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Application of abietane-type diterpenoids in the preparation of medicines for preventing and/or treating thrombotic diseases

A technology for thrombotic diseases and rosinane, applied in the field of medicine, can solve the problems of high platelet reactivity, poor thrombosis inhibitory effect, large individual differences in pharmacokinetics and pharmacodynamics, etc., and achieve significant antithrombotic activity, potential The effect of clinical application value

Active Publication Date: 2021-12-21
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the large individual differences in the efficacy of drugs and the tendency to bleed at high doses, the existing antiplatelet and antithrombotic drugs have the disadvantages of a narrow safety window and may cause drug resistance (McFadyen JD, Schaff M and Peter K. Current and futureantiplatelet therapies: emphasis on preserving haemostasis. Nat Rev Cardiol. 2018; 15, 181-191)
For example, the use of aspirin still cannot completely avoid ischemic events, and its thrombus inhibitory effect is poor in an inflammatory state with a large amount of COX-2 expression, and side effects such as aspirin resistance, allergies, and gastrointestinal bleeding may occur when using this drug
Thienopyridine P2Y 12 Receptor antagonists such as clopidogrel and prasugrel need to be metabolized in vivo to produce active molecules, and their pharmacokinetics and pharmacodynamics vary greatly among individuals, and may lead to therapeutic platelet hyperresponsiveness

Method used

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  • Application of abietane-type diterpenoids in the preparation of medicines for preventing and/or treating thrombotic diseases
  • Application of abietane-type diterpenoids in the preparation of medicines for preventing and/or treating thrombotic diseases
  • Application of abietane-type diterpenoids in the preparation of medicines for preventing and/or treating thrombotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Physicochemical properties, nuclear magnetic resonance spectrum carbon ( 13 C) and mass spectrometry data are as follows:

[0049] Compound 1:C 21 h 28 o 4 ; colorless crystals; 13 C NMR (150MHz, acetone-d 6 ):δ C 37.9 (CH 2 ,C-1),19.3(CH 2 ,C-2),43.2(CH 2 ,C-3),33.5(C,C-4),62.7(CH,C-5),201.0(C,C-6),130.1(CH,C-7),138.0(C,C-8) ,124.4(C,C-9),43.3(C,C-10),145.2(C,C-11),183.9(C,C-12),133.4(C,C-13),163.0(C, C-14),26.7(CH,C-15),21.8(CH 3 ,C-16),20.9(CH 3 ,C-17),33.5(CH 3 ,C-18),26.7(CH 3 ,C-19),19.3(CH 3 ,C-20),64.3(-OCH 3 ); EIMS m / z 344[M] + .

[0050] Compound 2:C 20 h 26 o 3 ; colorless crystals; 13 C NMR (150MHz, acetone-d 6 ):δ C 34.1 (CH 2 ,C-1),18.1(CH 2 ,C-2),38.5(CH 2 ,C-3),36.3(C,C-4),144.7(C,C-5),160.3(C,C-6),179.9(C,C-7),120.8(C,C-8) ,140.1(C,C-9),40.8(C,C-10),111.9(CH,C-11),155.5(C,C-12),135.1(C,C-13),125.4(CH, C-14),27.5(CH,C-15),22.5(CH 3 ,C-16),22.5(CH 3 ,C-17),35.6(CH 3 ,C-18),27.9(CH 3 ,C-19),28.5(CH 3 ,C-20); EIMS m / z 314...

Embodiment 2

[0061] The compound described in embodiment 1 is to the effect of rabbit platelet aggregation induced by arachidonic acid (AA):

[0062] 1. Solution preparation

[0063] AA solution: add the marked volume of pure water according to the instructions, fully dissolve the prepared AA solution with a concentration of 15mM, subpackage and refrigerate (-20°C) for later use;

[0064] Test sample (compound described in Example 1) solution or reference substance (aspirin) solution: use dimethyl sulfoxide (DMSO) preparation concentration to be the test sample mother solution or reference substance mother solution of 10mg / mL, then use DMSO was used to dilute and prepare the test sample solution or reference solution of the required concentration;

[0065] Ca-free 2+ Tyrode's solution (Ca 2+ free Tyrode's buffer): containing NaCl 137mM, KCl 2.68mM, MgSO 4 ·7H 2 O 0.2mM, NaH 2 PO 4 2H 2 O 0.42mM, NaHCO 3 11.9 mM, glucose 5.05mM, EGTA0.2 mM, pH 6.5;

[0066] Tyrode's buffer (0.25%...

Embodiment 3

[0087] Compound described in embodiment 1 is to FeCl 3 Inhibition of Induced Carotid Artery Thrombosis in Rats:

[0088] 1. Solution preparation

[0089] 50%FeCl 3 Solution: Dissolve ferric chloride solid with physiological saline to prepare FeCl with a concentration of 50% (W / V) 3 solution;

[0090] Dispensing vehicle: dissolve 2.5% CMC-Na (W / V) and 0.25% Tween80 (V / V) in normal saline;

[0091] Drug solution: after fully dissolving the compounds described in Example 1 with DMSO, dilute 10 times with the above-mentioned dispensing vehicle;

[0092] 2. FeCl 3 Induced carotid artery thrombosis experiment in rats

[0093] Instrument operation: After turning on the Transonic ultrasonic blood flow meter, set zero, calibrate, and complete the unit conversion (V----mL / min);

[0094] Animal model: rats were anesthetized by intraperitoneal injection of 10% chloral hydrate (350mg / kg), fixed, fixed in supine position, cut an incision along the middle of the neck, separated the ri...

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Abstract

The invention provides the application of abietane-type diterpenoids in the preparation of medicines for preventing and / or treating thrombotic diseases, and belongs to the technical field of medicines. The abietane-type diterpenoid compound involved in the present invention has significant inhibitory activity on rabbit platelet aggregation induced by arachidonic acid, and has significant antithrombotic activity in vivo, and is prepared by using the abietane-type diterpenoid compound as an active ingredient The drug for preventing and / or treating thrombotic diseases has potential clinical application value.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to the application of abietane-type diterpenoids in the preparation of medicines for preventing and / or treating thrombotic diseases. Background technique [0002] Salvia (Salvia) is one of the famous medicinal plant groups. There are 82 species in my country, among which Hengduan Mountain is one of the three major distribution centers in the world, and its resources are extremely rich. In addition to Salvia (S.miltiorhiza), which is listed as the top grade in "Shen Nong's Materia Medica", there are more than 20 kinds of plants of this genus, such as Yunnan sage, red root grass, and purple salvia, which are used as medicines in various places. Blood stasis, cooling blood and hemostasis. Plants of the genus Salvia mainly contain diterpenoids and polyphenols, among which diterpenoids have variable structures and significant activities, and have always been an international research ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/122A61K31/343A61K31/365A61K31/05A61K31/335A61P7/02A61P9/10A61P9/00
CPCA61K31/122A61K31/343A61K31/365A61K31/05A61K31/335A61P7/02A61P9/10A61P9/00
Inventor 许刚赵金华夏凡林丽莎
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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