scholarly journals Circumdatin-Aspyrone Conjugates from the Coral-Associated Aspergillus ochraceus LCJ11-102

Marine Drugs ◽  
2019 ◽  
Vol 17 (7) ◽  
pp. 400 ◽  
Author(s):  
Yaqin Fan ◽  
Yalin Zhou ◽  
Yuqi Du ◽  
Yi Wang ◽  
Peng Fu ◽  
...  

Ochrazepines A−D (1−4), four new conjugates dimerized from 2-hydroxycircumdatin C (5) and aspyrone (6) by a nucleophilic addition to epoxide, were isolated from the fermentation broth of the coral-associated Aspergillus ochraceus strain LCJ11-102. Their structures including absolute configurations were determined based on spectroscopic analysis and chemical methods. Compounds 1−4 were also obtained by the semisynthesis from a nucleophilic addition of 2-hydroxycircumdatin C (5) to aspyrone (6). New compound 1 exhibited cytotoxic activity against 10 human cancer cell lines while new compounds 2 and 4 selectively inhibited U251 (human glioblastoma cell line) and compound 3 was active against A673 (human rhabdomyoma cell line), U87 (human glioblastoma cell line), and Hep3B (human liver cancer cell line) with IC50 (half maximal inhibitory concentration) values of 2.5–11.3 μM among 26 tested human cancer cell lines.

2011 ◽  
Vol 66 (3-4) ◽  
pp. 143-148 ◽  
Author(s):  
Hossam M. Abdallah ◽  
Shahira M. Ezzat

The aerial parts of Pituranthos tortuosus (Desf.) Benth and Hook (Apiaceae), growing wild in Egypt, yielded 0.8%, 0.6%, and 1.5% (v/w) of essential oil when prepared by hydrodistillation (HD), simultaneous hydrodistillation-solvent (n-pentane) extraction (Lickens- Nickerson, DE), and conventional volatile solvent extraction (preparation of the “absolute”, SE), respectively. GC-MS analysis showed that the major components in the HD sample were β-myrcene (18.81%), sabinene (18.49%), trans-iso-elemicin (12.90%), and terpinen- 4-ol (8.09%); those predominent in the DE sample were terpinen-4-ol (29.65%), sabinene (7.38%), γ-terpinene (7.27%), and β-myrcene (5.53%); while the prominent ones in the SE sample were terpinen-4-ol (15.40%), dill apiol (7.90%), and allo-ocimene (4E,6Z) (6.00%). The oil prepared in each case was tested for its cytotoxic activity on three human cancer cell lines, i.e. liver cancer cell line (HEPG2), colon cancer cell line (HCT116), and breast cancer cell line (MCF7). The DE sample showed the most potent activity against the three human cancer cell lines (with IC50 values of 1.67, 1.34, and 3.38 μg/ml against the liver, colon, and breast cancer cell lines, respectively). Terpinen-4-ol, sabinene, γ-terpinene, and β-myrcene were isolated from the DE sample and subjected to a similar evaluation of cytotoxic potency; signifi cant activity was observed


2008 ◽  
Vol 7 (5) ◽  
pp. 699-708 ◽  
Author(s):  
Hanna Berglind ◽  
Yudi Pawitan ◽  
Shunsuke Kato ◽  
Chikashi Ishioka ◽  
Thierry Soussi

2010 ◽  
Vol 2 (3) ◽  
pp. 139-151 ◽  
Author(s):  
Makoto Takeuchi ◽  
Toshiya Inoue ◽  
Takeshi Otani ◽  
Fumiyuki Yamasaki ◽  
Shuji Nakamura ◽  
...  

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1986066
Author(s):  
Cheng-Ting Zi ◽  
Liu Yang ◽  
Bang-Lei Zhang ◽  
Yan Li ◽  
Zhong-Tao Ding ◽  
...  

Novel podophyllotoxin xyloside derivatives 8 to 11 were synthesized and evaluated for their cytotoxicities against a panel of 5 human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, SW480) using [3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide] assays. These derivatives showed good to moderate activities, with compound 9 having an IC50 value of 4.42 μM against the A-549 cell line. Overall, compound 9 might be a promising candidate for further development.


2016 ◽  
Vol 14 (26) ◽  
pp. 6304-6315 ◽  
Author(s):  
Trieu N. Trinh ◽  
Eileen A. McLaughlin ◽  
Mohammed K. Abdel-Hamid ◽  
Christopher P. Gordon ◽  
Ilana R. Bernstein ◽  
...  

A series of quinolone-2-(1H)-ones derived from a Ugi-Knoevenagel three- and four-component reaction were prepared exhibiting low micromolar cytotoxicity against a panel of eight human cancer cell lines known to possess the Hedgehog Signalling Pathway (HSP) components, as well as the seminoma TCAM-2 cell line.


2021 ◽  
Vol 22 (15) ◽  
pp. 7798
Author(s):  
Elena G. Varlamova ◽  
Mikhail V. Goltyaev ◽  
Valentina N. Mal’tseva ◽  
Egor A. Turovsky ◽  
Ruslan M. Sarimov ◽  
...  

In recent decades, studies on the functional features of Se nanoparticles (SeNP) have gained great popularity due to their high biocompatibility, stability, and pronounced selectivity. A large number of works prove the anticarcinogenic effect of SeNP. In this work, the molecular mechanisms regulating the cytotoxic effects of SeNP, obtained by laser ablation, were studied by the example of four human cancer cell lines: A-172 (glioblastoma), Caco-2, (colorectal adenocarcinoma), DU-145 (prostate carcinoma), MCF-7 (breast adenocarcinoma). It was found that SeNP had different concentration-dependent effects on cancer cells of the four studied human lines. SeNP at concentrations of less than 1 μg/mL had no cytotoxic effect on the studied cancer cells, with the exception of the A-172 cell line, for which 0.5 μg/mL SeNP was the minimum concentration affecting its metabolic activity. It was shown that SeNP concentration-dependently caused cancer cell apoptosis, but not necrosis. In addition, it was found that SeNP enhanced the expression of pro-apoptotic genes in almost all cancer cell lines, with the exception of Caco-2 and activated various pathways of adaptive and pro-apoptotic signaling pathways of UPR. Different effects of SeNP on the expression of ER-resident selenoproteins and selenium-containing glutathione peroxidases and thioredoxin reductases, depending on the cell line, were established. In addition, SeNP triggered Ca2+ signals in all investigated cancer cell lines. Different sensitivity of cancer cell lines to SeNP can determine the induction of the process of apoptosis in them through regulation of the Ca2+ signaling system, mechanisms of ER stress, and activation of various expression patterns of genes encoding pro-apoptotic proteins.


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