Summary of the invention:
The purpose of this invention is to provide the extracting method and the application thereof of a kind of Chinese yew genus plants extract and this extract, it had both solved the problem of Chinese yew genus plants continuous utilization, again under the prerequisite that guarantees curative effect, improved the utilization ratio of Chinese yew genus plants, brought up to more than 5/1000ths from single extraction taxol utilization ratio less than 2/10000ths.Chinese yew genus plants of the present invention is that the branches and leaves with taxus chinensis in northeast are that raw material extracts and forms, it comprises following compositions: Taxan diterpene compound, total lignans, total flavones, described Taxan diterpene compound account for three kinds of composition cumulative volumes 18~68%, total lignans account for three kinds of composition cumulative volumes 14~61%, total flavones accounts for 10~50% of three kinds of composition cumulative volumes.Its extracting method is prepared according to following step: a, be that 40~95% alcohol solvent returns and carries 1~3 hour with the branches and leaves volumetric concentration of Chinese yew genus plants medicinal material, be condensed into former medicinal extract; B, add the distilled water of 30~80 times of former medicinal extract weight then, the former medicinal extract of dissolving under 60~80 ℃ or ultransonic condition leaves standstill centrifugal, the precipitation of after-filtration; C, to be 50~90% ethanol with volumetric concentration extract above-mentioned throw out under 60~80 ℃ or ultransonic condition, extract three times, and the each add-on of ethanol is 5~15 times of weight of precipitate, leaves standstill after-filtration, centrifugal; D, merge ethanol extract, in extracting solution, add ethanol, be mixed with and contain that the alcohol amount is 20~40%, volume is the solution of 30~70 times of above-mentioned former medicinal extract; E, with above-mentioned solution by the macroporous adsorption resin chromatography post, the consumption of macroporous adsorbent resin is 10~20 times of former medicinal extract weight; F, be 20~40% ethanolic soln upper prop, wash to look light that the ethanol consumption is 8~12 times of column volume with volumetric concentration, flow velocity 0.5~1.5 column volume/hour; G, be 40~60% ethanolic soln upper prop with volumetric concentration then, wash to look light that the ethanol consumption is 8~15 times of column volume, flow velocity 0.5~1.5 column volume/hour; H, be 65~80% ethanolic soln upper prop with volumetric concentration again, wash to look light that the ethanol consumption is 10~15 times of column volume, flow velocity 0.5~1.5 column volume/hour; I, collect elutriant respectively, be evaporated to driedly, obtain the extract of Chinese yew genus plants.This extract can be used as the effective constituent of cancer therapy drug.When extract of the present invention used as the effective constituent of cancer therapy drug, this medicine can be processed into various formulations according to ordinary method in the pharmacy field, as injection, tablet, capsule etc.Chinese yew genus plants extract of the present invention is to be that feed purification forms with the taxus chinensis in northeast, Ramulus et folium taxi cuspidatae has anti-cancer and kill cancer action, advolution that can anticancer, can also improve simultaneously the circulation and the metabolic function of human body, make to be accumulated in the intravital virus of people and to be scavenged into externally by diuresis, defecation, reach the effect of preventing cancer, to the particularly postoperative patient of patient of cancer, can reduce the side effect of radiotherapy chemotherapy, play the effect of assisting therapy.Chinese yew genus plants extract of the present invention is a main component with Taxan diterpene compound, total lignans and total flavones, wherein the Taxan diterpene compound has unique antitumor action, it can combine the stable underwater pipeline stabilizing bundle of formation with tubulin and make by depolymerization, cancer cells is stopped at G2 late period or M phase, suppress cellular replication, stop cancer cells Z propagation; Total lignans has antineoplastic activity; Flavones has antioxygenation (removing free radical) and to the influence of multiple bioenzyme activity; Behind Taxan diterpene compound, total lignans and the total flavones compatibility, not only improve the curative effect of medicine, and had the effect that improves body immunity.Drug main of the present invention will be used for the treatment of lung cancer, melanoma, mammary cancer etc.It is obvious that this medicine is taken effect to postoperative patient, alternative or cooperate put, chemotherapy treats, the improvement of patient's lung cancer symptom is mainly shown on cough-relieving, hemostasis, the analgesic effect, and effect is remarkable.Simultaneously patient's appetite, physique etc. also there is significant improvement.The present invention is the medicine that utilizes the new medicinal part of Chinese yew genus plants branches and leaves to make, it contains multiple anticancer effective ingredient, has characteristics such as yield height, cost be low, and its anticancer effect is not less than taxol, realized simultaneously the continuous utilization of Chinese yew genus plants again, and side effect is extremely low.Under the prerequisite that guarantees curative effect, improved the utilization ratio of Chinese yew genus plants, to bring up to more than 5/1000ths from single extraction taxol utilization ratio less than 2/10000ths, utilization ratio improves more than 25 times.
Embodiment:
Embodiment one: the Chinese yew genus plants extract of present embodiment is that the branches and leaves with taxus chinensis in northeast are that raw material extracts and forms, and it comprises following compositions: Taxan diterpene compound, total lignans, total flavones.Described Taxan diterpene compound account for three kinds of composition cumulative volumes 18~68%, total lignans account for three kinds of composition cumulative volumes 14~61%, total flavones accounts for 10~50% of three kinds of composition cumulative volumes.Described Taxan diterpene compound comprises taxinine, taxinine B, 10-deacetylate baccatin III, 10-deacetylate taxinine B and Japanese yew cloud booth A; Described total lignans comprises conidendrin; Described total flavones comprises kaempferol and Naringenin.
Embodiment two: the Chinese yew genus plants extract of present embodiment is prepared according to following step: a, be that 40~95% alcohol solvent returns and carries 1~3 hour with the branches and leaves volumetric concentration of Chinese yew genus plants medicinal material, be condensed into former medicinal extract; B, add the distilled water of 30~80 times of former medicinal extract weight then, the former medicinal extract of dissolving under 60~80 ℃ or ultransonic condition leaves standstill centrifugal, the precipitation of after-filtration; C, to be 50~90% ethanol with volumetric concentration extract above-mentioned throw out under 60~80 ℃ or ultransonic condition, extract three times, and the each add-on of ethanol is 5~15 times of weight of precipitate, leaves standstill after-filtration, centrifugal; D, merge ethanol extract, in extracting solution, add ethanol, be mixed with and contain that the alcohol amount is 20~40%, volume is the solution of 30~70 times of above-mentioned former medicinal extract; E, with above-mentioned solution by the macroporous adsorption resin chromatography post, the consumption of macroporous adsorbent resin is 10~20 times of former medicinal extract weight; F, be 20~40% ethanolic soln upper prop, wash to look light that the ethanol consumption is 8~12 times of column volume with volumetric concentration, flow velocity 0.5~1.5 column volume/hour; G, be 40~60% ethanolic soln upper prop with volumetric concentration then, wash to look light that the ethanol consumption is 8~15 times of column volume, flow velocity 0.5~1.5 column volume/hour; H, be 65~80% ethanolic soln upper prop with volumetric concentration again, wash to look light that the ethanol consumption is 10~15 times of column volume, flow velocity 0.5~1.5 column volume/hour; I, collect elutriant respectively, be evaporated to dried, obtain the extract of Chinese yew genus plants, promptly as the effective constituent of cancer therapy drug, yield is 20~70%, and wherein the yield of each composition is: Taxan diterpene compound 8~25%, total lignans 7~20%, total flavones 5~15%, and mentioned component is through infrared, ultraviolet, nucleus magnetic resonance, mass spectrometric detection, its structural formula is:
Taxinine Japanese yew cloud booth A
Taxinine B 10-deacetylate baccatin III
10-deacetylate taxinine B kaempferol
The conidendrin Naringenin
Embodiment three: the Chinese yew genus plants extract of present embodiment is as the effective constituent of the cancer therapy drug of treatment lung cancer, melanoma, mammary cancer.
The pharmacodynamic experiment summary:
One, the standard of case selection:
1, lung cancer 40 examples, the male sex's 22 examples wherein, women's 18 examples, at minimum 29 years old of age, maximum 55 years old, 43 years old mean age, the course of disease is the shortest 2 years, and was the longest 10 years.
2, mammary cancer 32 examples are the women, and at minimum 33 years old of age, maximum 54 years old, 44 years old mean age, the course of disease is the shortest 1 year, and was the longest 11 years.
3, melanoma 25 examples, the male sex's 20 examples wherein, women's 5 examples, at minimum 44 years old of age, maximum 62 years old, 50 years old mean age, the course of disease is the shortest 5 years, and was the longest 20 years.
Two, the Case definition of disease:
1, lung cancer: cough, sputum mixed with blood, pectoralgia, shortness of breath.
2, mammary cancer: pain or sensation one or both sides breast turgor, nipple discharge.
3, melanoma: the melanochrome tubercle of growing up rapidly.
Three, the contained composition of medication: the injection of making by Chinese yew genus plants extract (500mg).
Four, administrated method: 7~10 days is a course of treatment, and inject once every day.
Five, the judging criterion of curative effect:
1, recovery from illness: symptom completely dissolve.
2, produce effects: symptom is clearly better.
3, effective: symptom turns for the better by and large.
4, invalid: symptom does not change.
Six, efficacy result analysis:
Case | The example number | Recovery from illness (%) | Produce effects (%) | Effectively (%) | Invalid (%) | Total effective rate (%) |
Lung cancer | 40 | 16(40) | 8(20) | 4(10) | 12(30) | 70 |
Mammary cancer | 32 | 12(37.5) | 8(25) | 4(12.5) | 8(25) | 75 |
Melanoma | 25 | 10(40) | 4(16) | 3(12) | 8(32) | 68 |
The pharmacodynamics preliminary study is found to answer Chinese yew genus plants extract to reach 68% as the curative effect of the application of cancer therapy drug under the situation of 125mg/kg, does not see any toxicity, and its therapeutic index is greater than taxol, and effectively the toxicity under the situation is starkly lower than taxol.