These results suggest that OATP2B1 plays an important role in the stereoselective pharmacokinetics of fexofenadine and that one-time apple juice ingestion probably inhibits intestinal OATP2B1-mediated transport of both enantiomers. In addition, this study demonstrates that the OATP2B1 inhibition effect does not require repeated ingestion or a large volume of apple juice.

Isoflavone glucosides (2'-hydroxy,5-methoxy genistein-7-O-glucoside (1), 2'-hydroxy genistein-7-O-gentibioside (2), 5-methoxy genistein-7-O-glucoside (3), 3',5-dimethoxy genistein-7-O-glucoside (4), 2'-hydroxy genistein-7-O-glucoside (5), genistein-7-O-gentibioside (6), 2'-hydroxy,5-methoxy genistein-4',7-O-diglucoside (7), and 2'-hydroxy genistein-4',7-O-diglucoside (8)) were isolated from the groundnut of Apios americana Medik. Their structures were elucidated on the basis of HR-ESI-MS and 1D- and 2D-NMR analyses. Compounds 1, 2, 4, and 7 are new compounds presented here for the first time. Compounds 2 and 5 were proven to be androgen receptor antagonists due to their binding activities for androgen receptors (IC50 280 and 160 μM, respectively) and the inhibitory activity of androgen-induced expression of prostate-specific antigen (PSA) mRNA in LNCaP (prostate adenocarcinoma) cells (IC50 20 and 18 μM, respectively).

Aside from the well-studied conventional actinomycetes such as Streptomyces, the less investigated genera of actinomycetes also represent a promising source of natural products. Genome mining indicated that members of the underexplored genus Pseudosporangium, from which no secondary metabolites have been reported to date, may harbor the biosynthetic machinery for the formation of novel natural products. The strain RD062863, that is available at a public culture collection, was obtained and subjected to metabolite analysis, which resulted in the discovery of a novel cyclopeptide, pseudosporamide (1), along with three new oligomycin-class polyketides, pseudosporamicins A–C (2–4). The unusual structure of compound 1, featured by a biaryl-bond bridging across a tripeptide scaffold, N-acetyl-ʟ-Tyr-ʟ-Pro-ʟ-Trp, was determined by a combination of spectroscopic analyses, chemical derivatization, ECD calculation, and DFT-based theoretical chemical shift calculation, revealing the presence of an (S a)-axial chirality around the biaryl bond. Compounds 2–4 lacked hydroxylation on the side chain of the spiroacetal rings, which showed clear contrast to other oligomycin congeners and related polyketides with ring-truncation or expansion. The new macrolides 2–4 displayed potent antimicrobial activity against the Gram-positive bacterium Kocuria rhizohpila and the plant pathogenic fungus Glomerella cingulata. All compounds showed moderate cytotoxicity against P388 murine leukemia cells with IC50 values in the micromolar to submicromolar ranges. These results exemplified the validity of phylogeny-focused strain selection combined with biosynthetic gene-directed genome mining for the efficient discovery of new natural products.

Abstract. Sibero MT, Siswanto AP, Frederick EH, Wijaya AP, Syafitri E, Farabi K, Murwani R, Saito S, Igaras Y. 2020. Antibacterial, cytotoxicity and metabolite profiling of crude methanolic extract from andaliman (Zanthoxylum acanthopodium) fruit. Biodiversitas 21: 4147-4154. The local community in North Sumatra has utilized andaliman fruit (Zanthoxylum acanthopodium) as spices for traditional cuisines because it has a unique flavor. Information on the antimicrobial activity of Z. acanthopodium fruit against aquaculture pathogens and its bioactivity against leukemia cell lines are limited. The purposes of this study were to evaluate the antimicrobial activity of Z. acanthopodium fruit against Tenacibaculum maritimum, Vibrio alginolyticus, V. anguillarum, V. harveyi that are known as pathogens in aquaculture; to determine cytotoxic property against murine P388 leukemia cells; and to characterize its metabolites profile. The sample was extracted using methanol by the maceration method. Antibacterial assay was conducted by Kirby-Bauer disc diffusion method; while cytotoxicity assay using the XTT method. Proximate analysis showed that Z. acanthopodium fruit contained 63.41% of moisture, 24.73% of crude fiber, 9.81% of crude protein, 6.90% of ash, and 2.55% of crude fat. Several phytochemical components were detected, such as alkaloid, flavonoid, tannin, triterpenoid, and steroid. The GC/MS analysis indicated the presence of various compounds from terpenoid and terpenes derivatives. This study indicated that Z. acanthopodium fruit was not potential as antibacterial agents against the aquaculture pathogens; however, the methanol extract showed cytotoxic potential with IC50 19.14 µg/mL against murine P388 leukemia cells.

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