Eleven previously undescribed arylnaphthalide lignans (1−11) together with seven known compounds were isolated from the whole plant of Justicia depauperata. The structures of 1−11 were elucidated by spectroscopic analysis and mass spectrometry. Compounds 6 (IC 50 = 4.1 μM) and 9 (IC 50 = 9.5 μM) displayed cytotoxic activity against the KB-3-1 cervical carcinoma cell line. This report provides an insight into the conformational equilibria occurring in the arylnaphthalide lignan constituents of this plant.
The chemical investigation of the n-hexane fraction from the methanol extract of the stem bark of Symphonia globulifera Linn f., which displayed good in vitro activity against Leishmania donovani NR-48822 promastigotes (IC50 43.11 µg/mL), led to the isolation of three previously unreported polyprenylated benzophenones, guttiferone U (1), V (2)/W (3), and a new tocotrienol derivative named globuliferanol (4), along with 11 known compounds (5–15). Their structures were elucidated based on their NMR and MS data. Some isolated compounds were assessed for both their antileishmanial and cytotoxic activities against L. donovani and Vero cells, respectively. Guttiferone K (5) exhibited the best potency (IC50 3.30 μg/mL), but with low selectivity to Vero cells. The n-hexane fraction and some compounds were also assessed in vitro for their antibacterial activity against seven bacterial strains. All the samples exhibited moderate to potent antibacterial activity (MICs ≤ 15.6 µg/mL) against at least one of the tested strains.
The search for antileishmanial plants used in traditional medicine led to the choice of CH2Cl2–MeOH (1:1) crude extract of the fruits and stem bark of Pentadesma butyracea Sabine (Clusiaceae) which displayed good activity in vitro against Leishmania donovani 1S (MHOM/SD/62/1S) promastigotes during preliminary screening with IC50 values 5.96 and 26.43 μg mL−1, respectively. The fractionation of both extracts using flash chromatography yielded active fractions with IC50 values ranging from 2.71 to 18.88 μg mL−1. Fourteen compounds (1–14) were isolated from the obtained fractions using successive column chromatographies and their structures were elucidated based on the analysis of their NMR and MS data. Daphnifolin (1), epicathechin (3), α-mangostin (9) and 9-hydroxycalabaxanthone (14) exhibited potent antileismanial activity against L. donovani 1S (MHOM/SD/62/1S) promastigotes with IC50 values of 2.01, 9.09, 3.37, and 6.87 μg mL−1, respectively and good selectivity towards Raw 264.7 macrophage cells (SI > 2.4). Extracts, fractions and some isolates were also assessed in vitro for their antibacterial activity against six bacterial strains [Salmonella typhi (CPC), Enterobacter cloacae (CPC), Pseudomonas aeruginosa HM801, Staphylococcus aureus ATCC 43300, Streptococcus pneumoniae ATCC 491619, Escherichia coli ATCC 25322] using serial microdilution method. Among the tested samples, the stem bark extract of P. butyracea as well as compounds 2 and 8 showed good to moderate activity against the aforementioned bacterial strains with MIC ≤ 250 μg mL−1.
The CH2Cl2−MeOH (1:1) extract of the roots of Rumex nepalensis (Polygonaceae) displayed significant antibacterial activity against five bacterial strains with MICs (62.5-31.2 μg.mL −1 ). The EtOAc soluble fraction displayed a significant activity against the same strains with MICs (31.2-3.9 μg.mL −1 ). The purification of the EtOAc fraction yielded one new phenylisobenzofuranone derivative, berquaertiide (1), along with 19 known compounds (2-20). Their structures were elucidated based on the analysis of their NMR and MS data. All the isolated compounds were assessed for their antibacterial activity. Compound 2 was the most active against all the tested strains (15.7 to 1.9 μg.mL −1 ), while compounds 3-7 displayed good activities on at least one of the tested strains. In addition, seven analogues (21-27) of compound 2 were prepared and further assessed for their antibacterial activity. Compounds 26 and 27 were most active than 2 against Salmonella enterica and Klebsiella pneumoniae with MIC (125 and 15.6 μg.mL −1 , respectively).
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