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Preparation methods of diterpene lactone compounds and application of the same to antifertility
| Details |
Inventors: Qian, Shoa-Zhen; Zheng, Jia-Run; Lu, Xie-Yu; Ma, Peng-Cheng; Zhang, Chong-Pu; Chen, Yun; Gu, Ke-Xian; Xu, Wen-Yan; Zhang, Zheng-Xing; Sheng, Long-Sheng; An, Deng-Kui; Xu, Ye; Zhen, Qi-Tai;
Assignee: Jiangsu Family Planning Institute (all of, CN); China Pharmaceutical University (all of, CN); Institute of Dermatology, Chinese Academy of Medical Sciences (all of, CN)
Primary Examiner: Rotman; Alan L.
Assistant Examiner: Owens; A. A.
Attorney, Agent or Firm: Merchant, Gould, Smith, Edell, Welter & Schmidt
The invention provides methods of preparing a male antifertility agent composed of a diterpene lactone compound obtained from plants of the genus Tripterygium, the diterpene lactone compounds obtained from that method, and the use of the compounds as an antifertility agent. |
|
DETAILED DESCRIPTION What is claimed is: 1.
A method of producing a purified diterpene lactone compound, comprising: (a) treating a plant part derived from a Tripterygium plant with an organic solvent to provide an extract containing the diterpene lactone compound; and (b) separating the diterpene lactone compound from other substances in the extract.
2.
The method according to claim 1, wherein step (b) comprises separating the diterpene lactone compound from the other substances in the extract by gradient elution column chromatography using a second organic solvent.
3.
The method according to claim 2, wherein the second organic solvent is selected from the group consisting of chloroform, methyl alcohol, ethyl alcohol, acetone, benzene, cyclohexane, petroleum ether, ethyl ether, ethyl acetate, and combinations thereof.
4.
The method according to claim 3, further comprising: step (c) purifying the diterpene lactone compound.
5.
The method according to claim 4, wherein step (c) comprises purifying the diterpene compound by chromatographic separation, crystallization, or a combination thereof.
6.
The method according to claim 1, wherein prior to step (a), the plant part is boiled in water to provide an aqueous extract containing the diterpene lactone compound; and step (a) comprises treating the aqueous extract with the organic solvent.
7.
The method according to claim 1, wherein the Tripterygium plant is T.
wilfordii Hook.
f.
or Multiglycosidorom tripterygii.
8.
The method according to claim 1, wherein the Tripterygium plant is T.
Regelii Sprague et Takada or T.
Hypoglaucum (L'evl).
9.
The method according to claim 1, wherein the diterpene lactone compound has a chemical formula: ##STR8## wherein R.
sub.
1,R.
sub.
2 =--Cl and --OH, or --O--; R.
sub.
3 =CH.
sub.
3 ; R.
sub.
4 =H or OH; R.
sub.
5 =OH or =O; and R.
sub.
6,R.
sub.
7 =--O--; and when (a) R.
sub.
1 =--Cl and R.
sub.
2 =--OH: R.
sub.
4 =H and R.
sub.
5 =OH; and (b) R.
sub.
1,R.
sub.
2 =--O--: R.
sub.
4 =OH and R.
sub.
5 =OH; or R.
sub.
4 =H and R.
sub.
5 =O.
10.
The method according to claim 9, wherein the diterpene lactone compound is selected from the group consisting of tripchlorolide, triptolidenol, triptonide, and combinations thereof
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