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1.
Carbohydr Res ; 537: 109074, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38452719

RESUMEN

Two new glycosides, sindosides A-B (1-2), along with 11 previously identified metabolites (3-13), were isolated from an ethanolic extract of the leaves of Sindora siamensis var. maritima. The structures of the purified phytochemicals were elucidated by interpreting their spectroscopic data (IR, NMR, and HRMS). The absolute configuration of compound 1 was established by experimental and calculated ECD spectra. The antimicrobial results revealed that compound 8 selectively inhibited C. albicans fungal with a MIC value of 64 µg/mL, whereas 11 presented a weak inhibition toward E. faecalis, S. aureus, and B. cereus bacterial strains with the same MIC value of 128 µg/mL. Interestingly, compounds 1, 2, 8, 9, and 11 showed α-glucosidase inhibitory activity with IC50 values ranging from 14.42 ± 0.21 to 30.62 ± 0.18 µM, which were more active than the positive control (acarbose, with an IC50 value of 46.78 ± 1.37 µM). Enzyme kinetic analysis revealed that compounds 1, 2, and 11 behaved as uncompetitive inhibitors with Ki values of 8.60 ± 1.04, 5.16 ± 0.73, and 7.17 ± 0.98 µM, respectively.


Asunto(s)
Antiinfecciosos , alfa-Glucosidasas , alfa-Glucosidasas/metabolismo , Cinética , Staphylococcus aureus , Antiinfecciosos/farmacología , Extractos Vegetales/química , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/química
2.
Nat Prod Res ; : 1-8, 2023 Dec 12.
Artículo en Inglés | MEDLINE | ID: mdl-38084396

RESUMEN

Repeated column chromatography resulted in the isolation of two new megastigmane derivatives, methyl-tiliaceates A and B (1 and 2), along with four known metabolites (3-6) from the leaves of Hibiscus tiliaceus L. The structures of the purified phytochemicals were elucidated by interpreting their NMR, HRESIMS, and CD spectroscopic data, as well as comparison with the previous literature. The compounds isolated were subjected to in vitro antimicrobial assays against a panel of pathogenic microorganisms (Enterococcus faecalis, Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enterica, and Candida albicans). Compound 1 showed obvious selective inhibition against the B. cereus strain, whereas 3 - 5 showed weak inhibitory activities against E. faecalis and S. aureus bacterial, and C. albicans fungal strains (with MIC values ranging from 128 to 256 µg/mL).

4.
Bioorg Chem ; 88: 102921, 2019 07.
Artículo en Inglés | MEDLINE | ID: mdl-30991191

RESUMEN

In a search for anti-inflammatory activity in resources from Vietnamese mangroves, we found that a methanolic extract from the leaves of Calophyllum inophyllum (CIL) showed significant anti-inflammatory effects in vitro. Using various chromatographic techniques, we subsequently isolated 12 compounds (1-12) from a methanolic extract of CIL, including two novel compounds (1-2). The inhibitory effects of these compounds on lipopolysaccharide-induced nitric oxide (NO) production in RAW264.7 cells were also evaluated. Compound 1 significantly suppressed NO production (IC50 = 2.44 ±â€¯0.88 µM), the secretion of pro-inflammatory cytokines (including interleukin-1 beta and tumor necrosis factor alpha), and the expression of inducible nitric oxide synthase through downregulation of nuclear factor-kappa-B signaling cascades. These results suggest that C. inophyllum leaves might be a useful resource for the development of drugs for the treatment of inflammation.


Asunto(s)
Antiinflamatorios/farmacología , Calophyllum/química , Triterpenos/farmacología , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Lipopolisacáridos/farmacología , Ratones , Subunidad p50 de NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Células RAW 264.7 , Estereoisomerismo , Triterpenos/química , Triterpenos/aislamiento & purificación , Factor de Necrosis Tumoral alfa/metabolismo
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