| Morinda plantation is the Guangdong authentic herbs,with obvious regional characteristics,are widely used for the treatment of sexual impotence,spermatorrhea,female infertility,cold dampness,rheumatoid and so on.However,the research on Morinda officinalis has focused on the pharmacological effects,the main chemical composition and the processing technology,few studies on the diversity of endophytic fungi and secondary metabolites have been reported so far.Endophytic fungi of plants are promising sources of a variety of bioactive metabolites.In the process of co-evolution with the host,the endophytes not only can produce the same or similar secondary metabolites with host plant,but also produce other potential value of secondary metabolites in medicinal field.The various natural products from endophytic fungi has become a new hotspot in the study of medicinal plant resources.This paper got 28 strains of endophytic fungi from different parts of Morinda officinalis which was collected from Gaoyao city,Guangdong province,in January 2015.Each strain was cultured by a small amount of liquid fermentation to get the broth extract.By screening the TLC plate,cytotoxicity and antibacterial activity we found the crude extracts of Alternaria sp.A744 and Penicillium sp.A735 showed excellent activities against four tumor cell lines,including MCF-7,HepG-2,NCI-H460 and SF-268.The result of in vitro cytotoxic showed the growth rate 95.53%?86.14%?92.02%?95.50% and 85.70%?91.44%?93.08%?86.86% in the concentration 10 ?g/m L,with the positive control cisplatin were 65.55%?85.64%?86.70%?82.81%,respectively.Simultaneously,the Endophytic fungal stains Alternaria sp.A744 and Penicillium sp.A735 showed significant inhibitory effects on staphylococcus aureus and bacillus subtilis,with MIC was 0.39,1.56 mg/m L and 0.78,0.39 mg/mL.The stain Alternaria sp.A744 showed obviously inhibitory activity against Candida albicans,Aspergillus niger,Aspergillus flavus and Trichoderma viride,with the bacteriostatic diameter were 9,11,10 and 10 mm,with the positive control nystatin were 30?35?20 ? 25 mm,respectively.23 compounds were isolated from the fermentation extracts of stains Alternaria sp.A744 and Penicillium sp.A735 by repeated colum chromatography(CC),RP-18,Sephadex LH-20 gel,HPLC,as well as by preparative thin layer chromatography(PTLC),recrystallization and so on.The structures of these compounds were elucidated by means of spectroscopic techniques,including(1H-NMR?13C-NMR?COSY?HMQC?HMBC)together with MS?IR?UV?CD as well as chemical method.Totally,23 compounds were structures elucidated,16 compounds were isolated from A744 and identified as isobenzofuranone A(1)and indandione B(2),isosclerone(3),2,4,8-trihydroxy-1-tetralone(4),3,4-dihydro-3,4,8-trihydroxy-1[2H]-naphthalenone(5),6-hydroxyisosclerone(6),cis-4-hydroxyscytalone(7),alternariol-4-methyl ether(8),6-epi-stemphytriol(9),dihydroalterperylenol(10),alterperylenol(11),altertoxin II(12),stemphyperylenol(13),dibutyl phthalate(14),?-acetylcholine(15),p-hydroxybenzoic acid(16);7 compounds were isolated from A735 and identified as penicillic acid(17),2,5-dihydroxyphenylacetic acid methyl ester(18),5-hydroxymethylfurfural(19),Protocatechuic acid(20),3,4-dihydroxybenzyl alcohol(21),2,5-dihydroxyphenylacetic acid(22),curvulinic acid(23).Compounds 1-2 were isolated from Alternaria sp.A744 for the first time.Simultaneously,compounds 1-16 were evaluated for their cytotoxic and ?-glucosidase inhibitory activities,the new compounds showed no obvious activities.The known compounds 9?11 and 12 showed significant inhibitory activities against four tumor cell lines with IC50 values in the range of 1.92-9.62 ?M,while the positive control cisplatin was 3.09,1.39,2.43 and 2.37 ?M,respectively.Compounds 4,5,9,10,12,13 and 14 showed excellent inhibitory activity against ?-glucosidase with IC50 values in the range of 12.05-166.13 ?M,being obviously stronger than the positive control Acarbose(an oral antidiabetic agent,IC50 = 427.34?12.03 ?M). |
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