Malotilate

Description

Malotilate is a hepatoprotective agent reported to be effective in the treatment of cirrhosis, chronic hepatitis and similar liver disorders. It appears to improve hepatic function by increasing blood and bile flow and improving protein synthesis.

Description

Malotilate is a hepatoprotective agent. It inhibits A23187-induced metabolism of arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) to the 5-lipoxygenase (5-LO) metabolites leukotriene B₄ (LTB₄; ) and 5-HETE in macrophages isolated from the ascitic fluid of patients with alcoholic liver cirrhosis. Malotilate (50 mg/kg) prevents increases in plasma glutamic-pyruvic transaminase (GPT) and glutamic-oxaloacetic transaminase (GOT) activities in a rat model of carbon tetrachloride-induced liver injury. It reduces hepatic deposition of type III procollagen, type IV collagen, laminin, and fibronectin in a rat model of dimethylnitrosamine-induced hepatic fibrosis when administered at a dose of 100 mg/kg.

Originator

Nihon Nohyaku (Japan)

Definition

ChEBI: Malotilate is an isopropyl ester.

brand name

KANTEC

in vitro

the in-vitro invasion assay employing a rat lung endothelial cell monolayer indicated that pretreatment of the lung endothelial cells, but not c-sst-2 cells, with malotilate reduced the invasion of the rle monolayer by c-sst-2 cells significantly. the in-vitro vascular permeability assay also demonstrated malotilate could prevent the permeability increase of the lung endothelial cell monolayer by serum starvation. in contrast, the gelatinase production and adhesion to the rle cell monolayer of c-sst-2 cells were not affected by malotilate treatment [1].

in vivo

malotilate was administered to syngeneic shr rats orally from 7 days before or after s.c. inoculation of c-sst-2 cells until the end of the experiments. in the malotilate-treated rats, pulmonary metastasis was suppressed markedly when compared with the non-treated rats. moreover, in the rats treated with malotilate for 19 days after inoculation of c-sst-2 cells, lung metastasis was also suppressed significantly [1].

References

[1] nagayasu h,hamada j,kawano t,konaka s,nakata d,shibata t,arisue m,hosokawa m,takeichi n,moriuchi t. inhibitory effects of malotilate on invasion and metastasis of rat mammary carcinoma cells by modifying the functions of vascular endothelial cells. br j cancer.1998 may;77(9):1371-7.
[2] takase s,matsuda y,yasuhara m,takada a. effects of malotilate treatment on alcoholic liver disease. alcohol.1989 may-jun;6(3):219-22.