Bulk Malotilate Raw Materials Powder

CAS:59937-28-9

MF:C12H16O4S2

MW:288.38 

EINECS:261-987-3

Specification: 99% min Malotilate Powder

Sample: Malotilate Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Malotilate Powder Usage and Synthesis.

Malotilate inhibits pulmonary metastases and lung metastases in rats. In rat liver, Malotilate prevented the increase in serum markers of collagen type III and IV synthesis and the accumulation of collagen, laminin and fibronectin. In rat liver, the combination of Malotilate and carbon tetrachloride significantly reduced hydroxyproline accumulation, hepatic prolyl 4-hydroxylase and hepatic and serum galactosylhydroxylysylglucosyltransferase activities.Malotilate also prevented morphologic changes such as focal necrosis, fatty infiltration, and inflammation in rat liver. Malotilate also normalised almost completely standard liver function tests. In rat liver microsomes, Malotilate decreased CYP2E1 levels and increased CYP2B1 levels, while CYP1A expression was unchanged.

Uses and functions of Malotilate.

Hepatic protein metabolism improvement drug. It can activate liver function and inhibit the progress of liver fibrosis. It is suitable for the treatment of chronic hepatitis, liver cirrhosis in the compensatory stage and advanced schistosomiasis-induced cirrhosis with hypoproteinaemia, etc.

Hepatitis adjuvant, used for the improvement of liver function in compensated cirrhosis

Malotilate acts on hepatocytes, promotes RNA synthesis, activates ribosomes and improves protein synthesis, thus activating liver function and inhibiting the progress of liver fibrosis.

Experiments with carbon tetrachloride cirrhosis rat model, found that the product on the serum total protein, albumin, cholinesterase activity and low total liver protein have improved; on the serum aminotransferase activity rise, serum total cholesterol is low, have the effect of restoring it to normal.

Malotilate can also inhibit the increase in the amount of 4-hydroxyproline (an indicator of collagen fibres) in the liver, and pathological histology has also proved that the product improves the proliferation of connective tissue and fibre formation.

Malotilate can improve lipid metabolism and reduce hepatic lipid peroxidation in rats with fatty liver caused by carbon tetrachloride and ethylthionine. It is suitable for the improvement of liver function in compensated cirrhosis.

Pharmacological Effects of Malotilate.

Malotilate has an ameliorating effect on the low levels of total plasma protein, albumin, cholinesterase activity and total hepatic protein after oral administration, and it can normalise the increase in serum aminotransferase activity and the low level of total plasma cholesterol.

Malotilate acts on hepatocytes, promotes ribonucleic acid (RNA) synthesis, activates ribosomes and improves protein synthesis, thus activating liver function and inhibiting the progression of hepatic fibrosis, and improves hepatic protein metabolism, accompanied by the improvement of aminotransferase, gliadin and gamma-globulin. It is suitable for the improvement of liver function in compensated cirrhosis.

It is also used clinically for hypoproteinaemia caused by chronic hepatitis and cirrhosis.

Production method of Malotilate Powder

Method 1: 44.4g (0.2mo1) 1,3-dithiomo-2-thione-4,5-dicarboxylic acid was dissolved in 240ml nitromethane and heated to 80℃. Then 100 ml of iodomethane was added slowly and dropwise, and reflux was continued for 6 h. At the end of the reaction, the crystals formed were collected by filtration, washed with 100 ml of ether, and dried in air to give 48.4 g of 2-methylsulfanyl.1,3-dithiomo-2-thiophenone iodide with melting point of 114-116°C (decomposition) in 87.0% yield.1.1 g (0.03mo1) of 69% sodium hydride was suspended in 30 ml of tetrahydrofuran and 5.6 g (0.03mo1) of diisopropyl malonate was added slowly dropwise under cooling in an ice bath. When no hydrogen escaped, 8.2g (0.03mo1) of iodide obtained above was added and refluxed for 1 h. The reaction solution was poured into a large amount of ice water, the crystals formed were collected by filtration, dried, and recrystallised with n-hexane to give 6.7g of white malonate crystals with melting point of 59-60°C and yield of 77.5%.

Method 2: Diisopropyl malonate and carbon disulfide were reacted in dimethyl sulfoxide in the presence of potassium hydroxide. The product obtained and 1,1,1-trichloroethane, reacted in the presence of potassium hydroxide to obtain malotilate.