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J Nat Pharm. – Page 2

The in vitro anticancer activity of the crude extract of the sponge-associated fungus Eurotium cristatum and its secondary metabolites

Ana Paula Almeida, Tida Dethoup, Narong Singburaudom, Raquel Lima, Maria Helena Vasconcelos, Madalena Pinto, Anake Kijjoa

Journal of Natural Pharmaceuticals 2010 1(1):25-29

Background: Marine natural products has captivated many researchers over the years and there is always a need for sources of diverse and pharmacologically active leads in the area of anticancer drugs. Materials and Methods: The ethyl acetate extract of the fungus Eurotium cristatum (ECE), isolated from the marine sponge Mycale sp., furnished 2-(2', 3-epoxy-1',3'-heptadienyl)-6-hydroxy-5-(3-methyl-2-butenyl) benzaldehyde (1), 1,8-dihydroxy-6-methoxy-3-methyl-9,10-anthracenedione (physcion,2), and the dioxopiperazine alkaloid echinulin (3). The structures of the compounds were established by Nuclear Magnetic Resonance (NMR) spectral analysis (1H, 13C, DEPT, COSY, HSQC, and HMBC). The ECE and its metabolites were evaluated for their growth inhibitory activity on the following three human tumor cell lines: breast adenocarcinoma (MCF-7), non-small lung cancer (NCI-H460), and melanoma (A375-C5). Results: The results showed that the ECE was active in all the three cell lines, with the values of GI50 = 44.3 ± 1.2, 45.5 ± 7.5, and 71.3 ± 2.1 μg/ml for MCF-7, NCI-H460, and A375-C5, respectively. Compound 1 also exhibited moderate growth inhibitory activity against all the three cell lines (GI50 = 58.3 ± 1.2, 46.0 ± 5.5, and 116.7 ± 7.2 μM for MCF-7, NCI-H460, and A375-C5, respectively), whereas compound 3 showed only weak inhibition against MCF-7 (GI50 = 109.7 ± 0.3 μM) and NCI-H460 (GI50 = 96.7 ± 1.5 μM) but was inactive against A375-C5 (GI50 >150 μM). On the contrary, compound 2 was inactive in all the three cell lines at the highest concentration tested (150 μM). Furthermore, ECE was investigated for its effect on the cell cycle in the NCI-H460 cells. Analysis of the cell cycle profile showed that ECE was able to cause a slight cell arrest in the G1 phase, with a corresponding decrease of cells in the S and G2/M phases. Conclusion: The secondary metabolites isolated [Compound 1] from the crude ethyl acetate extract of the culture of the marine fungus E. cristatum were found as the most potent compound regarding cell growth inhibition.

Antibacterial, antifungal and free radical scavenging activity of Croton gibsonianus Nimm. Grah. (Euphorbiaceae)

KS Vinayaka, D Swathi, TR Prashith Kekuda, K Bhagath, N Mallikarjun

Journal of Natural Pharmaceuticals 2010 1(1):46-50

Background: Croton gibsonianus Nimm. Grah is a shrub belonging to the family Euphorbiaceae and grows in the under-story of the evergreen forests of the Western Ghats. The present study was performed to investigate the antibacterial, antifungal and free radical scavenging potentials of the methanol extract of C. gibsonianus leaves. Materials and Methods: The powdered leaf material was subjected to soxhlet extraction using methanol. The antibacterial and antifungal activities of the methanolic extract were determined by the agar well diffusion method. The free radical scavenging activity was performed using the DPPH free radical scavenging assay. Results: The extract was found to cause marked inhibition of Pseudomonas aeruginosa followed by Escherichia coli and Staphylococcus aureus. Among fungi, Aspergillus niger was inhibited to a greater extent, followed by Chrysosporium indicum, Candida albicans and Trichophyton rubrum. The inhibition of test fungi was dose-dependent. The radical scavenging activity was found to be concentration dependent and the IC 50 value for the extract was found to be 43.78 μg/ml. A phytochemical analysis of the extract showed the presence of saponins, tannins, glycosides and terpenoids. Conclusion: The methanolic extract of C. gibsonianus leaves could be used in the treatment of bacterial and fungal infections and damage caused by free radicals. The presence of various phytochemicals might be responsible for these activities of the extract. Further studies on isolation of constituents from the extract and their biological activities are under investigation.

Potent insecticidal activity of two Streptomyces species isolated from the soils of the western ghats of Agumbe, Karnataka

TR Prashith Kekuda, KS Shobha, R Onkarappa

Journal of Natural Pharmaceuticals 2010 1(1):30-32

Background: The Western ghats, the range of hills running along India's west coast, are well known for their rich and unique assemblage of flora and fauna. The present study was performed to evaluate the insecticidal potential of Actinomycetes isolated from the soils of the Western ghats of Agumbe, Karnataka. Methods: For isolation, the serially diluted soil sample was plated on Starch casein agar and incubated aerobically. The actinomycete isolates were identified by various parameters such as colony morphology, spore arrangement, staining, and biochemical reactions. The isolates were grown in Starch casein broth for seven days, the culture broth was extracted with butanol solvent and concentrated to get crude extract. Insecticidal activity of different concentrations of butanol extract of the isolates was determined against the second instar larvae of Aedes aegypti. The larvicidal effect, in terms of mortality of larvae, of the extracts was determined by counting the number of dead larvae after 24 hours. Results: Two actinomycete isolates were recovered from the soil sample and were identified as the species of Streptomyces on the basis of phenotypic, microscopic, biochemical, and staining characteristics. The colonies of the Streptomyces isolate 1 were creamish-white with yellow pigmentation and the spore arrangement was straight, whereas colonies of the Streptomyces isolate 2 were light grey with dark green pigmentation. The spore arrangement in isolate 2 was of the open loop type. Both the isolates were Gram-positive, non-acid fast, and caused hydrolysis of starch and casein. The insecticidal activity of different concentrations, namely 1.0, 2.5, and 5.0 mg/ml, of butanol extract of the Streptomyces isolates was tested against the second instar larvae of Aedes aegypti. The insecticidal potential of butanol extracts, in terms of larval mortality, was found to be dose dependent. Among the isolates, isolate 2 showed a marked insecticidal activity than isolate 1. At a concentration of 5 mg/ml, both the isolates caused 100% mortality of the larvae. At concentrations of 1 and 2.5 mg/ml, isolate 2 exhibited a stronger larvicidal activity than isolate 1. Conclusion: The insecticidal efficacy of the Streptomyces species might be due to the presence of active constituents in the extract. Isolation and characterization of active constituents from the butanol extract possessing insecticidal potential are to be investigated.

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