroscopic data and chemical methods. Compounds 1 – 5 were tested in vitro for their cytotoxic effects against colon (HCT-116), cervix (Hela), and breast (MCF-7 and MDA-MB-231) cancer cell lines. Compound 1 showed moderate cytotoxic activities against HCT-116, MCF-7, and MDA-MB-231 cancer cell lines with IC 50 values ranging from 15.84 to 24.18 μM and weak cytotoxicity to Hela cell line with IC 50 value of 68.81 μM. [ABSTRACT FROM AUTHOR]

Four new neolignans ( 1 – 4 ), together with two known lignans ( 5 and 6 ), were isolated from the root of Paeonia lactiflora . Compounds 1 and 2 were two racemates and were separated by chiral high performance liquid chromatography (HPLC) to give all of the four stereoisomeric forms sharing a common planar structure. Compounds 3 and 4 were two neolignan glycoside diastereomers but interestingly appeared to be enantiomers: they had the extremely similar 1 H and 13 C NMR spectra and had to be solved only by chiral HPLC. Their structures were determined by spectroscopic analysis, including 1D and 2D NMR, HRESIMS and electronic circular dichroism experiments. All compounds were evaluated for their inhibitory effects on β-amyloid aggregation, and the optical pure compound 2b was found to show the optimal Aβ 1–42 aggregation inhibition potency (81.1% at 20 μM). In addition, despite large amount of chemical studies performed on genus Paeonia , the lignans were reported for the first time. [ABSTRACT FROM AUTHOR]