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In alternative medicine, plants pay a major role. Some plants are known for their poisonous nature but still have some importance in the herbal drug industry for their medicinal value. Strychnos nux-vomica is one such plant. Its nuts are called as poison nut due to the presence of alkaloids. Both the nut and its minerals are having medicinal properties and hence the present study was indented to understand the nature of primary metabolites and multi elemental composition. The nuts of S. nux-vomica were procured, authenticated, powdered and subjected to proximate analysis parameters, visualization of thin layer chromatographic separation (TLC) and finger print profiling through high performance thin layer chromatographic (HPTLC); surface morphology by scanning electron microscopy, energy dispersive X-ray analysis, X-ray fluorescence spectrometry, X-ray photoelectron spectrometry, powder X-ray diffractometry and inductively coupled plasma optical emission spectrometry. In HPTLC, 7 spots each under 254 nm, 366 nm, derivatization with vanillin sulphuric acid (VSR) reagent appeared and 2 spots with Dragendorff's reagent. In HPTLC, 12 peaks at 254 nm, 9 peaks at 366 nm, 7 peaks at 520 nm after derivatization with VSR reagent detected. Elements such as potassium, calcium, magnesium, chlorine, aluminium, iron, manganese, sodium, nickel, phosphorus, copper, zinc, sulphur and silicon were identified. PXRD revealed that the presence of potassium chloride, calcite and dolomite as major elemental composition. The presence of all the above elements has vital roles on human physiology. Potassium, calcium, chlorine, aluminium, nickel, phosphorus, sulphur and silicon are reported for the first time in this study. [ABSTRACT FROM AUTHOR]

One new aspidosperma-type alkaloid, melotenine A (1), together with five known ones (2-6), was isolated from the leaves of Melodinus axillaris. Their structures were elucidated by detailed spectroscopic analysis and quantum chemical ECD calculation. The isolated aspidosperma-type alkaloids were evaluated for their cytotoxicity against four human cancer cell lines and melotenine A showed significant cytotoxicity against all cells with IC50 values ranging from 0.6 to 1.5 μM. [ABSTRACT FROM AUTHOR]

A new prenylated xanthone, garcixanthone A (5), together with eight known compounds, mangostanaxanthones I (1) and II (2), garcinone E (3), β-mangostin (4), 8-hydroxycudraxanthone G (6), garcinone C (7), cudraxanthone G (8), and (-)-epicatechin (9) were isolated from the EtOAc-soluble fraction of the air-dried pericarps of Garcinia mangostana (family Clusiaceae). Their structures were verified on the basis of spectroscopic data interpretation as well as comparison with the literature. The cytotoxic and antimicrobial activities of the new compound were assessed using sulforhodamine B (SRB) and agar disk diffusion assays, respectively. Compound 5 showed significant cytotoxic potential against epithelial lung carcinoma (A549) and breast carcinoma (MCF7) cell lines with IC50s 3.0 and 4.2 μM, respectively, compared to doxorubicin (0.74 and 0.41 μM, respectively). [ABSTRACT FROM AUTHOR]

Abstract Two new nucleoside derivatives, named asponguanosines A and B (1 and 2), three new N -acetyldopamine analogues, aspongamides C–E (3 – 5), one new sesquiterpene, aspongnoid D (6) , and three known compounds were isolated from the medicinal insect Aspongopus chinensis. Their structures including absolute configurations were assigned by using spectroscopic methods and ECD and 13C NMR calculations. Biological activities of compounds 3 – 7 towards human cancer cells, COX-2, ROCK1, and JAK3 were evaluated. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Ethnopharmacological relevance Acanthus mollis is a plant native to the Mediterranean region, traditionally used as diuretic, anti-inflammatory and soothing of the mucous membranes of the digestive and urinary tract and externally as healing of wounds and burns, also demonstrating analgesic and anti-inflammatory activities. However, studies focused on its phytochemical composition as well as scientific proof of Acanthus mollis efficacy are scarce. Aim of the study The proposed work aims to perform a phytochemical characterization and evaluation of the therapeutic potential of Acanthus mollis , based on biological properties that support its traditional uses. Material and methods In this study, an 96% ethanol extract from Acanthus mollis leaves was obtained and its phytochemical composition evaluated using High Performance Liquid Chromatography with Photodiode Array Detector coupled to Electrospray Ionization Mass Spectrometry (HPLC-PDA-ESI/MSn). The chemical structure of the compound isolated was elucidated using 1H and 13C Nuclear Magnetic Resonance (NMR), 1H-correlation spectroscopy (1H–COSY), heteronuclear single quantum correlation (HSQC) and heteronuclear multiple-bond correlation (HMBC). The quantification of the constituents was performed using two external standards (2,4-dihydroxy-1,4-benzoxazin-3-one and verbascoside). The antioxidant activity was determined by the 2,2-diphenyl-1-pycrylhydrazyl (DPPH) assay. Anti-inflammatory activity was determined measuring the inhibition of nitric oxide production by RAW 264.7 macrophages stimulated with the TLR4 agonist lipopolysaccharide (LPS) and through lipoxygenase (LOX) inhibition assay. The cytotoxicity was screened on two lines (RAW 264.7 and HaCaT) using the resazurin assay. Results Compounds such as verbascoside and its derivatives, as well as benzoxazinoids were found as the main constituents. A percentage of 5.58% was verified for the 2,4-dihydroxy-1,4-benzoxazin-3-one (DIBOA) derivatives. DIBOA was the main compound of the extract. Significant concentrations were also found for phenylpropanoids, which constitute about 4.39% of the total compounds identified. This extract showed antioxidant capacity against DPPH (IC 50 = 40.00 ± 1.59 μg/mL) and superoxide anion (IC 50 = 29.42 ± 1.99 μg/mL). It also evidenced anti-inflammatory potential in RAW 264.7 macrophages, presenting capacity for nitric oxide reduction (IC 50 = 28.01 μg/mL). Moreover, in vitro studies have shown that this extract was able to inhibit the lipoxygenase, with an IC 50 of 104.39 ± 4.95 µg/mL. Importantly, all effective concentrations were devoid of cytotoxicity in keratinocytes, thus highlighting the safety of the extract for the treatment of skin inflammatory related diseases. Concerning macrophages it was also possible to disclose concentrations showing anti-inflammatory activity and without cytotoxicity (up to 30 µg/mL). The benzoxazinoid DIBOA demonstrated a considerable anti-inflammatory activity suggesting its important contribution to this activity. Conclusions These results corroborate the anti-inflammatory properties traditionally attributed to this plant. Among the compounds identified in this study, benzoxazinoids exhibited a significant anti-inflammatory activity that was never previously described. Ethanol seems to be a good option for the extraction of these bioactive compounds, since relevant antioxidant/anti-radical and anti-inflammatory activities were found for this extract. Graphical abstract fx1 [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 The phytochemical investigation of the fruit extracts of Uvaria cherrevensis led to the isolation and characterization of four new C-benzyl flavonoids; cherrevenones A-D (1 – 4) together with 11 known compounds. The isolated compounds were characterized using spectroscopic techniques. Compounds 1 , 3 , 5 and 11 showed moderate inhibitory activities against the P. falciparum strains TM4/8.2 and K1CB1 with IC 50 values ranging from 21.0 ± 3.10 – 33.7 ± 7.69 and 21.0 ± 5.44 – 43.5 ± 11.9 μM, respectively. Compounds 1 , 2 , 5 , 10 and 11 exhibited strong cytotoxic activities against KB cells with IC 50 values ranging from 0.60 ± 0.17 – 4.91 ± 2.69 μM which were similar to their cytotoxic activities found against Vero cells, except for compound 5 , which was non-toxic to Vero cells. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Four new naphthylisoquinoline alkaloids, the 5,8′-coupled ancistroyafungines A-C (1 - 3) and the 5,1′-linked ancistroyafungine D (4), have been isolated from the stem bark of an as yet unidentified Ancistrocladus (Ancistrocladaceae) liana recently discovered near the village Yafunga, in the North-Central region of the Democratic Republic of the Congo. Likewise obtained were eleven analogs previously identified in related African and Asian Ancistrocladus species, exhibiting five different coupling types, viz., 5,8′, 5,1′, 7,1′, N ,6′, and N ,8′. All of the alkaloids are S -configured at C-3 and possess an oxygen function at C-6 in the isoquinoline portion, and, thus, belong to the subclass of "Ancistrocladaceae-type" alkaloids. This finding is geo- and chemotaxonomically remarkable, since – apart from one other Ancistrocladus species from the Central Congo Basin – only Southeast Asian and East African Ancistrocladaceae are known to exclusively produce naphthylisoquinolines with these structural features. Moreover, the alkaloid pattern of this Congolese liana clearly demarcates this plant from all other Ancistrocladus taxa that have so far been botanically described, which suggests that it might represent a new species or subspecies. The new ancistroyafungines display strong preferential cytotoxic activities towards human PANC-1 pancreatic cancer cells in nutrient-deprived medium, without showing toxicity in normal, nutrient-rich conditions. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Matrix metalloproteinase 9 (MMP-9) is one of the structurally related zinc-dependent endopeptidases families and provides a new target for cancer therapy owing to its pivotal role in metastatic tumors. In this paper, fourteen lignans, including three novel lignans, named selamoellenin B–D (1 – 3), and eleven known lignan derivatives (4 – 14) were isolated from the plant of Selaginella moellendorffii. Among them, compound 3 is optically active, which was enantiomerically seperated to afford a pair of enantiomers, (−)- 3 and (+)- 3. Their structures were elucidated by extensive spectroscopic analyses. Their cytotoxic activities were evaluated against four human cancer cell lines. Among them, five compounds (4 , 5 , 6 , 11 and 13) exhibited great potent cytotoxicity and their structure-activity relationships were also discussed. All compounds except for 3 lignan analogues with low cytotoxicity were selected for further in vitro enzyme inhibition, surface plasmon resonance (SPR), and molecular docking assays based on the MMPs target. The results shown that, compound 11 have the best inhibitory effect and can be considered as a potential drug candidate targeting at MMP-9 for cancer therapy. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract We report here for the first time antinociceptive effects of extracts from Baccharis flabellata. Two extracts in this analysis, one obtained in summer and the other during winter time. Our results indicate that both extract show strong antinociceptive effects, being the extracts obtained during the summer significantly more active. Our results suggest that this activity is mainly due to the presence of the diene-acid clerodane ent-15,16-epoxy-19-hydroxy-1,3,13(16),14-clerodatetraen-18-oic acid (DAC) and its dimer called DACD. Employing naloxone as an antagonist of opioid receptors, we demonstrated that both compounds act on opioid receptors, being the antinociceptive effect of DACD stronger than DAC. Thus, the antinociceptive activity of DACD was almost two times stronger than DAC (44.8 over 24.6 s in the hot-plate test) after one hour of treatments. In order to better understand the mechanism of action at molecular level of these compounds, we conducted a molecular modeling study analyzing the molecular interactions of DAC and DACD complexes with the κ-ORs. Our results suggest interactions for both DAC and DACD with Gln115, Val118, Tyr119, Asn122 and Tyr313 stabilizing their complexes; however, these interactions are significantly stronger for DACD with respect to DAC. This finding could explain why DACD have a higher affinity for the κ-ORs. These results are in agreement with the obtained antinociceptive effect. In addition, our results indicate that these neoclerodanes would have a mechanism of action similar to that of salvinorin A; such information can be very useful for the design of new inhibitors of κ-ORs. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract In previous work, a series of bioactive natural products had been isolated from the plant endophytic Streptomyces sp. CS, which was isolated from Maytenus hookeri. To mine new active metabolites, we describe introducing an alien carbamoyltransferase (asm21) gene into the strain CS by conjugal transfer. As a result, three recombinatorial mutants named CS/ asm21 -1, CS/ asm21 -2 and CS/ asm21 -4 were successfully constructed. Three mutants and wild type CS were cultured on solid medium, and the extracts were detected and analyzed by liquid chromatography-mass spectrometry (LC-MS). The LC-MS profiles showed several unknown peaks that were present in the spectra of extracts of the CS/ asm21 -4 cultured on oatmeal solid medium. Then, three new naphthomycins O-Q (1 – 3), a new macrolide hookerolide (4) as well as nine known compounds were obtained from the solid cultured medium. Their structures were identified by spectra data. These new compounds showed moderate antimicrobial activities. Graphical abstract Unlabelled Image Highlights • Streptomyces sp. CS was isolated from Chinese medicinal plant Maytenus hookeri. • Mutants of S. sp. CS were constructed for mining secondary metabolites. • Four new compounds (1 – 4) were isolated from the fermentation extracts. • These new compounds showed moderate antimicrobial activities. [ABSTRACT FROM AUTHOR]

Abstract The aim of this study was to contribute to the characterization of Crocus taxa using morphological, phytochemical and genetic analysis. The styles of C. cartwrightianus , C. oreocreticus and C. laevigatus, collected in the island of Crete were compared to those of C. sativus cultivated at the region of Western Macedonia (Greece). Phytochemical analysis was done using GC–MS and HPLC methods, while ISSR markers were used for their genetic characterization. Safranal was the major volatile component of the styles of C. sativus , 4-hydroxy-2,6,6-trimethyl-1-cyclohexene-1-carboxaldehyde of C. cartwrightianus and C. oreocreticus , and isophorone of C. laevigatus. C. sativus had the highest content of crocins and picrocrocin, while C. laevigatus the lowest (only 5% of C. sativus' quantity) and negligible amount of picrocrocin. According to both the genetic and the chemical analysis, C. cartwrightianus is more related to C. oreocreticus, while C. sativus and C. laevigatus are more distinct. Concordance between the two different types of data was also confirmed by the Mantel test (r = 0.932, P =.68). This is the first thorough screening of secondary metabolites (volatile and non-volatile) and also genetic and morphological characters of wild Crocus styles simultaneously, that contributes to the identification and valorisation of genotypes with similar to C. sativus traits which may be introduced as new cultivars through breeding. Graphical abstract Unlabelled Image Highlights • Comparison of C. cartwrightianus , C. oreocreticus, C. laevigatus from Crete to C. sativus. • C. sativus has the highest style volatile (GC–MS) and crocin/picrocrocin (HPLC) content. • Concordance of genetic (ISSR markers) and phytochemical analysis • C. cartwrightianus is more related to C. oreocreticus • C. laevigatus styles are morphologically, chemically and genetically distinct. [ABSTRACT FROM AUTHOR]

Abstract Two new terpenoids, named biperovskatone B (1) and 1α- hydroxyl demethylsalvicanol quinine (2), were isolated from the cultured Perovskia atriplicifolia. Their structures were elucidated by comprehensive analyses of the MS, IR, 1D and 2D NMR spectra. Compound 1 was a novel diterpenoid dimer, containing two different rearranged 9(10 → 20)-abeoabietane type diterpenoid fragments. Compound 2 was a new icetexane diterpenoid with characteristic ortho -quinone carbonyl groups. Both compounds were assayed for their anti-HBV activity in vitro. Results suggested compounds 1 and 2 showed noticeable anti- anti-HBV activity, inhibiting the replication of HBV DNA with IC 50 values of 10.78 and 8.61 μM, respectively. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Five new metabolites belonging to two backbones of pulvilloric acid-type azaphilone and tremulane sesquiterpene were obtained and their structures were determined by spectral analysis. Based on the biogenesis analysis, tremulane sesquiterpenes were obtained from Irpex lacteus by the stimulation of mixed-culture. The antifungal selectivities of metabolites produced by fungus against their co-culture fungus and common pathogens , exhibited competitive interaction of this mix-culture. The tremulane sesquiterpene conocenol B produced by I. lacteus through the induction of Nigrospora oryzae showed selectivity of anti-fungal activity against its co-culture fungus, N. oryzae , with MICs at 16 μg/mL and 128 μg/mL against I. lacteus. The fungus can metabolize these new compounds to inhibit the growth of co-culture fungus while not inhibiting its own growth. Compound 5 was active against acetylcholinesterase (AChE) with a ratio of 35% at the concentration of 50 μM. Graphic abstract The antifungal selectivities of new metabolites against its co-culture fungus, produced by different fungus, exhibited the competitive interactions. 5 indicated anti-AChE activity. Unlabelled Image Highlights • The antifungal selectivities of new microbial metabolites against its co-culture fungus showed the competitive interactions. • 5 indicated anti-AChE activity. [ABSTRACT FROM AUTHOR]

Abstract Five new guaiane-type sesquiterpenoid dimers vielopsides A-E, connecting patterns through two direct C C bonds (C-2 to C-2′, C-4 to C-1′), were isolated from the roots of Xylopia vielana. Their absolute configurations were established by NOE analysis, the Cu Kα X-ray crystallographic and circular dichroism (CD) experiment. Among them, compound 5 showed moderate activity IC 50 values of 33.8 μM on NO production in RAW 264.7 macrophages. Graphical abstract Vielopsides A-E, five new guaiane-type sesquiterpenoid dimers, connecting mode (C-2 to C-2′, C-4 to C-1′), were isolated from the roots of Xylopia vielana. Among them, compound 5 showed moderate activity IC 50 values of 33.8 μ M on NO production in RAW 264.7 macrophages. 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]

Carpesium humile Winkl is an endemic Chinese species and no previous phytochemical studies have been reported for this species. Two new germacranolides ( 1 and 2 ) and a new phytane diterpene ( 5 ), together with five known compounds (two sesquiterpenoids and three diterpenoids), were isolated from the aerial parts of C. humile . Their structures were elucidated on the basis of extensive spectroscopic analysis. The conformations and absolute configurations of 1 and 2 were established by combinative analysis of NMR, CD exciton chirality, and X-ray crystallography data. Four germacranolides ( 1 – 4 ) showed strong cytotoxic activities, with broad spectrum activities against six human cancer (HepG2, HeLa, HL60, SGC7901, Lewis, and MDA231) cell lines in vitro using MTT assay, with IC 50 values from 3.09 to 7.71  μ g/mL. Diterpenes ( 5 , 6 , and 8 ) also displayed good cytotoxic activities for selected cancer cell lines, with IC 50 values in the range 5.46–8.08  μ g/mL. [ABSTRACT FROM AUTHOR]

Four new nerolidol-type sesquiterpene glucosides, triptergosidols A-D ( 1 - 4 ) were isolated from the leaves of Tripterygium wilfordii . Three aglycones, named triptergerols A ( 1 a), B ( 2 a), and C ( 3 a), were acquired by enzymatic hydrolysis of 1 - 3 . The structures of nerolidol-type sesquiterpenes were elucidated on base of kinds of spectroscopic analysis, and their absolute configurations were determined by CD method. In addition, compounds 1 - 4 were tested for cytotoxicity against two cell lines and inhibitory effects against NO production in RAW264.7 macrophage. [ABSTRACT FROM AUTHOR]

The mushroom Stereum hirsutum is parasitized by Tremella aurantia to form a heterogeneous basidiocarp Jin'er, which has been used as food and folk medicine in Chinese society. In present work, the S. hirsutum was fermented in YMG broth, and four novel mixed terpenes, stereumamides A-D ( 1 – 4 ), which are sesquiterpenes combined with α-amino acids to form quaternary ammonium hybrids, were isolated from the Stereum hirsutum FP-91666 and their structures were elucidated by spectroscopic data analysis. Stereumamides A and D showed antibacterial activity against Escherichia coli , Staphylococcus aureus , and Salmonella typhimurium , with the minimum inhibitory concentration (MIC) values of 12.5–25.0 μg/mL. The stereumamides A-D should be apparently the first example of naturally occurring a quaternary ammonium compound (QAC) conjugated by sesquiterpene with an α-amino acid. QAC is a common antibacterial agent in food industry, which is found in the mycelium of Stereum hirsutum would suggest that the complex basidiocarp is a functional food and veritable folk medicine. [ABSTRACT FROM AUTHOR]

Three new cleistanthane diterpenoids, phyllanglins A–C ( 1 – 3 ), a new natural product, 4-acetyl-bergenin ( 4 ), and three known compounds ( 5 – 7 ) were isolated from the roots of Phyllanthus glaucus . Their structures were elucidated by extensive spectroscopic data analyses and single-crystal X-ray diffraction. Phyllanglins A–C were unusual cleistanthane diterpenoids with phenylacetylene moieties, and a plausible biogenetic pathway was proposed to discuss the origins of them. All of the isolates were evaluated for their anti-inflammatory activities. [ABSTRACT FROM AUTHOR]

Nine new isoquinoline alkaloids, including two proaporphine ( 1 – 2 ), three aporphine ( 3 – 5 ), two oxoaporphine ( 6 – 7 ), and two seco -bisbenzylisoquinoline ( 8 – 9 ), together with three known alkaloids ( 10−12 ) were isolated from the whole plant of Thalictrum wangii. Their structures were established on the basis of spectroscopic data. The antitumor activities of the isolated compounds were evaluated in vitro against glioma stem cells. Compounds 3–8 showed the cytotoxicity with IC 50 values 15–20 μg/mL. [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]

Due to the great economic, health, and medicinal importance, Phoenix dactylifera seeds were chosen for the synthesis of silver nanoparticles (AgNPs) because of their ecofriendly, nonhazardous, cost effectiveness advancement over physical and chemical methods, as green methods are safe, one step, and simple and did not require any chemical reducing and stabilizing agents. The green synthesized AgNPs were characterized by UV-Vis spectroscopy, SEM, HR-TEM, and DLS. Further, the bactericidal activity of synthesized AgNPs against Methicillin-resistant Staphylococcus aureus (MRSA) was investigated by determining MIC/MBC, agar diffusion methods, and electron microscopy. TEM images of the so-formed AgNPs revealed that the NPs were spherical in shape, with a size range of 14–30 nm. The MIC and MBC of AgNPs for MRSA were found to be 10.67±0.94 and 17.33±1.89 μg/ml, respectively. The antibacterial activities were found to be increased with the increasing concentration of AgNPs. The zone of inhibition was greater (24mm) at highest concentrations (500μg/ml) of AgNPs, while smaller (11mm) at lowest concentrations (7.8μg/ml). The SEM images of treated MRSA cells showed wrinkled and damaged cell wall, indicating the disruption and disorganization of membrane. HR-TEM analysis exhibits extensive injury and complete disintegration of cell wall and membrane. Large translucent zones have been seen in the cytoplasm, due to either localized or complete separation of the cell membrane from the cell wall. Overall, these results indicate that green synthesized AgNPs should be considered as an effective treatment and prevention option for the medical devises related infections caused by deadly MRSA and other drug resistant pathogens. [ABSTRACT FROM AUTHOR]

Three new C-methylated phenylpropanoid glycosides (1, 2), a new 8-4′-oxyneolignan (3), together with two known analogs (4, 5), were isolated from the rhizomes of Imperata cylindrical Beauv. var. major (Nees) C. E. Hubb. Their structures were determined by spectroscopic and chemical methods. Compounds 1, 2, and 5 (10 μM) exhibited pronounced hepatoprotective activity against N-acetyl-p-aminophenol (APAP)-induced HepG2 cell damage in vitro assays. Furthermore, their antioxidant activities against Fe2+-cysteine-induced rat liver microsomal lipid peroxidation and the effects on the secretion of TNF-α in murine peritoneal macrophages (RAW264.7) induced by lipopolysaccharides were evaluated. [ABSTRACT FROM AUTHOR]

Chemical investigation of two Irciniidae sponges collected by hand (SCUBA) from Australian near shore waters, afforded six new examples of a rare class of sesterterpene lactam; ircinialactams B ( 1 ), G ( 2 ), H ( 5 ), and I ( 6 ), and 8-hydroxyircinialactams C ( 3 ) and G ( 4 ); together with the new biosynthetically related lactone, ircinialactone A ( 7 ). Also isolated were seven biosynthetically related known Irciniidae metabolites; ircinialactams A ( 8 ) and C ( 9 ), (7 E ,12 E ,20 Z ,18 S )-variabilin ( 10 ), (7 Z ,12 Z ,20 Z ,18 S )-variabilin ( 11 ), (7 E ,12 Z ,20 Z ,18 S )-variabilin ( 12 ), (7 Z ,12 E ,20 Z ,18 S )-variabilin ( 13 ) and irciniafuran A ( 14 ). The structure elucidation of 1 – 14 was achieved by detailed spectroscopic analysis, and consideration of a plausible biosynthetic relationship linking Irciniidae sesterterpene β-furans, lactams and lactones. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The theory of “eighteen incompatible medicaments” (EIM) in traditional Chinese medicine (TCM) is the most representative case of herbal-herbal interactions. Gancao and Gansui are one of the incompatible herbal pairs in EIM. Gancao, also known as “licorice”, is the most frequently used Chinese herb or food additive. Gansui, the root of Euphorbia kansui T.P. Wang, is another famous Chinese herb usually used to treat edema, ascites and asthma but could induce gastrointestinal (GI) tract irritation. Although Gancao and Gansui are incompatible herbal pairs, they are still used in combination in the famous “Gansui-Banxia” decoction. Aim of the study This study was conducted to investigate if Gancao-Gansui combination could exacerbate Gansui induced GI tract injury. Moreover, the impact of Gancao-Gansui combination to gut microbiota and related metabolism pathways were evaluated. Materials and methods Normal mice were divided into different groups and treated with Gancao extracts, Gansui extracts, and Gancao-Gansui combination extracts for 7 days. Serum biomarkers (diamine oxidase activity, lipopolysaccharide, motilin, IL-1β, IL-6, TNF-α) were determined to reflect GI tract damage. Gut microbiota diversity was studied by 16S rDNA sequencing and metagenomes analysis were also conducted to reflect functional genes expression alteration. Fecal hydrogen sulfide concentrations were measured by spectrophotometry to confirm the alteration of Desulfovibrio genus. Fecal lipid metabolomics study was conducted by GC-MS analysis to confirm the change of metagenomes and Mycoplasma abundance. Results Gancao-Gansui combination did not exacerbate GI tract tissue or functional damage but caused gut microbiota dysbiosis and increased some rare genus's abundance including Desulfovibrio and Mycoplasma. Desulfovibrio genus proliferation was confirmed by the disturbance of fecal hydrogen sulfide homeostasis. Gancao-Gansui combination also dys-regulated the metabolic genes in metagenomes. Mycoplasma genus proliferation and the metagenomes changes were both confirmed by metabolic profile analysis of fecal lipids, especially cholesterol. Conclusions Gancao-Gansui combination can impact the gut microbiota diversity and related metabolic functions. Further studies should be carried out when the combination of Gancao-Gansui is used in herbal formulations as this may alter the diversity of the microbiota. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Ficus hispida L.f. (Moraceae) has been used as alternative for traditional medicine in the treatment of various ailments including cancer-cure. The aim of this study was to evaluate the cancer chemopreventive and anticancer activities of crude extracts of F. hispida , with the objective to screen the inhibition of Epstein–Barr virus early antigen, and cytotoxic active components, and provide foundation for potential applications of this promising medical plant. Materials and methods Compounds were isolated from the MeOH extract of F. hispida fruits, and their structure elucidation was performed on the basis of extensive spectroscopic analysis. The isolated compounds were evaluated for their inhibitory activities against the Epstein–Barr virus early antigen (EBV-EA) activation induced by 12- O -tetradecanoylphorbol 13-acetate (TPA) in Raji cells, and cytotoxic activities against human cancer cell lines (HL60, A549, SKBR3, KB, Hela, HT29, and HepG2) and a normal cell (LO2) using MTT method. For the compound with potent cytotoxic activity, its apoptosis inducing activity was evaluated by the observation of ROS generation level expression, and membrane phospholipid exposure and DNA fragmentation in flow cytometry. The mechanisms of the apoptosis induction were analyzed by Western blotting. Results Nineteen compounds, 1 – 19 , including two new isoflavones, 3′-formyl-5,7-dihydroxy-4′-methoxyisoflavone ( 2 ) and 5,7-dihydroxy-4′-methoxy-3′- (3-methyl-2-hydroxybuten-3-yl)isoflavone ( 3 ), were isolated from the MeOH extract of F. hispida fruits. Five compounds, isowigtheone hydrate ( 1 ), 2 , 3 , 9 , and 19 , showed potent inhibitory effects on EBV-EA induction with IC 50 values in the range of 271–340 molar ratio 32 pmol −1 TPA. In addition, five phenolic compounds, 1 – 3 , 10 , and 13 , exhibited cytotoxic activity against two or more cell lines (IC 50 2.5–95.8 μM), as well as compounds 1 and 3 were also displayed high selectivity for LO2/HepG2 (SI 23.5 and 11.8, respectively), while the compound 1 -induced ROS generation leads to activated caspases-3, −8, and −9 apoptotic process in HL60 cells. Conclusion This study has established that the MeOH extract of F. hispida fruits contains isoflavones, coumarins, caffeoylquinic acids, along with other compounds including phenolics and steroid glucoside as active principles, and has demonstrated that the chemical constituents of F. hispida may be valuable as potential chemopreventive and anticancer agents. [ABSTRACT FROM AUTHOR]

Five new tremulane sesquiterpenes, named irlactins F–J ( 1–5 ), were isolated from cultures of the basidiomycete Irpex lacteus together with two known analogues ( 6 and 7 ). Structures and relative configurations of compounds 1–5 were elucidated by spectroscopic data analysis. Compund 4 exhibited moderate cytotoxicities on HL-60, SMMC-7721, A-549, MCF-7, and SW480 cells with IC 50 values of 16.23, 20.40, 25.55, 19.05, and 18.58 μM, respectively. [ABSTRACT FROM AUTHOR]

Six new compounds, including three pyrone derivatives ( 2 – 4 ), one new flavone ( 5 ), and two new naturally-occurring compounds ( 1 and 6 ), together with 16 known compounds were isolated from the leaves and twigs of Hypericum monogynum . In addition, compounds 2–4 are racemates. Their structures and absolute configurations were determined on the basis of extensive analysis of spectroscopic data and ECD calculation. All compounds were evaluated for the inhibitory effects on α-glucosidase, compounds 1 , 5 , and 7 showed moderate inhibitory activities with IC 50 values of 161.46, 257.78, and 11.54 μg/ml, respectively. Compound 8 exhibited weak anti-oxidant activity with IC 50 value of 12.55 μg/ml. [ABSTRACT FROM AUTHOR]

A new phenylspirodrimane dimer, named stachartarin A ( 1 ), was isolated from cultures of the tin mine tailings-associated fungus Stachybotrys chartarum . Its structures were elucidated by means of spectroscopic methods. At the same time, the compound was tested for its cytotoxicity against HL-60, SMMC-7721, A-549, MCF-7, and SW480 cells. [ABSTRACT FROM AUTHOR]

A series of new terminal cyclohexane-type meroterpenoids, ganotheaecoloids A − N ( 1 − 6 , 8 − 13 , 15 , and 16 ), along with three known ones ( 7 , 14 , and 17 ), were isolated from the dried fruiting bodies of Ganoderma theaecolum . Their chemical structures were identified by using spectroscopic data and computational methods. Biological activity of all the new meroterpenoids against COX-2 was evaluated in vitro, only ganotheaecoloid J ( 11 ) was found to have COX-2 inhibitory activity with IC 50 value of 9.96 μM. [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]

Five new compounds, including four new isocoumarin derivatives [orychophramarin A–D ( 1–4 )] and a new monoterpene glycoside [orychovioside A ( 5 )], together with fourteen known compounds were isolated from the seeds of Orychophragmus violaceus . Their structures were established on the basis of chemical evidence and spectroscopic analysis. Compound 1 showed significant cytotoxicity against HCT-116 and Hela cell lines compared with the positive control group (Cisplatin) with IC 50 values of 5.10 and 8.91 μM, respectively. Compound 1 exhibited evident cell cycle retardation that arrested HCT-116 cells at G 2 phase and induced apoptosis in HCT-116 cells in the further mechanism study. [ABSTRACT FROM AUTHOR]

A rare C 12 -norabietane diterpene racemate ( 1 ) and a new abietane diterpene alkaloid ( 2 ) were isolated from the roots of Salvia miltiorrhiza Bunge. Their structures were established by comprehensive spectroscopic analyses, and 1 was successfully resolved by chiral HPLC, demonstrating that 1 is racemic. The absolute configurations of 1a [(+)-miltiorolide A], 1b [(−)-miltiorolide A], and 2 were determined using TDDFT-ECD calculations. 1a and 1b are the first examples of enantiomeric C 12 -norabietane diterpenes featuring an isobutylene with a tetrahydronaphthalene-butyrolactone ring system. The cytotoxic activities of the isolates ( 1 and 2 ) were evaluated against three human cancer cell lines BEL-7402, HT-29 and PANC-28. A plausible biogenetic pathway of 1 was also proposed. [ABSTRACT FROM AUTHOR]

Three new diterpenoids, spicatusenes A–C ( 1 – 3 ), and eleven known ones ( 4 – 14 ) were isolated from the aerial parts of Clerodendranthus spicatus . Their structures were identified by spectroscopic methods. The cytotoxic activities of all the compounds against human cancer cells (HL-60, SMMC-7721, A-549, MCF-7, and SW-480) were examined and found that compounds 2 , 3 , 6 , 8 , 10 , and 13 were active against one or more cancer cell lines. Besides, the renoprotective effects of all the isolates in TGF-β1-induced rat kidney fibroblasts revealed that compounds 3 – 7 , 9 , 13 , and 14 were beneficial for renal fibrosis. Finally, a plausible biosynthetic pathway for 1 via a Hantzsch-type reaction was proposed. [ABSTRACT FROM AUTHOR]

Seven new compounds, including four new chlorinated diphenyl ethers, namely chrysines A–D ( 1 – 4 ), one new dichlorinated xanthone, chrysoxanthone ( 5 ), dichloroorcinol ( 6 ), and one new benzeneacetic acid derivative, 3-isopentyl-4-hydroxy phenylacetic acid methyl ester ( 7 ), along with fourteen known compounds ( 8 – 21 ), were isolated from a deep-sea-derived fungus Penicillium chrysogenum SCSIO 41001. Their structures were determined by extensive spectroscopic methods and X-ray single-crystal diffraction analysis. All of the isolated compounds ( 1 − 21 ) were evaluated for their α-glucosidase inhibitory activity using PNPG method. Among them, nine compounds ( 2 , 3 , 5 , 6 , 8 , 9 , 13 , 17 , and 18 ) exhibited inhibitory activity against α-glucosidase with IC 50 values of 0.35, 0.20, 0.04, 0.16, 0.15, 0.09, 0.14, 0.14, and 0.12 mM, respectively (IC 50 0.28 mM for the positive control acarbose). [ABSTRACT FROM AUTHOR]

Three new diterpenoids, ebractenoids O ~ Q ( 1 – 3 ), and a new phenolic glucoside, γ -pyrone-3- O - β - d -(6-galloyl)-glucopyranoside ( 4 ), together with 6 known compounds, were isolated from the 95% ethanol extract of the roots of Euphorbia ebracteolata , and their structures were elucidated on the basis of spectroscopic data. The absolute configurations of 1 – 3 were determined by electronic circular dichroism (ECD) calculations. The inhibitory effects of all the isolates with exception of compounds 8 and 10 on the NO production in lipopolysaccharide (LPS)-induced macrophages were evaluated. All of them exhibited significant inhibitory activity. [ABSTRACT FROM AUTHOR]

Four new cleistanthane diterpenoids, phyllaciduloids A–D ( 1 – 4 ), were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their structures were elucidated on the basis of extensive spectroscopic analysis. Phyllaciduloids B–D ( 2 – 4 ) present in their structures with ether bond between C-7 and C-16, which were rarely reported. All the isolates were evaluated for their cytotoxic activities against five human cancer cell lines. [ABSTRACT FROM AUTHOR]

Five rare sesquiterpene lactone dimers, vlasouliolides E-I, were isolated from Vladimiria souliei . Their chemical structures were elucidated by spectroscopic analysis. Furthermore, 2 and 4 were unambiguously confirmed by Cu-K α X-ray crystallographic analysis. Compounds 1 , 2 , 4 and 5 exhibited significant anti-inflammatory activity against LPS-induced NO production in RAW 264.7 cells with IC 50 values of 1.88, 4.89, 7.24 and 2.46 μM, respectively. Additionally, compounds 1 and 2 were revealed with potent inhibitory activity of the phosphorylation progress of NF- κ B P65. [ABSTRACT FROM AUTHOR]

Five new limonoids, swieteliacates A–E (1–5) and a tirucallane-type triterpenoid, swietesenin (6), together with four known compounds (7–10) were isolated from fruit of Swietenia macrophylla . Their structures were determined by spectroscopic analyses. The new compounds were tested in vitro for their cytotoxic effects against five human cancer cell lines. Compound 2 exhibited moderate cytotoxic activities against SW480 and HL-60 cancer cell lines with IC 50 values of 30.6 and 32.9 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]

Bioassay-guided fractionation of the dichloromethane extract of the fungus Neofusicoccum austral SYSU-SKS024 led to the isolation of three new ethylnaphthoquinone derivatives, neofusnaphthoquinone A ( 1 ), 6-(1-methoxylethy1)-2,7-dimethoxyjuglone ( 2 ), (3 R ,4 R )-3-methoxyl-botryosphaerone D ( 6 ), together with six known analogs ( 3 – 5 and 7 – 9 ). Their structures were elucidated by spectroscopic analysis and single crystal X-ray diffraction analysis. Neofusnaphthoquinone A ( 1 ) is the third example of the unsymmetrical naphthoquinone dimer, which is rarely found in natural source. All of the isolates were evaluated for their indoleamine 2, 3-dioxygenase (IDO) inhibitory activity, compounds 1 – 6 showed in vitro inhibitory effects against IDO with IC 50 values ranging from 0.11 to 10.92 μM. This is the first time naphthoquinone dimer ( 1 ), as a novel carbon skeleton possessing IDO inhibitory activity, was reported. [ABSTRACT FROM AUTHOR]

Five pairs of new 2-oxoindole alkaloids, (±)-peganumalines A–E ( 1 – 5 ), and a new indole alkaloid, peganumaline F ( 6 ), along with two known analogues, were isolated from the seeds of Peganum harmala . Their structures and absolute configurations were elucidated through spectroscopic analyses and quantum chemistry calculations. Notably, (±)-peganumalines A ( 1 ) represent a pair of rare 2-oxoindole dimeric alkaloid enantiomer with the hitherto unknown carbon skeleton. All isolates were tested for antiproliferative and antibacterial activities. [ABSTRACT FROM AUTHOR]

The seeds of Swietenia macrophylla King (SM) (Meliaceae) are used as a folk medicine for the treatment of hypertension in Malaysia. However, the antihypertensive and vasorelaxant effects of SM seeds are still not widely studied. Thus, this study was designed to investigate the in vivo antihypertensive effects and in vitro mechanism of vasorelaxation of a 50% ethanolic SM seed extract (SM50) and the fingerprint of SM50 was developed through tri-step Fourier transform infrared (FTIR) spectroscopy. The vasorelaxant activity and the underlying mechanisms of SM50 were evaluated on thoracic aortic rings isolated from Sprague-Dawley rats in the presence of antagonists. The pharmacological effect of SM50 was investigated by oral administration of spontaneously hypertensive rats (SHRs) with three different doses of SM50 (1000, 500, and 250 mg/kg/day) for 4 weeks and their systolic blood pressure (SBP) and diastolic blood pressure (DBP) values were measured weekly using tail-cuff method. The tri-step FTIR macro-fingerprint of SM50 showed that SM50 contains stachyose, flavonoids, limonoids, and ester, which may contribute to its vasorelaxant effect. The results showed that the vasorelaxant activity of SM50 was mostly attributed to channel-linked receptors pathways through the blockage of voltage-operated calcium channels (VOCC). SM50 also acts as both potassium channels opener and inositol triphosphate receptor (IP3R) inhibitor, followed by β2-adrenergic pathway, and ultimately mediated through the nitric oxide/soluble guanylyl cyclase/cyclic 3′,5′-guanosine monophosphate (NO/sGC/cGMP) signaling pathways. The treatment of SM50 also significantly decreased the SBP and DBP in SHRs. In conclusion, the antihypertensive mechanism of SM50 was mediated by VOCC, K+ channels, IP3R, G-protein-coupled β2-adrenergic receptor, and followed by NO/sGC/cGMP signaling mechanism pathways in descending order. The data suggested that SM50 has the potential to be used as a herbal medicament to treat hypertension. [ABSTRACT FROM AUTHOR]

Four new chromenopyridine derivatives, phochrodines A–D ( 1 − 4 ), were identified from mangrove entophytic fungus Phomopsis sp. 33# by means of various modern chromatographic, spectroscopic and single crystal X-ray diffraction techniques. Compounds 1 − 4 with an unusual 5 H -chromeno[4,3-b]pyridine skeleton were the first naturally occurring chromenopyridines. Their anti-inflammatory, antioxidant and cytotoxic activities were evaluated. 3 and 4 showed moderate inhibition of nitric oxide production with IC 50 values of 49.0 as well as 51.0 μM, respectively. 4 had well ability to scavenge DPPH radical with IC 50 value of 34.0 μM. The four had no cytotoxic activity for MDA-MB-435 breast cancer cells. [ABSTRACT FROM AUTHOR]

Four new phenylisotertronic acids ( 1a/1b , 2a , and 3a ) were isolated from a TCM endophytic fungal strain Phyllosticta sp. J13-2-12Y obtained from the leaves of Acorus tatarinowii , along with two known ones ( 2b and 3b ). Compounds 1 − 3 all existed as mixtures of enantiomers, and their corresponding optically pure enantiomers were successfully isolated by chiral HPLC. The structures of isolated compounds were determined by comprehensive spectroscopic analyses and X-ray diffraction. Their absolute configurations were determined by ECD experiments and quantum chemical calculations. In addition, the antimicrobial activities and the cytotoxicities of these three pairs of optically pure enantiomers ( 1a/1b , 2a / 2b , and 3a/3b ) had been evaluated. [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]

Phytochemical investigation of the roots of Cynanchum bungei Decne (Asclepiadaceae) led to the elucidation of seven C 21 -steroidal glycosides ( 1 – 7 ) including three new compounds ( 1 – 3 ), named cynabungosides A–C, one new eudesmane-type sesquiterpene ( 8 ), named cynabungone, and one new humulane-type sesquiterpene ( 9 ), named cynabungolide. Their structures were elucidated on the basis of extensive spectroscopic analysis. The absolute configurations of 8 and 9 were defined unequivocally by ECD analysis and X-ray crystallography, respectively. A putative biosynthetic pathway of humulane-type sesquiterpenes 9 and 10 is proposed. [ABSTRACT FROM AUTHOR]