45 results about "Flavonolignan" patented technology

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 application of aromatic carbamoyl dehydro-silibinin as a medicament for treating viral hepatitis B, in particular to application of todehydro-silibinin flavonolignans with a ring A and a ring E which are substituted by double base aromatic carbamoyl methoxyl and pharmaceutically acceptable salt thereof for preparing medicaments for removing HBsAg and HBeAg and medicaments for inhibiting HBV DNA. The todehydro-silibinin flavonolignans has extremely obvious activity on inhibiting the HBsAG and the HBeAg, has the intensity of 46.2 percent and 68.9 percent for respectively removing the HBsAG and the HBeAg in the presence of the concentration of 100 microgram/milliliter, which is 2.9 times and 4.1 times higher than that of positive control medicament alpha-interferon, and has the inhibition ratio of 96 percent on HBV DNA in the presence of the concentration of 100 microgram/milliliter, which is higher than that of lamivudine and the alpha-interferon. Accordingly, the flavonolignans and the pharmaceutically acceptable salt thereof can be expected to be used for preparing non-nucleoside medicaments applied for removing HBsAg and HBeAg, inhibiting HBV DNA replication and treating hepatitis B virus infection diseases.

The invention relates to application of ring A coupling flavonolignan in preparing medicaments for treating viral hepatitis B, in particular to application of a compound of the formula (1) 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 intensities of the flavonolignan for clearing away the HBsAg and the HBeAg are respectively 29.4 percent and 29.1 percent in the presence of a concentration of 20 micrograms/milliliter, which is respectively 1.8 times and 1.7 times of the corresponding activity of a positive control medicament (10,000 units/milliliter of alpha-interferon). What is even more exciting is that in the presence of the concentration, the suppression rate of the flavonolignan to the HBV DNA is higher than 83 percent, which is higher than that of Lamivudine which is a positive control and is 2.2 times of that of the alpha-interferon to the HBV DNA. Accordingly, the flavonolignan and the pharmaceutically acceptable salt thereof are indicated to be capable of being expected to be used for preparing non-nucleoside medicaments for clearing away the HBsAg and the HBeAg, suppressing the HBV DNA replication and treating HBV infection diseases.

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 flavonolignan and its medicine salt or solvates. The invention also relates to the method preparing its important mediate and its drug combination and medical application. The compound can protect primary hepatocyte from oxidative damage for SD newly born rat hepatitis virus, so it is expected to be used as drug preventing liver damage. The compound can remove superoxide anion free radical and diphenyl picryl phenylhydrazine free radical, inhibit free radical from inducing generation of fat oxidatant, protect PC 12 cell from being damaged by free radical, so it is expected to be used as drug treating diseases caused by free radical.

A method is disclosed for increasing blood serum levels of dehydroepiandrosterone by administering the combination of one of a flavonoid, isoflavonoid, coumarin and a flavonolignan; dehydroepiandrosterone; and a plant extract.

The invention relates to application of dehydrogenation silybin in preparation of a medicament for treating virus hepatitis B, in particular to application of the dehydrogenation silybin or pharmaceutically acceptable salt thereof in preparation of the medicament for inhibiting HBV DNA replication. The medicament has obvious high hepatitis B virus desoxyribonucleic acid (HBV DNA) inhibiting activities and shows over 55 percent of inhibition rate for the HBV DAN at the concentration of 20 mg/ml, which is 1.5 times higher than that of a positive control medicament (10,000 unit/ml of alpha-interferon). The pharmacodynamics result shows the flavonolignan or the pharmaceutically acceptable salt thereof can be expected for preparing the non-nucleoside medicament for inhibiting HBV DNA replication and curing diseases caused by infection of hepatitis B virus.

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 B ring methoxy substituted silybin to preparing glycosidase inhibitors and in particular discloses application of B ring methoxy 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 75.6%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 8 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 substituted silybin ester in preparing a medicament for treating virus hepatitis B, in particular to application of 23-position ethyl-malonyl substituted silybin ester or medicinal salt thereof in preparing a medicament for reducing hepatitis B virus surface antigen HBsAg, inhibiting HBV DNA replication and treating hepatitis B virus infected diseases. The flavonolignan has remarkable effect of inhibiting HBsAg activity, and the strength of the flavonolignan at the concentration of 100 micrograms per milliliter for clearing the HBsAg is two times and half that of a positive control medicament alpha-interferon; and meanwhile, the compound has strong inhibiting activity on the HBV DNA. Pharmacodynamical results show that the flavonolignan or the medicinal salt thereof can be expected to be used for preparing the medicament for reducing hepatitis B virus surface antigen, inhibiting HBV DNA replication and treating the hepatitis B virus infected diseases.

The invention relates to application of B/E ring changed silybin to preparing glycosidase inhibitors and in particular discloses application of B ring ethyoxyl or E ring de-methoxy 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 54.3%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 2.5 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 pharmaceutical application of p-bromocinnamoyl silybin to preparing glycosidase inhibitors and specifically discloses application of 23-p-bromocinnamoyl substituted silybin ester flavonolignans or medicinal 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 54.4% under the condition of 4mcg/ml concentration. The measured half-inhibitoryconcentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 76.8 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or medicinal 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 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 the field of natural medicinal chemistry, a preparation of a crude extract and flavonolignans compounds in milk thistle and an application thereof, and in particular to the activity-oriented separation and purification preparation as well as antidiabetic activity of the flavonolignans compounds in traditional Chinese medicine milk thistle. The invention also discloses theisolation and preparation of the compounds, the inhibitory activity on PTP1B enzyme, the evaluation of molecular simulation docking with PTP1B enzyme, the evaluation of enzyme kinetics of PTP1B, and the selective evaluation of homologous enzymes. The test results show that the crude extract from an ethyl acetate extraction layer of milk thistle and the flavonolignan compounds play better PTP1B enzyme inhibitory activity; and the flavonolignans compounds can inhibit the activity through a hydrogen bond with strong binding to a catalytically active region of PTP1B enzyme.

A method of treatment of a subject suffering from liver disease comprising the administration of (i) an oral slow-release formulation of a calcium channel blocker with antioxidant effects and (ii) at least one flavonolignan.

The invention relates to application of substituted benzoyl silybin in preparing a medicament for treating virus hepatitis B, in particular to application of 3-amino-5-nitrobenzoyl substituted silybin ester type flavonolignan or medicinal salt thereof in preparing a medicament for inhibiting HBV DNA replication and treating hepatitis B virus infected diseases. The flavonolignan has the effect of definitely inhibiting HBV DNA activity, the activity of the flavonolignan in high dosage (100 micrograms per milliliter) for inhibiting the HBV DNA replication is 55 percent higher than the inhibiting activity of alpha-interferon at highest concentration of 10,000 units per milliliter, and the flavonolignan belongs to an effectual non-nucleoside natural product for inhibiting the hepatitis B virus. Pharmacodynamical results show that the flavonolignan or the medicinal salt thereof can be expected to be used for preparing the medicament for inhibiting HBV DNA replication and treating the hepatitis B virus infected diseases.