Metabolites from mangrove endophytic fungus Dothiorella sp.

Mangroves are special woody plant communities in the intertidal zone of tropical and subtropical coasts. They prove to be a natural microorganisms and new metabolites storage. In the study of mangrove endophytic fungi metabolites, four new compounds, Compounds 1, 2, 3 and 4, as well as a known octaketide, oytosporone B (5), are isolated from an endophytic fungus, Dothiorella sp., HTF3. They all show cytotoxic activities. The elucidation of these structures is mainly based on 1D/ 2D NMR and ESI-MS spectral analyses.

Secondary Metabolites from the Endophytic Fungus Xylaria sp.hg1009

A detailed chemical investigation of the secondary metabolites produced by the endophytic fungus Xylaria sp.isolated from the stems of Isodon sculponeatus afforded six new compounds,xylariahgins A-F(1-6),two new natural products(7 and 8),along with two known compounds(9 and 10)(Fig.1).The structures of all compounds were unambiguously established by analyzing their spectroscopic data or referring to pertinent literature.Compounds 1-8 were tested for their cytotoxic activity against five human tumor cell lines.

中国南海海岸红树真菌Xylaria sp.代谢产物在体外对乙酰胆碱酯酶活性的影响

目的 :体外研究中国南海海岸红树林真菌Xylariasp 代谢产物XyloketalA～D对乙酰胆碱酯酶(AChE)活性的影响。方法 :采用改良Ellmen法测定AChE活性 ,考察受试化合物在体外对AChE活性及其酶动力学特征的影响 ,并就这些化合物对AChE和丁酰胆碱酯酶 (BuChE)的选择性进行比较。结果 :xyloketalA～D在体外对AChE活性均有不同程度的抑制作用 ,并呈一定剂量依赖关系 ,IC50 值分别为 2 9 9、137 4、10 9 3和 4 2 5 6μmol/L。通过对AChE酶抑制动力学曲线进行分析发现 ,xyloketals对AChE的抑制表现为可逆非竞争性抑制。此外 ,对于另一种胆碱酯酶BuChE ,阳性药维那克林及xyloketals均表现出一定降低作用 ,但相对而言xyloketals对AChE的选择性较强。结论 :xlylketals在体外对AChE活性有可逆非竞争性抑制作用 ,表明该类化合物可能作为抗早老性痴呆 (AD)药物进行开发 ,同时该结果亦提示 。

Griseofulvin enantiomers and bromine-containing griseofulvin derivatives with antifungal activity produced by the mangrove endophytic fungus Nigrospora sp.QQYB1

Marine microorganisms have long been recognized as potential sources for drug discovery.Griseofulvin was one of the first antifungal natural products and has been used as an antifungal agent for decades.In this study,12 new griseofulvin derivatives[(±)-1-2,(+)-3,(±)-4,10-12,and 14-15]and two new griseofulvin natural products(9 and 16)together with six known analogues[(-)-3,5-8,and 13]were isolated from the mangrove-derived fungus Nigrospora sp.QQYB1 treated with 0.3%NaCl or 2%NaBr in rice solid medium.Their 2D structures and absolute configurations were established by extensive spectroscopic analysis(1D and 2D NMR,HRESIMS),ECD spectra,computational calculation,DP4+analysis,and X-ray single-crystal diffraction.Compounds 1-4 represent the first griseofulvin enantiomers with four absolute configurations(2S,6'S;2R,6'R;2S,6'R;2R,6'S),and compounds 9-12 represent the first successful production of brominated griseofulvin derivatives from fungi via the addition of NaBr to the culture medium.In the antifungal assays,compounds 6 and 9 demonstrated significant inhibitory activities against the fungi Colletotrichum truncatum,Microsporum gypseum,and Trichophyton mentagrophyte with inhibition zones varying between 28 and 41 mm(10μg/disc).The structure-activity relationship(SAR)was analyzed,which showed that substituents at C-6,C-7,C-6'and the positions of the carbonyl and double bond of griseofulvin derivatives significantly affected the antifungal activity.

(+)/(-)-Mycosphatide A,a pair of highly oxidized polyketides with lipid-lowering activity from the mangrove endophytic fungus Mycosphaerella sp.SYSU-DZG01

(±)-Mycosphatide A(1a/1b),a pair of highly oxidized enantiomeric polyketides featuring a unique5/5/6/5-fused tetracyclic ring system,were isolated from the mangrove endophytic fungus Mycosphaerella sp.SYSU-DZG01.Their structures were established by extensive spectroscopic analyses,single crystal Xray diffraction,and experimental electronic circular dichroism(ECD)spectra comparison.The plausible biosynthetic pathway of 1 was proposed,which involved the generation of a key spiro[4.5]decane scaffold.Compounds(+)-1a and(-)-1b exhibited significant lipid-lowering activity in 3T3-L1 adipocytes model,with EC50values of 7.85±1.56 and 8.87±0.80μmol/L,respectively.

Two new diterpenoids from the endophytic fungus Trichoderma sp.Xy24 isolated from mangrove plant Xylocarpus granatum

Two new harziane diterpenoids, named（9R,10R）-dihydro-harzianone（1） and harzianelactone（2）, were isolated from the endophytic fungus Trichoderma sp. Xy24 by using various column chromatography techniques. Their structures were determined on the basis of extensive spectroscopic（HR-ESI-MS, 1D NMR, 2D NMR and CD） analyses. Among them, 1 was the reductive product of harzianone and 2 was the Baeyer–Villiger monooxygenase catalyzed oxidation product of harzianone. Compound 1 exhibited cytotoxic activity against He La and MCF-7 cell lines with IC（50） values of 30.1 μmol/L and 30.7 μmol/L,respectively.

Talaketides A-G,linear polyketides with prostate cancer cytotoxic activity from the mangrove sediment-derived fungus Talaromyces sp.SCSIO 41027

Seven novel linear polyketides,talaketides A-G(1-7),were isolated from the rice media cultures of the mangrove sed-iment-derived fungus Talaromyces sp.SCSIO 41027.Among these,talaketides A-E(1-5)represented unprecedented unsaturated lin-ear polyketides with an epoxy ring structure.The structures,including absolute configurations of these compounds,were elucidated through detailed analyses of nuclear magnetic resonance(NMR)and high-resolution mass spectrometry(HR-MS)data,as well as elec-tronic custom distributors(ECD)calculations.In the cytotoxicity screening against prostate cancer cell lines,talaketide E(5)demon-strated a dose-dependent inhibitory effect on prostate cancer PC-3 cell lines,with an IC50 value of 14.44 μmol·L-1.Moreover,com-pound 5 significantly inhibited the cloning formation of PC-3 cell lines and arrested the cell cycle in S-phase,ultimately inducing ap-optosis.These findings indicate that compound 5 may serve as a promising lead compound for the development of a potential treat-ment for prostate cancer.