scholarly journals Two New Ramulosin Derivatives from the Entomogenous Fungus Truncatella angustata

2015 ◽  
Vol 10 (2) ◽  
pp. 1934578X1501000
Author(s):  
Shenxi Chen ◽  
Zhuowei Zhang ◽  
Li Li ◽  
Xingzhong Liu ◽  
Fengxia Ren

Two new ramulosin derivatives, 7α-hydroxy-8-dihydroramulosin (1) and 7-ketoramulosin (2), along with three known metabolites, (+)-ramulosin (3), 6-hydroxyramulosin (4), and 8-dihydroramulosin (5), were isolated from the crude extract of Truncatella angustata, an entomogenous fungus isolated from the Septobasidium-infected insect Aspidiotus sp. The structures of 1 and 2 were elucidated by nuclear magnetic resonance experiments, and 1 was further confirmed by X-ray crystallography. The absolute configuration of 1 was assigned by single-crystal X-ray diffraction analysis using Cu K α radiation, whereas that of 2 was determined by electronic circular dichroism (ECD) calculations. Compounds 1–5 were tested for cytotoxicity against four human carcinoma cell lines, HeLa, A549, MCF-7, and T24. Compound 4 showed weak cytotoxic effects against A549 and T24.

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 475 ◽  
Author(s):  
Elbanna ◽  
Khalil ◽  
Bernhardt ◽  
Capon

Chemical analysis of a cultivation of an Australian Mugil mullet gastrointestinal tract (GIT) derived fungus, Scopulariopsis sp. CMB-F458, yielded the known lipodepsipeptides scopularides A (1) and B (2). A comparative global natural product social (GNPS) molecular networking analysis of ×63 co-isolated fungi, detected two additional fungi producing new scopularides, with Beauveria sp. CMB-F585 yielding scopularides C–G (3–7) and Scopulariopsis sp. CMB-F115 yielding scopularide H (8). Structures inclusive of absolute configurations were assigned by detailed spectroscopic and C3 Marfey’s analysis, together with X-ray analyses of 3 and 8, and biosynthetic considerations. Scopularides A–H (1–8) did not exhibit significant growth inhibitory activity against a selection of Gram positive (+ve) and negative (−ve) bacteria, a fungus, or a panel of three human carcinoma cell lines.


2016 ◽  
Vol 52 (66) ◽  
pp. 10151-10154 ◽  
Author(s):  
Fabian Schneider ◽  
Tiankun Zhao ◽  
Thomas Huhn

A series of novel Zr(iv)salan complexes is reported. The initial metalation product[(L1)2Zr]is highly water sensitive whereas ligand exchanged[L1Zr(dipic)]hydrolyses rather slowly with a bis-hydroxo Zr(iv) species identified by MS as an intermediate.[L1Zr(dipic)]is cytotoxic in the range of cisplatin against two human carcinoma cell lines.


2014 ◽  
Vol 9 (5) ◽  
pp. 1934578X1400900
Author(s):  
Manyun Su ◽  
Shenxi Chen ◽  
Xingzhong Liu ◽  
Yuehu Pei

Three new polyketides, trichocladinols I-K (1-3) with oxabicyclic (1 and 3) and oxatricyclic (2) skeletons, together with three known metabolites, massarilactone G (4), massarigenin D (5), and rosigenin (6), were isolated from the solid-substrate fermentation cultures of the ascomycete fungus Trichocladium opacum. The structures of the new compounds were elucidated primarily by analysis of NMR data. The absolute configurations of 1-3 were deduced from circular dichroism (CD) data. Compounds 1-3 were tested for cytotoxicity against five human carcinoma cell lines, HeLa, A549, MCF-7, HCT116, and T24. Compound 1 showed a weak cytotoxic effect against HeLa cells, but 2 and 3 were inactive.


2021 ◽  
Vol 16 (10) ◽  
pp. 1934578X2110553
Author(s):  
Jiale Wu ◽  
Jiafeng Wang ◽  
Yinglong Han ◽  
Yu Lin ◽  
Jing Wang ◽  
...  

A series of novel betulin derivatives containing hydrazide-hydrazone moieties were synthesized. All compounds were evaluated for their cytotoxicity against four human carcinoma cell lines (HepG2, A549, MCF-7 and HCT-116) and a normal human gastric epithelial cell line (GES-1). Among them, compound 6i was the most potent against HepG2 and MCF-7 cell lines, with IC50 values of 9.27 and 8.87 μM, respectively. The results suggest that the incorporation of a hydrazide-hydrazone side chain at the C-28 position of betulin is beneficial for compounds to display significant cytotoxicity. Compound 6i may be used as a promising skeleton for antitumor agents with improved efficacy.


2015 ◽  
Vol 44 (37) ◽  
pp. 16475-16485 ◽  
Author(s):  
Tiankun Zhao ◽  
Martin Grützke ◽  
Kathrin H. Götz ◽  
Tetiana Druzhenko ◽  
Thomas Huhn

Two sulfonamide substituted heteroleptic salan titanium(iv)-bis-chelates showed potent anticancer activity better than cisplatin against the human carcinoma cell lines HeLa S3 and Hep G2a.


2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.


2019 ◽  
Vol 16 (6) ◽  
pp. 663-669
Author(s):  
Dan Liu ◽  
Aiqi Xue ◽  
Zhixin Liu ◽  
Yi Zhang ◽  
Penghui Peng ◽  
...  

Background: Three series of new 7-fluoro-4-(1-piperazinyl) quinolines (I1~I6, II1~II2 and IV1~IV4) were synthesized. Their anti-tumor activity was evaluated in vitro against three human carcinoma cell lines, namely SGC-7901 cells, BEL-7402 cells and A549 cells expressing high levels of EGFR by Methyl Thiazolyl Terazolium (MTT) assay. Methods: Three series of quinoline derivatives were synthesized, characterized and evaluated for their in vitro anti-tumor activities. Results and Discussion: Structures of the newly synthesized compounds were confirmed by spectral analysis. The preliminary bioassay indicated that compounds I1, I10 and II1 exhibited better anti-tumor activity than the rest of the target compounds and gefitinib against A549 cell based assay, which demonstrated that compounds I1, I10 and II1 are potential agents for cancer therapy. Results suggested that the substitutes on piperazinyl influenced anti-tumor activities remarkably. Conclusion: These results are useful for discovering more potent novel anti-tumor compounds and further studies are ongoing.


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