A Cytotoxic Principle of Tamarindus indica, Di-w-butyl Malate and the Structure-Activity Relationship of Its Analogues

1996 ◽  
Vol 51 (3-4) ◽  
pp. 233-242 ◽  
Author(s):  
Akio Kobayashi ◽  
Mohd Ilham Adenarr ◽  
Shin-ichiro Kajiyama ◽  
Hiroshi Kanzaki ◽  
Kazuyoshi Kawazu

Abstract Bioassay-guided fractionation of the methanolic extract of Tamarindus indica fruits led to the isolation of L -(-)-di-nbutyl malate which exhibited a pronounced cytotoxic activity against sea urchin embryo cells. In order to study structure-activity relationships, close-structure relatives of di-n-butyl malate were synthesized using d -(+) -and L -(-)-malic acid as starting materials, and their cytotoxic activities were exam in ed for the sea urchin em bryo assay. L -(-)-D i-n-pentyl malate was the most effective inhibitor to the development of the fertilized eggs. Significant inhibitory activity was not seen in the esters of D -(-)-isomer .

1982 ◽  
Vol 21 (1-3) ◽  
pp. 79-85 ◽  
Author(s):  
MICHIKO WATANABE ◽  
DONALD R. BERTOLINI ◽  
J. RANDOLPH SCHNTTMAN ◽  
ROBERT S. TURNER

2000 ◽  
Vol 53 (12) ◽  
pp. 909 ◽  
Author(s):  
Yoshikazu Hiraga ◽  
Mariko Ago ◽  
Munetaka Tokumasu ◽  
Ken Kaku ◽  
Katsuo Ohkata

Analogues of hippospongic acid A, which inhibit the gastrulation of sea urchin embryos, were synthesized. From a study on structure—activity relationships, the conjugated carboxylic acid moiety was found to be an essential feature for biological activity.


2001 ◽  
Vol 20 (3) ◽  
pp. 589-596 ◽  
Author(s):  
Isabelle Moubax ◽  
Nathalie Bontemps-Subielos ◽  
Bernard Banaigs ◽  
Georges Combaut ◽  
Philippe Huitorel ◽  
...  

2008 ◽  
Vol 3 (11) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Marcel T. Bayor ◽  
John S. K. Ayim ◽  
Gemma Marston ◽  
Roger M. Phillips ◽  
Steven D. Shnyder ◽  
...  

Croton membranaceus is used by herbalists and traditional healers in Ghana for the management of various cancers, especially prostate cancers. A methanolic extract of the roots showed cytotoxic activities against two cancer cell lines, and bioassay-guided fractionation of this extract revealed that the cytotoxic activity resided mostly in the ethyl acetate fraction. Six compounds were isolated from this fraction, including a new furano-clerodane diterpenoid (1), for which the trivial name crotomembranafuran is suggested. This compound exhibited an IC50 value of 4.1 μg/mL (10.6 μM) against human prostate (PC-3) cells, providing some support for the traditional use of C. membranaceus in the treatment of cancers.


2011 ◽  
Vol 344 (11) ◽  
pp. 703-709 ◽  
Author(s):  
Hamid Khaledi ◽  
Abeer A. Alhadi ◽  
Wagee A. Yehye ◽  
Hapipah Mohd Ali ◽  
Mahmood A. Abdulla ◽  
...  

2010 ◽  
Vol 5 (12) ◽  
pp. 1934578X1000501 ◽  
Author(s):  
Mary H. Grace ◽  
Carmen Lategan ◽  
Flaubert Mbeunkui ◽  
Rocky Graziose ◽  
Peter J. Smith ◽  
...  

The hexane extract from the leaves of Canella winterana exhibited strong activity against the chloroquine sensitive (CQS) strain of Plasmodium falciparum (D10) in vitro (IC50 2.53 μg/mL). Bioassay guided fractionation of this extract has led to the isolation of 5 drimane-type sesquiterpenoids: 9-epideoxymuzigadial, 9-deoxymuzigadial, muzigadial, 3-β-acetoxypolygodial and the newly isolated hemiacetal, named muzigodiol, with IC50-values of 1.01, 2.19, 0.31, 2.77 and 7.43 μg/mL, respectively. The first four compounds were tested for their cytotoxicity using Chinese Hamster Ovarian (CHO) cells, where they showed IC50-values of 1.82, 33.69, 1.18, and 58.31 μg/mL, respectively. A structure-activity relationship is discussed.


Author(s):  
Isabelle Moubax ◽  
Nathalie Bontemps-Subielos ◽  
Bernard Banaigs ◽  
Georges Combaut ◽  
Philippe Huitorel ◽  
...  

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