Study On The Metabolites Produced By Four Marine Mangrove Endophytic Fungi

The special living environment and unique metabolic pathway of the marine microbe result in the great diversity of their metabolites, which are the resources of pharmaceutical lead compounds. In this paper, the metabolites of the mangrove endophytic fungus Penicillium sp. V11, Phoma sp. L28 produced by single-strain culture and Phomopsis sp. K38 and Alternaria sp. E33 produced by co-culture were studied. The structures of the isolated compounds were established by comprehensive spectroscopic analyses and comparison with the published data. The antifungal activity, cytotoxicity activity, phytotoxicity activity of some compounds were tested. The results were summarized as follows.1. 28 compunds were isolated from the metabolites of the four fungus, they were identified as: penochalasin J(1), penochalasin I(2), o-hydroxyacetanilide(3),chaetoglobosin G(4), chaetoglobosin F(5), chaetoglobosin C(6), chaetoglobosin J(7),chaetoglobosin A(8), chaetoglobosin E(9), chaetoglobosin D(10), armochaetoglobin I(11),cytoglobosins C(12), 7-(?, ?)-dimethylallyloxy macrosporin(13), diisobutyl ether(14), N,N'-dicyclohexylurea(15), dibutyl phthalate(16), macrosporin(17), 7-methoxy macrosporin(18), p-hydroxybenzoic acid(19), ergosterol peroxide(20), 9, 11-dehydroergosterol peroxide(21), L-arabinitol(22), 1, 3-indandione(23), tetrahydroaltersolanol B(24),altersolanol L(25), ampelanol(26), cyclo(D-Pro-L-Tyr-L-Pro-L-Tyr)(27), cyclo(Gly-L-Phe-L-Pro-L-Tyr)(28). Compounds 1, 2, 13, 27, 28 were reported for the first time,and compounds 13, 17, 18, 24, 25, 26 were first found in Phoma sp.. Compund 2 has an unprecedented 6/5/6/5/6/13 six cyclic system, which is the first example of chaetoglobosins with this kind of skeleton. It is of great theoretical significance.2. The antifungal activity of some compunds were proformed by the paper dis-agardiffusion assay and the broth dilution method. The following six phytopathogenic fungi were used for bioassay: Colletotrichum musae, Colletotrichum gloeosporioides, Fusarium graminearum, Penicillium italicum, Fusarium oxysporum, Rhizoctonia solani. The tested compunds exhibited singificant antifungal activity against more than two fungal among the six, except of compunds 2, 13, 18, 24 and 25. Moreover compounds 1, 8, 11, 17 showed highly sensitive to some fungal with MICs < 6.25 ?g/m L, which were even better than the positive control carbendazim. These compounds have the potential to be agricultural antibiotics.3. The cytotoxicity activity of compunds 1, 2, 4-6, 8, 9, 11, 12 against three human tumor cell lines including a human breast cancer cell line(MCF-7) and a human gastric cancer cell line(SGC-7901) and a human lung adenocarcinoma epithelial cell line(A549)were tested by MTT method. Most of the compunds exhibited moderate cytotoxicity activity except compunds 9, 11; compunds 2, 8, 12 showed important cytotoxicity aganist two of the three cancer cell lines, with IC50 < 10 ?M. These compounds can be further studied as the lead comounds of antitumor and become potential antitumor durgs. The cytotoxicity of these compounds against MDA-MB-435, A549 and SGC-7901 cell lines were first report in this paper, except 11, 12 against A549.4. The phytotoxicity activity of the compunds 1, 2, 5-10, 12 against seeds of Brassica chinensis L., and Brassica campestris L. ssp. were studied by seed germination mothed.Compunds 6, 9, 12 showed the inhibition rate over 80 % to both of the seeds in Brassica chinensis L., Brassica campestris L. ssp. and these compounds can be developed as herbicides.In conclusion, five new compunds were isolated and identificated from the metabolites,along with some activities of some compounds were recovered, which provide basic information for the further research.