30 results about "Prostaglandin synthesis" patented technology

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required a-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Fused cyclopentane-4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

The invention discloses a method for preparing prostaglandin E1 by using genetic engineering cyclooxygenase-1 and genetic engineering prostaglandin E synthetase-1, belonging to the field of bioengineering. The method expresses the relevant enzymes required for the synthesis of prostaglandin E1 by means of prokaryotic expression, that is, cyclooxygenase-1 (COX-1) and prostaglandin E synthase-1 (mPGES-1), and utilizes enzymes and substrates reaction to synthesize prostaglandin E1. Through this method, prostaglandin synthase can be expressed in large quantities and prostaglandin E1 can be synthesized, which can avoid the problem of easy contamination of tissue enzymes taken from living bodies in industrial production. At the same time, the types of enzymes expressed by the prokaryotic are relatively single, and the concentration of the expressed enzymes is relatively high, and the organic matter impurities in the E. coli system are relatively small, and the product impurities after the enzymatic reaction are relatively small, which is conducive to the purification and utilization of prostaglandin E1. Synthetic prostaglandin E1 has opened up a new path.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

The invention relates to the use of ginkgoic acid in preparation of biological pesticide for killing Oncomelania snail and preventing schistosomiasis, wherein experiment result shows that, the ginkgolic acid can effectively inhibit key enzyme and de-coupling reaction to mitochondria oxidation phosphorylation in mollusk energy supply biochemical metabolism, effectively inhibit tyrosinase during insect exuviation procedure and prostaglandin synthetase during breeding process, thus can eradicate unwanted mollusk harming agronomic crops.

The invention discloses a recombinant Escherichia coli, which overexpresses the encoding gene of prostaglandin H synthetase and the encoding gene of prostaglandin E synthetase. The invention also discloses the application of the above-mentioned recombinant Escherichia coli in producing prostaglandin E2. The invention also discloses a method for producing prostaglandin E2, which uses arachidonic acid as a substrate to produce prostaglandin E2 by using the recombinant Escherichia coli. The invention constructs an Escherichia coli strain capable of expressing the prostaglandin H synthetase and the prostaglandin E2 synthetase, and the expressed enzyme can directly catalyze the transformation of arachidonic acid into the prostaglandin E2.

The present invention provides new methods for inhibiting the activity of the enzyme cycloxygenase-2 (or COX-2). Inhibitors of COX-2 are known to be useful anti-inflammatory, analgesic and anti-angiogenic agents. The compounds in the present case are heterocyclic substituted 4-aminoglutarimides. Methods of using the compounds to inhibit prostaglandin synthesis are claimed.

The invention provides a mesalazine enteric-coated tablet composition with a four-layer coating system and a preparation method of the mesalazine enteric-coated tablet composition, and belongs to thefield of medicines. The composition is formed by combining a mesalazine tablet core and four layers of coatings, wherein the coatings sequentially comprise a first layer, a second layer, a third layerand a fourth layer from inside to outside, wherein the first layer is an isolation layer; the second layer is a slow-release casing layer; the third layer is a positioning acid-resistant layer; and the fourth layer is a moisture-proof layer. A second method for determining the dissolution rate by adopting the appendix of the Chinese pharmacopoeia is adopted, the release rate of the product is determined at 50rpm, and the release behavior should be as follows: the release rate is less than 10% in a dissolution medium with the pH value of 1.0 for 2h, then the product is transferred into a 7.4 medium, the release rate is 10-30% in 45min, the release rate is 50-75% in 75min and the release rate is 85% or above in 105min. The product is slowly released in intestines, most of the medicines canreach colons and act on inflammatory mucous membranes, prostaglandin synthesis causing inflammation and formation of inflammatory mediator leukotriene are inhibited, and the product has a remarkable anti-inflammatory effect on intestinal wall inflammation and particularly has a good effect on inflammatory intestinal wall connective tissues.