45 results about "Flavonolignan" patented technology

The invention relates to application of E ring bromine substituted silybin to preparing glycosidase inhibitors and in particular discloses application of E ring bromine substituted silybin ester-type flavonolignans or pharmaceutical salt thereof to preparing drugs for inhibiting alpha-glycosidase and preventing and treating type II diabetes. The flavonolignans has extremely obvious activity for inhibiting alpha-glycosidase and the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase reaches 77.1% under the condition of 4mcg / ml concentration. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 32 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or pharmaceutical salt thereof can be expected to be applied to preparing glycosidase inhibitors, especially the drugs for preventing and treating type II diabetes.

The invention relates to application of diamine formyl dehydrogenated silybin serving as a medicament for curing viral hepatitis B, in particular to application of a flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents or pharmaceutically acceptable salts thereof in preparation of a medicament for clearing HBsAg and HBeAg and a medicament for inhibiting HBV DNA replication. The flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents has extremely high HBsAg and HBeAg inhibiting activities; when the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents is at a concentration of 20 mu g / ml, the inhibition rates of the HBsAg and the HBeAg are respectively 94.4 percent and 95.7 percent which exceed 5.9 times and 5.7 times those of a positive control alpha-interferon; and simultaneously the inhibition rate of the HBV DNA is 99.7 percent when the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents is at the same concentration, and the inhibition activity of the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents is higher than that of lamivudine and the alpha-interferon. In summary, the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents or the pharmaceutically acceptable salts thereof can be expected for preparing non-nucleoside medicaments for clearing the HBsAg and the HBeAg, inhibiting the HBV DNA replication, and curing the hepatitis B virus infection diseases.

The invention relates to medicinal use of dinitrobenzoylsilybin for preparing a glycosidase inhibitor, in particular discloses use of 3,5-dinitrobenzoyl substituted silybin ester type flavonolignan and pharmaceutically acceptable salts thereof for the preparation of medicaments for inhibiting alpha-glucuroide and controlling type 2 diabetes. The flavonolignan has extremely obvious activity for inhibiting alpha-glucuroide and has the activity strength for inhibiting the alpha-glucuroide of 71.19 percent at the concentration of 40mg / ml, and by measuring median inhibitory concentration, the strength of the flavonolignan for inhibiting the alpha-glucuroide is 9.5 times that of a positive control medicament acarbose. Pharmacodynamic results prove that the flavonolignan or the pharmaceutically acceptable salts thereof can be expectedly used as a glycosidase inhibitor medicament, particularly a medicament for controlling the type 2 diabetes.

The invention relates to application of 4-cinnamoyl chloride substituted silybin to preparing glycosidase inhibitors and in particular discloses application of 4-cinnamoyl chloride substituted silybin ester flavonolignans or pharmaceutical salt thereof to preparing drugs for inhibiting alpha-glycosidase and preventing and treating type II diabetes. The flavonolignans has extremely obvious activity for inhibiting alpha-glycosidase and the intensity of activity of the 40mcg / ml flavonolignans for inhibiting alpha-glycosidase reaches 92.1%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 30 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or pharmaceutical salt thereof can be expected to be applied to preparing glycosidase inhibitors, especially the drugs for preventing and treating type II diabetes.

The invention relates to application of E ring benzyloxy substituted silybin to preparing glycosidase inhibitors and in particular discloses application of E ring benzyloxy substituted silybin ester-type flavonolignans or pharmaceutical salt thereof to preparing drugs for inhibiting alpha-glycosidase and preventing and treating type II diabetes. The flavonolignans has extremely obvious activity for inhibiting alpha-glycosidase and the intensity of activity of the 40mcg / ml flavonolignans for inhibiting alpha-glycosidase reaches 93%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 13 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or pharmaceutical salt thereof can be expected to be applied to preparing glycosidase inhibitors, especially the drugs for preventing and treating type II diabetes.

The invention relates to application of ring B ethyoxyl silybin in preparing medicaments for treating viral hepatitis B, in particular to application of ring B ethyoxyl substituted silybin ester or a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away HBsAG (Hepatitis B Surface Antigen) and HBeAg (Hepatitis B e Antigen) and suppressing the HBV (Hepatitis B Virus) DNA replication. The compound has strong activity on suppressing the HBsAG and the HBeAg, and in the presence of a concentration of 20 micrograms / milliliter, the intensities for clearing the HBsAg and the HBeAg are respectively 64.6 percent and 44.8 percent which are 4.0 times and 2.7 times of that of alpha-interferon which is a positive control medicament. In the presence of the concentration, the suppression rate of the compound on the HBV DNA is 58.1 percent which is 1.5 times of the corresponding activity of the alpha-interferon. Accordingly, the flavonolignan or the pharmaceutically acceptable salt thereof are indicated to simultaneously have strong efficacy on suppressing the HBsAg, the HBeAg and the HBV DNA and can be expected to be used for preparing non-nucleoside medicaments for treating HBV infection diseases.

The invention relates to a silibinin flavonoid lignan compound with anti-free radical oxidation, liver protection, prevention and treatment of senile dementia and anti-aging activities and a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to the preparation method of the compound of formula (1) including its important intermediates and its pharmaceutical composition and medical application. The compound of the present invention has anti-oxidative damage protective effect on the primary cells of SD neonatal rats, and can be expected to be used as a medicine for preventing liver damage; Radicals, the activity of inhibiting the generation of lipid peroxides induced by free radicals, and the strong anti-free radical-induced damage to PC12 cells, so it can be expected to be a drug for treating various diseases caused by free radicals.

The invention relates to application of ring A substituted silybin ester in preparing medicaments for treating viral hepatitis B, in particular to application of silybin ester flavonolignan substituted by ethoxycarbonyl methyl on the ring A or a pharmaceutically acceptable salt thereof for preparing medicaments for reducing the hepatitis B virus surface antigen (HBsAg), suppressing the HBV (Hepatitis B Virus) DNA replication and treating HBV infection diseases. The flavonolignan has quite obvious activity on suppressing the HBsAg, and in the presence of a concentration of 100 micrograms / milliliter, the intensity of the flavonolignan for clearing away the HBsAG exceeds that of alpha-interferon which is a positive control medicament by 3.3 times. Meanwhile, in the presence of a concentration of 20 micrograms / milliliter, suppression ratio of the compound to the HBV DNA is close to 60 percent. The pharmacodynamical results indicate that the flavonolignan or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicaments for treating the HBV infection diseases.

The invention discloses an anti-hepatic fibrosis composition and its application, belonging to the technical field of medicine. Composition of flavonoid lignan compound and soluble guanylate cyclase agonist can improve liver fibrosis in mice in thioacetamide liver fibrosis model. The present invention better cures liver fibrosis or provides another feasible option for treating liver fibrosis, and improves the prognosis or quality of life of patients.