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Tanshinone derivative, preparation method and application thereof

A technology of derivatives and tanshinone, which is applied in the field of tanshinone derivatives and their preparation, can solve problems such as the preparation of angiogenesis drugs and anti-tumor drugs of tanshinone derivatives, and improve the activity of antioxidant enzymes, inhibit the release of glutamic acid, The effect of reducing the content

Active Publication Date: 2014-11-12
FENGXIAN CENT HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, the prior art does not teach that tanshinone derivatives can be used to promote the preparation of angiogenesis drugs and anti-tumor drugs

Method used

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  • Tanshinone derivative, preparation method and application thereof
  • Tanshinone derivative, preparation method and application thereof
  • Tanshinone derivative, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Effect of Tanshinone Derivatives on Vascular Depletion Induced by VRI in Zebrafish

[0049] Tanshinone derivatives (Compound 10) carried out (500 μg / ml) blood vessel recovery test on VRI (VEGFR tyrosine kinase inhibitor II, hereinafter referred to as VRI)-induced blood vessel loss zebrafish model, and the results showed that this compound was It exhibits different degrees of vascular rehabilitation activity, the highest vascular rehabilitation rate can reach 95%, and the EC50 is about 0.026μM. Such as figure 1 It was shown that low, medium and high doses of tanshinone derivatives can promote vascular recovery, the highest rate of vascular recovery can reach 95%, EC50 is about 0.026 μM, and the effect is dose-dependent. exist figure 1 Among them, compared with the blank control &p<0.01#p<0.001; compared with the model group *p<0.05, **p<0.01, ***p<0.001.

Embodiment 2

[0050] Example 2 The angiogenesis-promoting effect of tanshinone derivatives on human umbilical vein endothelial cells

[0051] Human umbilical vein endothelial cells (HUVE-12) use F-12K medium, which contains 2mM L-glutamic acid, 100U / ml penicillin and streptomycin, 100μg / ml heparin, 30μg / ml endothelial cell auxin and 10% FBS. Take the 2-5 passage cells and inoculate 96-well plates at 1×105 / ml per well. After 24 hours of normal culture, the culture medium was discarded and replaced with 0.5% FBS culture medium for pretreatment for 24 hours to achieve cell synchronization. The test was divided into negative control group, positive control group (VEGF), tanshinone derivatives group (6 dose groups, final concentrations were 1, 3, 10, 30, 100, 300 μg / L), and the control group only added 0.5% FBS and solvent, the positive control group contained VEGF at a concentration of 20 μg / L, and 6 replicate wells were set up for each group. After 48 hours of conventional culture, the cult...

Embodiment 3

[0052] Example 3 Promoting Effect of Tanshinone Derivatives on Intimal Hyperplasia in Animals with Vascular Endothelial Injury

[0053] After 40 Wistar rats, 30 of them were anesthetized, the distal end of the left femoral artery was ligated, and the proximal end was clamped with arterial forceps. A 0.035-inch elastic guide wire with rough surface was inserted into the distal end of the femoral artery, and pumped 5 times repeatedly. Then rotate the guide wire 120 degrees twice, and repeat pumping 5 times at each angle. The subcutaneous tissue and skin were sutured layer by layer, and penicillin was used locally after operation to prevent infection. After modeling, the animals were divided into 3 groups, namely high-dose and low-dose groups of tanshinone derivatives and a positive control group, respectively, intravenous injection of 3 mg / kg, 1 mg / kg of tanshinone derivatives and the same volume of solvent, 1 time / day, 14 days in total. After the test, the intimal damaged ves...

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Abstract

The present invention relates to a tanshinone derivative, a preparation method and an application thereof. The tanshinone derivative preparation method comprises: dissolving the total tanshinone effective fraction, benzaldehyde and ammonium acetate in ethanol, carrying out a stirring reaction at a temperature of 20-90 DEG C, taking the reactant, extracting to obtain the total tanshinone reactant dry extract, and purifying the reactant dry extract to obtain the tanshinone derivative. The present invention further discloses an application of the tanshinone derivative in preparation of angiogenesis promotion drugs and anti-tumor drugs. According to the present invention, the tanshinone derivative is provided, can be provided for treating ischemic cerebrovascular diseases, and had characteristics of rapid effect and safe medication; and the tanshinone derivative can be used for preparing treatment drugs of blood supply improvement and ischemic tissue rescue through angiogenesis, and preparing anti-lung cancer treatment drugs and other tumor disease treatment drugs.

Description

technical field [0001] The invention relates to a tanshinone derivative, in particular to a tanshinone derivative and a preparation method and application thereof. Background technique [0002] Angiogenesis is a complex process of generating new blood vessels by stimulating the budding of endothelial cells to form small blood vessel growth and collateral circulation in the surrounding tissue on the basis of the original vascular network. This process involves multiple steps such as degradation of vascular endothelial extracellular matrix, migration of endothelial cells to the degraded matrix, proliferation, stretching, formation of tubular structures, and production of endothelial extracellular matrix membrane. It mainly includes: degradation of vascular basement membrane in the activation phase; Activation, proliferation, migration; reconstruction of new blood vessels and vascular network is a complex process involving a variety of cells and molecules. Angiogenesis is a co...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D235/02A61K31/4184A61P35/00A61P9/10A61P9/00A61P7/02A61P19/08A61P13/12
Inventor 孙振亮
Owner FENGXIAN CENT HOSPITAL
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