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Phytochemical study on the methanol extract of the stems and leaves of Kadsura induta led to the isolation of six dibenzocyclooctadiene lignans, including three new compounds named kadsindutalignans A–C (1–3), and three known ones, heteroclitalignan B (4), kadsuphilin C (5) and kadsulignan E (6). Their structures were elucidated based on extensive spectroscopic analyses, including HRESIMS, 1D- (1H NMR and 13C NMR), 2D-NMR (HSQC, HMBC, 1H-1H COSY and NOESY), and experimental circular dichroism (CD) spectra. All the isolates inhibited NO production in LPS-activated RAW264.7 cells with IC50 values in the range from 5.67 ± 0.54 µM to 38.19 ± 2.03 µM, compared to that of the positive control of NG-monomethyl-L-arginine acetate (L-NMMA) with an IC50 value of 8.90 ± 0.48 µM. Interestingly, the new compound 2 showed potential inhibition of NO production with an IC50 value of 5.67 ± 0.54 µM, which was higher than that of the positive control. [ABSTRACT FROM AUTHOR]

One new indol, N-methoxymethyltryptophol (1), one new phenolic, (2 R)-2-(4-hydroxyphenyl)ethyl 2-hydroxy-3-phenylpropanoate (2) and fifteen known compounds (3–17) were isolated from the methanol extract of the fermentation of marine microalgae Aurantiochytrium sp. SC145. Their structures were elucidated by 1D-, 2D-NMR spectroscopic analysis, HR-ESI-MS, quantum chemical calculation methods and by comparing their NMR data with those reported in the literature. All compounds were evaluated for their antimicrobial activities against microorganisms. Compounds 2, 3 and 11 significantly exhibited antimicrobial activities on all tested Gram-(+), Gram-(-) bacteria and the yeast C. albicans with MIC values ranging from 32 to 256 µg/mL. [ABSTRACT FROM AUTHOR]

Two new iridoid glycosides link with phenylpropanoids, rehmanniosides G (1) and H (2) along with 11 known compounds, 6-O-(E)-caffeoylajugol (3), 6-O-(E)-feruloylajugol (4), verbasoside (5), jionoside C (6), acteoside (7), leucosceptoside A (8), brachynoside (9), jionoside B1 (10), jionoside A1 (11), isoacteoside (12) and isomartynoside (13) were isolated from the roots of Rehmannia glutinosa (Gaertn.) DC. Their chemical structures were elucidated on the basis of extensive spectroscopic methods, including 1D, 2D NMR and mass spectra. Compounds 7 − 11 showed significant inhibitory α-glucosidase with IC50 values ranging from 261.4 to 408.7 μM (acarbose, IC50 of 204.2 ± 19.9 μM). [ABSTRACT FROM AUTHOR]

Four new aaptamine alkaloids, named as 9-methoxy-N-demethylaaptanone (1), 3,5-dicarbomethoxy-1,​6-​naphthyridine (2), aaptosvanphongs A and B (3 and 4), and three known aaptamine alkaloids as 2-methoxy-3-oxoaaptamine (5), 8,9,9-trimethoxy-9H-benzo[de][1,6]-naphthyridine (6), and demethyl(oxy)aaptamine (7) were isolated from the sponge Aaptos by various chromatographic methods. Their structures were established by extensive spectroscopic analyses (HR-ESI-MS, 1 D and 2 D NMR) and by comparison of the spectral data with those reported in the literature. Compounds 1-7 significantly showed cytotoxic effects against SK-LU-1, MCF-7, HepG2, and SK-Mel-2 cell lines with IC50 values in range from 7.7 ± 0.8 to 51.4 ± 1.8 µM. Among them, compound 7 exhibited the most cytotoxic activity with corresponding IC50 values of 9.2 ± 1.0, 7.8 ± 0.6, 8.4 ± 0.8, and 7.7 ± 0.8 µM. [ABSTRACT FROM AUTHOR]

Three undescribed dihydrostilbene glycosides, 3,5-dihydroxyldihydrostilbene 4′-O-[6′′-O-(4′′′-hydroxylbenzoyl)]-β-D-glucopyranoside (1), 3,5-dihydroxyldihydrostilbene 4′-O-(6′′-O-galloyl)-β-D-glucopyranoside (2), and 3,5-dihydroxyldihydrostilbene 4′-O-[6′′-O-(3′′′,4′′′-dimethoxyl)galloyl]-β-D-glucopyranoside (3), and seven known compounds, kaempferol 3-O-β-D-glucopyranoside (4), isoquercitrin (5), kaempferol 3-O-α-L-rhamnoside (6), quercitrin (7), (6S,9R)-roseoside (8), (-)-epicatechin 3-O-gallate (9), and (-)-epigallocatechin 3-O-gallate (10) have been isolated from the methanol extract of the leaves of Camellia sinensis var. assamica (J.W.Mast.) Kitam. (synnonym of Camellia assamica (Mast.) H.T.Chang) (Theaceae). Their structures were elucidated by spectroscopic methods (1 D-, 2 D-NMR) and mass spectra. All compounds were evaluated for cytotoxic activity against human oral cancer (CAL27) and human breast cancer (MDAMB231) cell lines. Compound 10 showed significant cytotoxic activity against CAL27 and MDAMB231 cell lines with IC50 values of 9.78 ± 0.25 and 3.27 ± 0.18 μM, respectively, compared to those of positive control, capecitabine (IC50 values of 8.20 ± 0.75 and 5.20 ± 0.89 μM). [ABSTRACT FROM AUTHOR]

A new stereoisomer Meso-araguspongine C together with nine reported macrocyclic bis-quinolizidine alkaloids araguspongines A, C, E, L, N−P, petrosin, and petrosin A were isolated from marine sponge Xestospongia muta. Stereochemistry of meso-araguspongine C (2) and araguspongines N-P (3−5) were established by their NMR data and conformational analyses. Both araguspongine C (1) and meso-araguspongine C (2) exhibited great cytotoxic activity towards HepG-2, HL-60, LU-1, MCF-7, and SK-Mel-2 human cancer cells (IC50 in the range of 0.43–1.02 μM). At a concentration of 20 μM, isolated compounds (1−10) also showed modest inhibitory effects (from 7.6 to 40.8%) on the NO production in LPS activated RAW264.7 macrophages. [ABSTRACT FROM AUTHOR]

Context: Traditional Chinese medicines have attracted increasing interest as potential sources of novel drugs with a wide range of biological and pharmacological activities.Annona glabraLinn (Annonaceae) is used in traditional medicine as an anticancer drug. Phytochemical investigation of this plant led to the isolation of acetogenins,ent-kauranes, peptides, and alkaloids. In addition, compounds exhibited anticancer, anti-HIV-reserve, and antimalaria. Objective: Isolation, structure determination, and cytotoxic activity evaluation of compounds from the methanol extract fromA. glabrafruits. Materials and methods: Using chromatographic methods to isolate compounds from theA. glabramethanol extract. The cytotoxic activity of compounds was evaluated by a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. In addition, compounds which showed significant cytotoxic activity were chosen for further study apoptosis characteristics. Results: One new, (2E,4E,1′R,3′S,5′R,6′S)-dihydrophaseic acid 1,3′-di-O-β-d-glucopyranoside, and eight known compounds, (2E,4E,1′R,3′S,5′R,6′S)-dihydrophaseic acid 3′-O-β-d-glucopyranoside (2), icariside D2(3), icariside D26′-O-β-d-xylopyranoside (4), 3,4-dimethoxyphenylO-β-d-glucopyranoside (5), 3,4-dihydroxybenzoic acid (6), blumenol A (7), cucumegastigmane I (8), and icariside B1(9), were isolated from the fruits ofA. glabra.Icariside D2(3)was found to show significant cytotoxic activity on the HL-60 cell line with the IC50value of 9.0 ± 1.0 µM and did not show cytotoxic activity on the Hel-299 normal cell line. The further test indicated that compound3induced apoptosis via alteration of expression of apoptosis-related proteins and decreased phosphorylation of AKT in HL-60 cells. Discussion and conclusion: The results suggested that the constituents fromA. glabramay contain effective compounds which can be used as anticancer agents. [ABSTRACT FROM AUTHOR]