CN1541643A - Use of Wangzaozi secondary element as immunological inhibitors - Google Patents
Use of Wangzaozi secondary element as immunological inhibitors Download PDFInfo
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- CN1541643A CN1541643A CNA031133649A CN03113364A CN1541643A CN 1541643 A CN1541643 A CN 1541643A CN A031133649 A CNA031133649 A CN A031133649A CN 03113364 A CN03113364 A CN 03113364A CN 1541643 A CN1541643 A CN 1541643A
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- isodon amethystoides
- wuet hsuen
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Abstract
The present invention is the application of common rabdosia leaf essence B in preparing medicine for treating immunological diseases. The common rabdosia leaf essence B as one kind of active component in Chinese herbal medicine material common rabdosia leaf can obviously inhibit ConA induced and LPS induced mouse splenic lymphocyte proliferation and has the function of inhibiting cell mediated immunity and humoral immunity. It may be used in treating various autoimmune disease clinically.
Description
One, technical field
The present invention relates to the new indication of active component in a kind of Chinese herbal medicine, specifically in the Chinese herbal medicine Isodon amethystoides (Benth.) C.Y.Wuet Hsuen active component Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element as the application of immunosuppressant.
Two, background technology
Isodon amethystoides (Benth.) C.Y.Wuet Hsuen (Rabdosia amethytoides) is a kind of in the Labiatae Rabdosia plant, is medical herbs commonly used among the people, is used for anti-inflammation etc.Jiangsu Province's Chinese crude drug standard in 1989 is recorded.
Under normal circumstances, the immune system of human body protection body has the effect of three aspects, promptly resists the defense reaction of adventitious agents invasion, keeps self balance and stable effect, eliminates the supervision effect of mutant cell.In case immunoreaction abnormity all can cause histologic lesion and causes a disease, claim immune disease.Immune disease has two kinds, and a kind of is that immunologic hypofunction causes, claims immunodeficiency; To be that immunologic function is extraordinary cause another kind, claims autoimmune disease (autoimmune disease, allergy etc.).Divide two kinds of organ specificity and systemic autoimmune diseases again, the former pathological changes is limited to a certain certain organs, and latter's pathological changes jeopardizes multiple organ and tissue, as systemic lupus erythematosus (sle), rheumatoid arthritis, scleroderma, polymyositis etc.(" pathology ", the third edition, Wu Zhongbi chief editor, the People's Health Publisher publishes April nineteen ninety-five).
Regulate the effect of immunologic function about Rabdosia class plant, mostly disclosed is enhancing body's immunological function, just adapts to immunodeficiency symptoms.Point out that as " the largesepal rabdosia leaf total diterpene is to the regulating action of immune function of mice " literary composition total diterpene all has remarkable facilitation (" Chinese crude drug " 1999.22 (7) p348～350) to humoral immunization and the cellular immunization function of normal and immunologic hypofunction mice.The antitumor mechanism and the cellular immune function relevant (" Chinese Chinese medicine science and technology " 2000.7 (2) .p89～89) that improves tumor mice of Rabdosia excisa pointed out in " Rabdosia excisa is to the experimentation of tumor-bearing mice Immune Function " literary composition.
(Autoimmunity disease AID) is one of the common refractory disease of serious harm human health to autoimmune disease, does not still have the medicine of being satisfied with at present.For a long time, the standard care that modern medicine is implemented is that the hormone nonspecific immunity suppresses therapy, but can only improve symptom, but can't eliminate the cause of disease, and side effect is bigger.
In recent years, the correlational study of relevant natural drug treatment autoimmune disease is the research focus of pharmacy circle.From at present natural drug being treated the relevant pharmaceutical research of autoimmune disease, natural drug has remarkable advantages than the Western medicine of present clinical use, and it mainly is the effect of bringing into play the treatment autoimmune disease by immunosuppressant, immunomodulating, antioxidation, cell death inducing and the mediator that affects the nerves.The immune pharmacological action of natural drug is not the single effect that is independent of other functions, but the tight unified function system that interrelates with nerve, endocrine, immunomodulating network (NIM).Therefore, both at home and abroad seek the prefered method of the medicine of treatment autoimmune disease from occurring in nature as this type of drug research.
The king of Anhui Prov. Medical Science Inst. elder generation honor etc. was carried out systematic research to the active ingredient in the Isodon amethystoides (Benth.) C.Y.Wuet Hsuen, therefrom isolated Isodon amethystoides (Benth.) C.Y.Wuet Hsuen first element, second element and third element, and Bake China fir alkane type (ent-kaurane) diterpene basic framework is all arranged.The first element can change the second element into through Jone ' s reagent oxidation, and third is plain with the processing of 1% oxalic acid aqueous solution, C
14Also be converted into the second element after-acetyl group is hydrolyzed, thereby the structure of establishing Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element is
" the new diterpene of Isodon amethystoides (Benth.) C.Y.Wuet Hsuen-Isodon amethystoides (Benth.) C.Y.Wuet Hsuen first element " (the 13rd the 6th phase of volume of " Chinese herbal medicine " nineteen eighty-two p.12～13.
Three, summary of the invention
The applicant had once done body in and experiment in vitro to mice with regard to Isodon amethystoides (Benth.) C.Y.Wuet Hsuen decocting liquid and alcohol extract aspect Immune Function, the result shows, the pastille serum of decocting liquid and alcohol extract all can suppress lymphopoiesis, have immunosuppressive action, and applied for patent of invention (application number: 03112870.X) on February 21st, 2003.On this basis, the further separation and Extraction liquid of applicant adopts the pharmacodynamic experiment method to follow the trail of active site, and finally searching out Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element is the effective ingredient of Isodon amethystoides (Benth.) C.Y.Wuet Hsuen immunosuppressive action.
Result of study shows that Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element can significantly suppress ConA and the inductive mice spleen lymphocytes proliferation of LPS, and immunity capable of inhibiting cell and humoral immunization have stronger immunosuppressive action, can be used as immunosuppressant and uses.Clinically, can use treatment to autoimmune diseasees such as systemic lupus erythematosus (sle), rheumatoid arthritis, scleroderma, chronic nephritis, autoimmune hemolytic anemia, tuberculosis and organ transplantation.
Four, the specific embodiment
1, the Isodon amethystoides (Benth.) C.Y.Wuet Hsuen coarse powder obtains extracting solution with ethanol or acetone reflux, extract,, with active carbon or petroleum ether decolouring (chlorophyll), the decompression precipitation obtains extractum, extract again with ethyl acetate, extract passes through silica gel column chromatography, increase progressively eluting with chloroform-acetone, wherein obtain target product Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element in chloroform-acetone (10: 1) eluent, slough solvent and just obtain colourless needle shape Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element.
2, the pharmacodynamic experiment that carries out immunosuppressive action with Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element and Tripterygium glycosides see the following form 1, table 2.
Table 1 Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element and Tripterygium glycosides
Influence to concanavalin A (ConA) inducing mouse spleen lymphocyte proliferation
Group concentration (mg/L)
0.001 0.01 0.1 1 10 100
SI?0.237±0.046
**Δ 0.258±0.022
**ΔΔ 0.303±0.027
** 0.214±0.033
**Δ 0.199±0.019
**Δ 0.204±0.025
**ΔΔ
L 0.300±0.040
** 0.297±0.027
*Δ 0.302±0.024
** 0.236±0.023
** 0.224±0.022
** 0.229±0.039
**
D 0.408±0.092 0.371±0.027
* 0.300±0.042
** 0.273±0.037
** 0.286±0.057
** 0.279±0.030
**
ConA is simple to stimulate 0.534 ± 0.131
The same, decompose
Group concentration (mg/L)
0.001 0.01 0.1
Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element (SI) 0.237 ± 0.046
*Δ 0.258 ± 0.022
*Δ Δ 0.303 ± 0.027
*
Tripterygium glycosides (L) 0.300 ± 0.040
*0.297 ± 0.027
*Δ 0.302 ± 0.024
*
Cosolvent (DMS0) 0.408 ± 0.092 0.371 ± 0.027
*0.300 ± 0.042
*
ConA is simple to stimulate 0.534 ± 0.131
Group concentration (mg/L)
1 10 100
Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element (SI) 0.214 ± 0.033
*Δ 0.199 ± 0.019
*Δ 0.204 ± 0.025
*The Δ Δ
Tripterygium glycosides (L) 0.236 ± 0.023
*0.224 ± 0.022
*0.229 ± 0.039
*
Cosolvent (DMS0) 0.273 ± 0.037
*0.286 ± 0.057
*0.279 ± 0.030
*
ConA is simple to stimulate 0.534 ± 0.131
* expression is compared with the simple stimulating group of ConA, P＜0.05, and * * represents to compare P＜0.01 with the simple stimulating group of ConA; Δ is represented to compare with the DMS0 of same concentrations, P＜0.05, and the Δ Δ is represented to compare P＜0.01 with the DMS0 of same concentrations.
The result shows that Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element (0.001mg/L, 0.01mg/L, 1mg/L, 10mg/L, 100mg/L) and Tripterygium glycosides (0.01mg/L) can significantly suppress the inductive mice spleen lymphocytes proliferation of ConA, have the cellular immunization inhibitory action.
Table 2 Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element and Tripterygium glycosides
Influence to lipopolysaccharide (LPS) inducing mouse spleen lymphocyte proliferation
Group concentration (mg/L)
0.001 0.01 0.1 1 10 100
SI?0.211±0.041
**?0.194±0.025
** 0.208±0.011
** 0.185±0.035
** 0.218±0.022
** 0.163±0.014
**
L 0.325±0.039 0.225±0.061
** 0.231±0.042
** 0.247±0.016
** 0.185±0.020
** 0.181±0.019
**
LPS is simple to stimulate 0.321 ± 0.010
The same, decompose
Group concentration (mg/L)
0.001 0.01 0.1 1
Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element (SI) 0.211 ± 0.041
*0.194 ± 0.025
*0.208 ± 0.011
*0.185 ± 0.035
*
Tripterygium glycosides (L) 0.325 ± 0.039 0.225 ± 0.061
*0.231 ± 0.042
*0.247 ± 0.016
*
LPS is simple to stimulate 0.321 ± 0.010
Group concentration (mg/L)
1 10 100
Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element (SI) 0.185 ± 0.035
*0.218 ± 0.022
*0.163 ± 0.014
*
Tripterygium glycosides (L) 0.247 ± 0.016
*0.185 ± 0.020
*0.181 ± 0.019
*
LPS is simple to stimulate 0.321 ± 0.010
*Expression is compared with the simple stimulating group of LPS, P＜0.05,
*Expression is compared P＜0.01 with the simple stimulating group of ConA.
The result shows that Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element (0.001mg/L, 0.01mg/L, 0.1mg/L, 1mg/L, 10mg/L, 100mg/L) and Tripterygium glycosides (0.01mg/L) can significantly suppress the inductive mice spleen lymphocytes proliferation of LPS, have the humoral immunization inhibitory action.
Claims (1)
1, Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second element is characterized in that as the application of immunosuppressant: the plain application as preparation treatment autoimmune disease medicine of Isodon amethystoides (Benth.) C.Y.Wuet Hsuen second.
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| CN 03113364 CN1254238C (en) | 2003-04-29 | 2003-04-29 | Use of Wangzaozi secondary element as immunological inhibitors |
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| CN 03113364 CN1254238C (en) | 2003-04-29 | 2003-04-29 | Use of Wangzaozi secondary element as immunological inhibitors |
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| CN1254238C CN1254238C (en) | 2006-05-03 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018153235A1 (en) | 2017-02-23 | 2018-08-30 | 苏州沪云肿瘤研究中心股份有限公司 | Glaucocalyxin a derivative, pharmaceutically acceptable salt thereof, or pharmaceutical composition thereof and uses thereof in preparation of drugs for treating psoriasis |
| CN110063949A (en) * | 2019-05-14 | 2019-07-30 | 大连理工大学 | Common rabdosia leaf B prime is preparing the purposes in the drug for treating lung cancer |
| CN110507698A (en) * | 2019-09-04 | 2019-11-29 | 淮北师范大学 | A kind of agent of common rabdosia leaf extract particles and preparation method of anti-mycobacterium tuberculosis |
| CN111888389A (en) * | 2020-08-28 | 2020-11-06 | 宿州绿源中医药科技有限公司 | A semen Ziziphi Spinosae extract for treating interstitial pneumonia, and its preparation method |
| CN111956683A (en) * | 2020-08-28 | 2020-11-20 | 宿州绿源中医药科技有限公司 | A semen Ziziphi Spinosae extract for treating tuberculosis and tuberculous chronic osteomyelitis, and its preparation method |
-
2003
- 2003-04-29 CN CN 03113364 patent/CN1254238C/en not_active Expired - Lifetime
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018153235A1 (en) | 2017-02-23 | 2018-08-30 | 苏州沪云肿瘤研究中心股份有限公司 | Glaucocalyxin a derivative, pharmaceutically acceptable salt thereof, or pharmaceutical composition thereof and uses thereof in preparation of drugs for treating psoriasis |
| US11406622B2 (en) | 2017-02-23 | 2022-08-09 | Suzhou Pharmavan Co., Ltd. | Glaucocalyxin a derivative, pharmaceutically acceptable salt thereof, or pharmaceutical composition thereof and uses thereof in preparation of drugs for treating psoriasis |
| CN110063949A (en) * | 2019-05-14 | 2019-07-30 | 大连理工大学 | Common rabdosia leaf B prime is preparing the purposes in the drug for treating lung cancer |
| CN110507698A (en) * | 2019-09-04 | 2019-11-29 | 淮北师范大学 | A kind of agent of common rabdosia leaf extract particles and preparation method of anti-mycobacterium tuberculosis |
| CN111888389A (en) * | 2020-08-28 | 2020-11-06 | 宿州绿源中医药科技有限公司 | A semen Ziziphi Spinosae extract for treating interstitial pneumonia, and its preparation method |
| CN111956683A (en) * | 2020-08-28 | 2020-11-20 | 宿州绿源中医药科技有限公司 | A semen Ziziphi Spinosae extract for treating tuberculosis and tuberculous chronic osteomyelitis, and its preparation method |
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| CN1254238C (en) | 2006-05-03 |
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