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Total unsaturated toad lactone, and preparation method and use thereof

A bufa lactone and unsaturated technology, applied in the field of natural medicinal chemistry, can solve problems such as cardiotoxicity, and achieve the effects of low cost, simple preparation method and good anti-prostate cancer activity

Active Publication Date: 2013-04-03
GUANGXI WUZHOU PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these compounds have a steroidal skeleton very similar to digoxin, which can cause significant cardiotoxicity (Roger, J.B.; Brian, J.P.; Roxanne, R S.; Amitava, D. Effects of Chan Su, a traditio-nal Chinese medicine. Life sciences. 2002, 72(6), 699-709.)

Method used

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  • Total unsaturated toad lactone, and preparation method and use thereof
  • Total unsaturated toad lactone, and preparation method and use thereof
  • Total unsaturated toad lactone, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] (1) The preparation of total unsaturated bufalides comprises the following steps:

[0048] A. Grind 20g of dried Chansu (commercially available) with a stirrer, pass through a 100-mesh sieve, and extract 3 times with ethanol (absolute ethanol) with a volume percentage of 95% at room temperature through a KQ 250DE ultrasonic machine, each time using ethanol 100ml, each time for 1 hour, combine the three extracts, filter with filter paper to remove the residue, and obtain the toad venom extract.

[0049] B. Then use the N-1100V-W type rotary evaporator to concentrate the extract of toad venom under reduced pressure to form a slurry to obtain the total extract of toad venom.

[0050] C, suspending the total extract of Bufo venom with ultrapure water, extracting with 250ml dichloromethane, and removing dichloromethane under reduced pressure to obtain 12.2g of dichloromethane parts, which are total bufolides;

[0051] D. Dissolve the total bufolide obtained in step (3) with...

Embodiment 2

[0091] (1) The preparation of total unsaturated bufalides comprises the following steps:

[0092] A. Grind 20g of dried Chansu (commercially available) with a stirrer, pass through a 100-mesh sieve, and extract 3 times with ethanol (absolute ethanol) with a volume percentage of 95% at room temperature through a KQ 250DE ultrasonic machine, each time using ethanol 100ml, each time is 1 hour, combine the three extracts, filter with filter paper, to obtain the extract of Buad venom.

[0093] B. Then use the N-1100V-W type rotary evaporator to concentrate the extract of toad venom under reduced pressure to form a slurry to obtain the total extract of toad venom.

[0094] C, suspending the total extract of Bufo venom with ultrapure water, extracting with 200ml dichloromethane, and decompressing to remove dichloromethane to obtain 11.8g of dichloromethane parts, which are total bufolides;

[0095] D. Dissolve the total bufalide obtained in step (3) with 50ml of dichloromethane, add...

Embodiment 3

[0103] (1) The preparation of total unsaturated bufalides comprises the following steps:

[0104] A. Grind 20g of dried toad venom (commercially available) with a blender, pass through a 100-mesh sieve, and extract 3 times with 95% ethanol (absolute ethanol) at room temperature through a KQ 250DE ultrasonic machine, each time using ethanol 100ml, each time is 1 hour, combine the three extracts, filter with filter paper, to obtain the extract of Buad venom.

[0105] B. Then use the N-1100V-W type rotary evaporator to concentrate the extract of toad venom under reduced pressure to form a slurry to obtain the total extract of toad venom.

[0106] C, suspending the total extract of toad venom with ultra-pure water, extracting with 300ml dichloromethane, and decompressing to remove dichloromethane to obtain 12.8g of dichloromethane parts, which are total bufolides;

[0107] D. Dissolve the dichloromethane part obtained in step (3) with 50ml of dichloromethane, add 10% sulfuric aci...

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Abstract

The invention discloses a total unsaturated toad lactone, and a preparation method and a use thereof. The preparation method for the total unsaturated toad lactone comprises the following steps: (1), crushing the toad, ultrasonically extracting the crushed toad 3-4 times using ethanol solution, and filtering to remove the dredges to obtain the toad extracting solution; (2), concentrating the toad extracting solution under reduced pressure to obtain pulp as the toad total extract; (3), suspending the toad total extract with water, extracting the suspended toad total extract using dichloromethane, and evaporating under reduced pressure to remove dichloromethane to obtain the dichloromethane part; and (4), dissolving the dichloromethane part with a solvent A and regulating the pH value of the solution to 1-6, stirring and reacting the solution for 1-8 hours at a temperature of 0 DEG C to 100 DEG C, adding water to stop the reaction when at least two compounds of Bu-1, Bu-2, Bu-3, Bu-4 and Bu-5 in the solution are detected, extracting using a solvent B, and evaporating under reduced pressure to remove the solvent B to obtain the total unsaturated toad lactone. The total unsaturated toad lactone disclosed by the invention has the activity of inhibiting male sex hormone dependent form prostate cancer cell multiplication and non-male sex hormone dependent form prostate cancer cell multiplication, and can be used for preparing the medicine for preventing and treating the prostate cancer.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and particularly relates to a total unsaturated bufa lactone and a preparation method thereof, and the application of the total unsaturated bufa lactone in the preparation of drugs for preventing and treating prostate cancer; the total unsaturated bufa lactone of the present invention Lactone is obtained by modifying bufolide as raw material. Background technique [0002] Prostate cancer is one of the most common cancers in men, and its incidence is related to race, age and lifestyle. Before the 1980s, the incidence rate in my country was significantly lower than that in Western countries. There are two main reasons: 1) The traditional Chinese diet contains less fat and more vegetables and soy products, so the Chinese diet contains a lot of phytoestrogens, which can inhibit the growth of prostate cancer cells; 2 ) The CAG polypeptide repeat sequence in the Chinese male prostate recept...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61P35/00C07J19/00
Inventor 江仁望余通田海妍李娟叶文才
Owner GUANGXI WUZHOU PHARMA GRP
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