Pharmaceutical intermediate Gentiopicrin Powder

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Gentiopicrin Powder Usage and Synthesis.

Gentianoside is the dried root and rhizome of Gentiana manshurica Kitag., Gentiana scabra Bge, Gentiana triflora pall, Gentiana rigescens Franch. Gentian Gentiana scabra Bge, Gentiana triflora pall or Gentiana rigescens Franch.

Gentian has the properties of choleretic, anti-inflammatory, stomachic, antihypertensive, etc. Gentian is known to be a biliverdin, anti-inflammatory, stomachic, and antihypertensive. Gentian mainly contains cyclic enol ether terpene glycosides, of which gentianoside is the main active ingredient.

Uses of Gentiopicrin.

Gentianoside has antidepressant, hepatoprotective, anti-inflammatory and other effects and efficacy, gentianoside is a kind of cyclic ether terpene glycoside compounds, is the extract of gentian herb, especially in the roots and rhizomes of gentian herb, the content of the substance is relatively high.

1, antidepressant: the occurrence of depression is mainly associated with abnormal levels of cortisol, damage to the central nervous system function, etc., and research has found that gentian bittersweet on the reversal of cortisol damage to the organism has a certain degree of help, so in the alleviation of symptoms of depression, such as depressed state of mind, loss of interest, slow thinking, decreased attention, etc. has a certain effect

2, liver: Gentianoside can improve the imbalance of lipid metabolism triggered by long-term alcoholism, but also reduce fat deposition, for alcoholic fatty liver, non-alcoholic fatty liver, etc. have a certain degree of efficacy, while also preventing hepatic steatosis triggered by mild hepatic fibrosis, is beneficial to the protection of the liver.

3, anti-inflammatory: the substance is also helpful in reducing allergic asthma, osteoarthritis, gastritis and other discomforts, with certain anti-inflammatory effects.

In addition, gentian bittersweet is also helpful in improving diabetes, osteoporosis, etc. It can also increase bile secretion, promote gallbladder contraction, and has an excitatory effect on the central nervous system, etc.. However, the substance is not widely used in the clinic, and the specific mechanism of action needs to be further studied.

In vitro studies of Gentiopicrin.

Gentiopicroside inhibited P450 activity with IC50 and Ki of 61 μM and 8.12 μM for CYP2A6, and also slightly inhibited CYP2E1 activity with IC50 of 1.6 mM, but had no inhibitory effect on CYP1A2 and CYP3A4.

Gentiopicroside (12.5, 25 and 50 μM) inhibited RANKL-induced osteoclast formation, blocked the expression of osteoclast-associated proteins, and prevented Receptor Activator of Nuclear Factor-κB Ligand (RANKL) )-triggered JNK and NF-κB activation in a dose-dependent manner in mouse bone marrow macrophages (BMMs). Gentiopicroside (50 μM) also inhibited RANKL-induced bone resorption.

Production Method of Gentiopicrin.

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