73584-64-2Relevant articles and documents
Pentacylic triterpenes from Lavandula coronopifolia: structure related inhibitory activity on α-glucosidase
Elsbaey, Marwa,Mwakalukwa, Rogers,Shimizu, Kuniyoshi,Miyamoto, Tomofumi
, p. 1436 - 1444 (2019/08/26)
Ten pentacyclic triterpenes (1-10) were isolated from Lavandula coronopifolia. We evaluated their α-glucosidase inhibitory activity, and found that the aglycones, 1, 2, 3, 4, 7 and 10 showed superior IC50 values to the positive control. In order to explain the structural requirements for α-glucosidase inhibitory activity, eleven derivatives were prepared, including one new compound, 2-formyl-(A)1–19α-hydroxy-1-norursane-2, 12-dien-28-oic acid 10c. The results demonstrated that a free hydroxyl at ring-A and a free carboxylic group at position 28 are key structural features for the α-glucosidase inhibitory activity, also that an ursane skeleton is optimum for the activity. Additionally, enzyme kinetic analysis of pomolic acid 2, the most potent compound, revealed that it inhibited α-glucosidase in a mixed-type manner. The molecular docking simulation validated this type of inhibition and highlighted the role of the C-3 hydroxyl and C-28 carboxylic groups in interaction with the enzyme in silico.
Application of methylsulfonyl 12-ketone oleanolic acid methyl ester in preparation of medicine for resisting viral hepatitis B
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Paragraph 0029-0030; 0034-0035, (2020/10/30)
The invention relates to application of methylsulfonyl 12-ketone oleanolic acid methyl ester in preparation of a medicine for resisting viral hepatitis B, and particularly provides application of 3 beta-methylsulfonyloxy-12-carbonyl oleanane-28-carboxylic acid methyl ester in preparation of a medicine for preventing and treating hepatitis B virus infection diseases. The compound has remarkable activity of inhibiting HBsAg and HBeAg secreted by HepG2.2.15 cells. On the eighth day, the intensity of the compound at a concentration of 100 micrograms/milliliter for inhibiting the HBeAg secretion ishigher than that of positive control drugs alpha-interferon and lamivudine. The HBsAg secretion inhibition strength of the compound is 69.9% at the concentration, and the inhibition rate on HBV-DNA replication is higher than 97%. The above results show that the methylsulfonyl 12-ketone oleanolic acid methyl ester can be expected to be used for preparing non-nucleoside drugs for treating hepatitisB virus infection diseases. Specifically, the compound has the application for preparing an HBV-DNA inhibitor, an HBsAg inhibitor and an HBeAg inhibitor; and the preparation method is simple in steps, low in cost, wide in raw material source and easy for industrial production.
Medicinal application of 12-ketone methyl oleanolate in preparation of anti-viral hepatitis B medicine
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Paragraph 0032; 0033, (2020/11/23)
The invention relates to medicinal application of 12-ketone methyl oleanolate in preparation of anti-viral hepatitis B medicines and particularly provides application of 3beta-hydroxyl-12-carbonyl oleanolate-28-methyl carboxylate in preparation of medicines for preventing and treating hepatitis B viral infectious diseases. The compound has remarkable activity of inhibiting HBsAg and HBeAg secreted from HepG2.2.15 cells, the strength of the compound on inhibiting secretion of HBsAg and HBeAg are respectively 89.1 percent and 95.1 percent under the concentration of 100mg/ml on the 8th day, replication of the compound on HBV-DNA can show the inhibition rate of 92.6 percent under the concentration of 100mg/ml, which is higher than that of positive medicines alpha-interferon. Thus, the 12-ketone methyl oleanolate is expected to be applied to preparation of non-nucleoside drugs for treating hepatitis B viral infectious diseases, especially applied to preparation of HBV-DNA inhibitors, HBsAginhibitors and HBeAg inhibitors. The preparation method has simple steps and low cost, is wide in raw material sources and is easy for industrial production.
