Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

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.

1996 ◽  
Vol 16 (1) ◽  
pp. 53-60 ◽  
Author(s):  
Elisa A. Spillare ◽  
Aikou Okamoto ◽  
Koichi Hagiwara ◽  
Douglas J. Demetrick ◽  
Manuel Serrano ◽  
...  

2002 ◽  
Vol 8 (6) ◽  
pp. 333-335
Author(s):  
Marcela López-Cardoso ◽  
Patricia García y García ◽  
Raymundo Cea-Olivares ◽  
María- Luisa Villareal

O-Cholesteryl-O-phenyl-N-phenylphosphoramidate (1) and four organotin (lV) derivatives of the ambidentate O-cholesteryl-O -phenyl phosphorothioate ligand formulated as Me3 SnOSPR’R”(2), Ph3 SnOSPR’R”(3), O(CH2CH2S)2 Sn(n-Bu)OSPR’R”(4), S(CH2CH2S)2 Sn(n-Bu)OSPR’R”(5), (R’ = O-phenyl; R”= O-cholesteryl) were subjected to cytotoxicity screening against KB (nasopharingel carcinoma), OVCAR-5 (ovarium carcinoma) and SQC-1 UlSO (squamous cell cervix carcinoma) cell cultures. The results of the bioassay showed that these compounds possess potent antitumor activities against the studied human carcinoma cell lines.


1991 ◽  
Vol 19 (03n04) ◽  
pp. 207-216 ◽  
Author(s):  
Wu-Lung Wu ◽  
Wen-Liang Chang ◽  
Chia-Fu Chen

Fifteen tanshinone analogues isolated from the chloroform extract of Danshen roots (Salviae Miltiorrhizae Radix) by chromatographic procedures were tested for their cytotoxic activities against KB, Hela, Colo-205 and Hep-2 carcinoma cell lines. Several of them were effective at concentrations below 1 μg/ml concentrations. Tanshinone analogues with either hydroxy substitutions or olefinic feature in ring A demonstrated higher biologic activities. Analysis of structure-activity relationship indicate that the basic requirement for activity is the presence of a furano-o-naphthoquinone in the molecule. Compounds which lack an intact furan ring were found to be inactive. It is suggested that the planar phenanthrene ring of the tanshinones may be essential for interaction with DNA molecule whereas the furano-o-quinone moiety could be responsible for the production of reactive free radicals in the close vicinity of the bases to cause DNA damage.


2009 ◽  
Vol 44 (6) ◽  
pp. 2736-2740 ◽  
Author(s):  
Sau Hing Chan ◽  
Kim Hung Lam ◽  
Chung Hin Chui ◽  
Roberto Gambari ◽  
Marcus Chun Wah Yuen ◽  
...  

2017 ◽  
Vol 111 ◽  
pp. 37-43 ◽  
Author(s):  
V. Kuete ◽  
F.L. Dongmo Mafodong ◽  
I. Celik ◽  
S.A.T. Fobofou ◽  
B.L. Ndontsa ◽  
...  

1996 ◽  
Vol 37 (6) ◽  
pp. 525-530 ◽  
Author(s):  
Y. Kano ◽  
Miyuki Akutsu ◽  
Saburo Tsunoda ◽  
Kenichi Suzuki ◽  
Yasuo Yazawa

2014 ◽  
Vol 4 (1) ◽  
Author(s):  
Kok Kwan Tan ◽  
Tracey D Bradshaw ◽  
Jessica Chu ◽  
Teng Jin Khoo ◽  
Christophe Wiart

Author(s):  
Yasuhiko Kano ◽  
Miyuki Akutsu ◽  
Saburo Tsunoda ◽  
Tohru Izumi ◽  
Hiroyuki Kobayashi ◽  
...  

2019 ◽  
Vol 10 (3) ◽  
pp. 325-337
Author(s):  
Hanan Abd Al-Hay Al-Ashaal

The target of this study is production of glycoalkaloids from cultures of Solanum nigrum var. judaicum Besser. Further, to evaluate their therapeutic effects. S. nigrum var. judaicum leaves were implanted in MS media containing growth regulators for in vitro study. HPLC analyses were applied for qualitative and quantitative determination of glycoalkaloids. Cytotoxic effects against human carcinoma cell lines were evaluated. In addition, antiviral, antioxidant, anti-inflammatory and antiparasitic activities of the formed glycoalkaloids were estimated.  HPLC data indicated the success of in vitro solasodine and solanidine glycosides production. Solasonine represented the highest concentration. Biological assays illustrated that obtained glycoalkaloids exhibited cytotoxic activity against human carcinoma cell lines that may be attributed to free radical scavenging activity (69.98%). Strong antiherps performance was observed (94%). In addition, the glycoalkaloids showed in vitro schistomicidal (IC50 76.4 ppm) and fasciolicidal (IC50 76.6 ppm) activities. In vivo anti-inflammatory assay revealed potent activity against carrageenan induced edema. Glycoalkaloids were formed 2-5 folds that of intact plant pointed to the efficiency of the cultures. The present findings referred to the pronounced biological performance of the produced glycoalkaloids including antiviral, cytotoxic anti-inflammatory and antiparasitic activities. Botanical derived medication from S. nigrum var. judaicum could be accomplished guided with the present data.  


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