Secondary Metabolites from Anthonotha cladantha (Harms) J.Léonard

The phytochemical investigation of the crude methanolic extracts roots and stem bark of Anthonotha cladantha (Harms) J.Léonard led to the isolation and identification of twelve secondary metabolites: 2,3-dihydroxypropyl hexacosanoate (1), hederagenine (2), cycloeucalenol (3), 2α-hydroxylupeol (4), betulinic acid (5), lupeol (6), heptacosan-2-one (7), triacontanoic acid (8), stigmast-4-en-3-one (9), β-sitosterol (10), stigmasterol (11), and stigmasterol-3-O-β-D-glucopyranoside (12). Their structures were elucidated with the help of their spectroscopic and physical data and by comparison with those reported in the literature. To the best of our knowledge, from all those compounds, 2,3-dihydroxypropyl hexacosanoate (1), hederagenine (2), cycloeucalenol (3), 2α-hydroxylupeol (4), and betulinic acid (5) are being reported for the first time from this genus. In addition, the acetylation of compound 1 afforded a new derivative 3-(hexacosanoyloxy)propane-1,2-diyl diacetate (1a).Compound 1 possessed a moderate α-glucosidase inhibitory activity with an IC50 value of 39.2 ± 0.22 µM; it neither showed antioxidant activity nor inhibition against the enzyme urease. Compound 1a exhibited weak antioxidant activity in the DPPH assay with an IC50 value of 80.3 ± 0.83 μM but was inactive against α-glucosidase and urease. Furthermore, both compounds 1 and 1a were inactive against seven pathogenic bacterial strains.

Chemicals Constituents from Leaves of Diospyros iturensis (Gürke) Letouzey & F. White and their Biological Activities

he chemical investigation of the methanolic crude extract of leaves of Diospyros iturensis gave us 15 known secondary metabolites identified as mixture of α-amyrenone (1) and β-amyrenone (2), β-amyrin (3), mixture of β-sitosterol (4) and stigmasterol (5), betulin (6), uvaol (7), betulinic acid (8), ursolic acid (9), corosolic acid (10), actinidic acid (11),11-O-p-hydroxybenzoylbergenin (12), bergenin (13) and mixture of stigmasterol glucoside (14) and β-sitosterol glucoside (15) respectively. The structures of secondary metabolites were elucidated with the help of NMR and mass spectral data and by comparison of their spectral data with literature.Among the fifteen isolated compounds, four compounds were identified for the first time in Diospyros genus.These included uvaol (7), corosolic acid (10), actinidic acid (11) and 11-O-p-hydroxybenzoylbergenin (12).Crude methanolic extract of leaves and four isolated compounds including betulin (6), betulinic acid (8), 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) were evaluated for their antiproliferative activity against two cancer cell lines CAL-27 and NCI-H460 by the MTT assay, antioxidant potential and inhibitory activity against the lipoxygenase and urease enzymes, respectively. The results indicated that the methanolic crude extract of leaves exhibited moderate antioxidant activity and was inactive against the two cancer cell lines. Betulin (6),11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) exhibited moderate antioxidant and lipoxygenase inhibition with IC 50 = 65.8, 85.6, 82.5 µM and IC50 = 58.5, 95.2, 76.2 µM, respectively. Furthermore, 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) exhibited moderate urease inhibition activity with IC50 values of 45.6 µM and 49.8 µM, respectively.

Chemicals Constituents from Leaves of Diospyros iturensis (Gürke) Letouzey & F. White and their Biological Activities

he chemical investigation of the methanolic crude extract of leaves of Diospyros iturensis gave us 15 known secondary metabolites identified as mixture of α-amyrenone (1) and β-amyrenone (2), β-amyrin (3), mixture of β-sitosterol (4) and stigmasterol (5), betulin (6), uvaol (7), betulinic acid (8), ursolic acid (9), corosolic acid (10), actinidic acid (11),11-O-p-hydroxybenzoylbergenin (12), bergenin (13) and mixture of stigmasterol glucoside (14) and β-sitosterol glucoside (15) respectively. The structures of secondary metabolites were elucidated with the help of NMR and mass spectral data and by comparison of their spectral data with literature.Among the fifteen isolated compounds, four compounds were identified for the first time in Diospyros genus.These included uvaol (7), corosolic acid (10), actinidic acid (11) and 11-O-p-hydroxybenzoylbergenin (12).Crude methanolic extract of leaves and four isolated compounds including betulin (6), betulinic acid (8), 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) were evaluated for their antiproliferative activity against two cancer cell lines CAL-27 and NCI-H460 by the MTT assay, antioxidant potential and inhibitory activity against the lipoxygenase and urease enzymes, respectively. The results indicated that the methanolic crude extract of leaves exhibited moderate antioxidant activity and was inactive against the two cancer cell lines. Betulin (6),11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) exhibited moderate antioxidant and lipoxygenase inhibition with IC 50 = 65.8, 85.6, 82.5 µM and IC50 = 58.5, 95.2, 76.2 µM, respectively. Furthermore, 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) exhibited moderate urease inhibition activity with IC50 values of 45.6 µM and 49.8 µM, respectively.

Synthesis, biological screening and molecular docking studies of some ethylated sulfonamides having 1,4-Benzodioxane moiety

The presented study comprises the synthesis of a new series of ethylated sulfonamides in which 1,4- benzodioxane moietyhas been incorporated. The reaction of 1,4-benzodioxane-6-amine [1] with ethane sulfonyl chloride [2] yielded N-[2,3-dihydrobenzo[1,4]dioxin-6-yl] ethanesulfonamide [3], which further on treatment with various alkyl/aralkyl halides, 4a-r, in N,N-dimethylformamide [DMF] and in the presence of lithium hydride [LiH] acting as a weak base and catalyst;yielded derivativesofN-alkyl/aralkyl substituted N-[2,3-dihydrobenzo [1,4] dioxin-6- yl] ethanesulfonamides [5a-r]. The characterization of these derivatives was carried out by different spectroscopic techniques like infra red, proton-NMR and mass spectrometry; then screened against various enzymes i.e. acetylcholinesterase, butyrylcholinesterase, lipoxygenase and alpha-glucosidase enzymes and five different bacterial strains. The synthesized compounds were found to be good inhibitors of lipoxygenase but moderate inhibitors of AChE, BChE and alpha-glucosidase; whereas compounds 3, 5a, 5f, 5n and 5r were found good antibacterial compounds. The interaction between inhibitors and target enzymes [cholinestrases and lipoxygenase] was computationally observed which correlated with the experimental results

Evaluation of Iyengariastellata for its hypolipidemic and hepatoprotective activity

Cholesterol is believed to be the major regulator involved in the formation and progression of atheroma plaque. Seaweeds are known to possess enormous biological activities. They contain variety of active constituents, which have pharmacological significance. The objective of this study is to explore hypolipidemic and hepatoprotective activities of the brown seaweed Iyengariastellata. Ethanolic extract of seaweed was suspended in distilled water and administered orally at 10mg/200g body weight to rabbits for 30 days and total lipid level, cholesterol, triglycerides, HDL, LDL, VLDL, alkaline phosphatase, SGPT, SGOT, Gamma GT were assessed. The results showed overall decrease in lipid profile whereas Iyengariastellata increased liver enzymes except SGPT which was decreased highly significantly, since SGPT is more specific indicator of liver injury, decreased value of SGPT indicates that Iyengariastellata toxicity is less severe and reversible with marked hypolipidemic effect, but during the course of ingestion of the seaweed the liver enzymes must be carefully monitored to ensure liver safety

Solanaceae: [the potato family]

In this article nomenclature, economic, ornamental, medicinal, food and nutritional importance of the family Solanaceae is described. Family composition in general, morphology and chemical composition are also discussed. Supporting literature with the help of which this information has been compiled is also given at the end