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Dammarane sapogenin and oleanane sapogenin derivatives as well as preparation and application thereof

A technology of dammarane saponin and oleanane, which is applied in the field of medicine and can solve the problems of limited number of researches

Active Publication Date: 2020-10-27
辽宁新中现代医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, about 25-OCH 3 -Limited number of studies on PPD metabolism

Method used

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  • Dammarane sapogenin and oleanane sapogenin derivatives as well as preparation and application thereof
  • Dammarane sapogenin and oleanane sapogenin derivatives as well as preparation and application thereof
  • Dammarane sapogenin and oleanane sapogenin derivatives as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0069] Step 1: Weigh 400 mg of the acid hydrolyzate of dammarane saponin or the separated saponin, put it in a 100 mL Erlenmeyer flask, dissolve it ultrasonically with 2 mL of ethanol, then slowly add 68 mL of propylene glycol, while continuously using a glass rod Stir, and finally add 32mL of distilled water dropwise to obtain a clear and transparent drug solution for gavage without drug precipitation;

[0070] Step 2: Administer the drug solution obtained in step 1 for intragastric administration (1mL / 100g) according to the weight of the rat, collect 24h of biological samples (including blood, urine, feces and bile), and after centrifugation, filtration, etc., Store in the refrigerator. After this process continued for 7 weeks, all the obtained biological samples were mixed, subjected to ultrasonic extraction, and concentrated under reduced pressure to obtain extracts of each biological sample;

[0071] Step 3: Carry out column chromatography separation of each biological s...

preparation Embodiment 2

[0082] Step 1: Weigh 400 mg of the acid hydrolyzate of dammarane saponin or the separated saponin, put it in a 100 mL Erlenmeyer flask, dissolve it ultrasonically with 2 mL of ethanol, then slowly add 68 mL of propylene glycol, while continuously using a glass rod Stir, and finally add 32mL of distilled water dropwise to obtain a clear and transparent drug solution for gavage without drug precipitation;

[0083] Step 2: Administer the drug solution obtained in step 1 for intragastric administration (1mL / 100g) according to the weight of the rat, collect 24h of biological samples (including blood, urine, feces and bile), and after centrifugation, filtration, etc., Store in the refrigerator. After this process continued for 7 weeks, all the obtained biological samples were mixed, subjected to ultrasonic extraction, and concentrated under reduced pressure to obtain extracts of each biological sample;

[0084] Step 3: Carry out column chromatography separation of each biological s...

preparation Embodiment 3

[0089] Step 1: Weigh 400 mg of the acid hydrolyzate of dammarane saponin or the separated saponin, put it in a 100 mL Erlenmeyer flask, dissolve it ultrasonically with 2 mL of ethanol, then slowly add 68 mL of propylene glycol, while continuously using a glass rod Stir, and finally add 32mL of distilled water dropwise to obtain a clear and transparent drug solution for gavage without drug precipitation;

[0090] Step 2: Administer the drug solution obtained in step 1 for intragastric administration (1mL / 100g) according to the weight of the rat, collect 24h of biological samples (including blood, urine, feces and bile), and after centrifugation, filtration, etc., Store in the refrigerator. After this process continued for 7 weeks, all the obtained biological samples were mixed, subjected to ultrasonic extraction, and concentrated under reduced pressure to obtain extracts of each biological sample;

[0091] Step 3: Carry out column chromatography separation of each biological s...

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Abstract

The invention belongs to the technical field of medicines, and relates to dammarane sapogenin and oleanane sapogenin derivatives as well as a preparation method and application thereof. The method comprises the following steps: giving an acid hydrolysate of plant-derived dammarane saponin or separated sapogenin to SD rats by intragastric administering; collecting 7-week biological samples, extracting the samples by using ethyl acetate, separating and purifying the extract obtained by extraction, accurately identifying the structure of the extract by depending on chemical and spectral experiments, and discussing the derivation process of the biosynthesis route of the extract. According to the invention, anticancer biological activity evaluation and mechanism research are carried out on thederivative, and results show that the prepared dammarane sapogenin and oleanane sapogenin derivative have an obvious anticancer effect. The dammarane sapogenin and oleanane sapogenin derivatives canbe used for preparing medicines for treating cancers.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, relates to dammarane sapogenin and oleanane sapogenin derivatives and their preparation methods and applications, in particular to a series of dammarane sapogenin with new metabolic sites for in vivo biotransformation Alkanesapogenin and oleananesapogenin derivatives and their preparation methods and applications in the preparation of anticancer drugs. Background technique: [0002] Dammarane saponins can be mainly divided into dammarane type, octilon type, oleanane type and other types through their core structure. Oleanane-type saponins are pentacyclic triterpene dammarane saponins, but in the current study, two dammarane saponins, Ro and Ri, were found to be oleanane-type nuclei. Dammarane-type saponins are mainly tetracyclic triterpenes. Habitually divided into diol types according to the number of hydroxyl groups on the parent nucleus (such as Ra 1 , Ra 2 , Rb 1 , Rb 2 , Rb 3 , Rc, ...

Claims

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Application Information

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IPC IPC(8): C07J9/00C07J17/00C07J63/00A61P35/00A61K31/56A61K31/58A61K31/575
CPCC07J9/00C07J17/00C07J63/008A61P35/00
Inventor 赵余庆丁萌王旭德张雨蒙徐磊
Owner 辽宁新中现代医药有限公司