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Pharmaceutical applications of hq-091212

A drug and pharmaceutical technology, applied in the field of drug application of HQ-091212, can solve the problems of limited application, severe side effects, and unclear anti-tumor spectrum, and achieve the effect of improving bioavailability

Inactive Publication Date: 2011-11-30
SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the relatively large toxic and side effects of the diterpenoid lactone triptolide derivatives and the narrow therapeutic window limit its clinical application.
In the past, most of the anti-tumor efficacy studies of such derivatives were not specific, so the anti-tumor spectrum was not clear enough

Method used

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  • Pharmaceutical applications of hq-091212
  • Pharmaceutical applications of hq-091212
  • Pharmaceutical applications of hq-091212

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0035] The following examples illustrate several representative dosage forms containing HQ-091212 suitable for human use.

[0036]

[0037]

[0038]

[0039]

[0040]

[0041]

[0042]

[0043] Example of Pharmacology and Pharmacodynamics Evaluation

experiment Embodiment 1

[0045] Inhibitory effect of HQ-091212 on the proliferation of human tumor cells in vitro

[0046] method

[0047] Tumor cells were cultured in RPMI 1640 or DMEM medium (Gibco) containing 10% fetal bovine serum at 37°C, 5% CO 2. Tumor cells were inoculated in 96-well plates. After 24 hours, HQ-091212 prepared with dimethyl sulfoxide was added to make the final concentration of HQ-091212 in the medium 0.0001-100 μM; The final concentration does not exceed 0.1%. After HQ-091212 treatment for 72 hours, the culture medium was discarded and the cells were fixed with cold trichloroacetic acid. Then stained with sulforhodamine B (Sulforhodamine B, SRB) solution. After washing away the unbound SRB, use Tris to dissolve the SRB bound to the protein, measure the OD value with a microplate reader at a wavelength of 520nm, and calculate the cell growth inhibition rate with the following formula:

[0048] Inhibition rate = (OD value control well - OD value administration well) / OD val...

experiment Embodiment 2

[0055] Efficacy of oral administration of HQ-091212 on human prostate cancer PC-3 xenografted tumor in nude mice

[0056] method

[0057] Human prostate cancer PC-3 was purchased from American Type Culture Collection (ATCC).

[0058] BALB / c nude mice, ♂, 6 weeks old, were purchased from Shanghai Experimental Animal Center, Chinese Academy of Sciences. Breeding environment: SPF grade.

[0059] Nude mice were subcutaneously inoculated with PC-3 human prostate cancer cell line, the inoculation volume was 5×10 per mouse 6 cells, and then cut the nude mouse tumor tissue into 2mm 3 Square small pieces, implanted subcutaneously in 5-6 week-old nude mice, until the tumor grows to at least 100mm 3 Afterwards, the animals were randomly divided into groups HQ-091212: oral administration of 1, 3, 10 mg / kg, once a day, for 3 consecutive weeks; positive control docetaxel 15 mg / kg, intravenous injection, once a week, a total of 3 weeks . The tumor volume was measured twice a week, and ...

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Abstract

The present invention relates to the application of the diterpene lactone compound (HQ-091212) represented by formula (1) in the preparation of antitumor drugs and immunosuppressants. The pharmaceutical composition of the present invention can be made into tissues and organs beneficial to mammals The dosage form for absorption and utilization has good application prospects in the treatment of proliferative diseases such as tumors and immunosuppression.

Description

technical field [0001] The present invention relates to the application of HQ-091212 in the preparation of anti-tumor and immunosuppressive drugs, and also relates to the pharmaceutical composition used in the application containing effective dosage of HQ-091212 and conventional pharmaceutical auxiliary materials and its dosage form. Background technique [0002] The diterpene lactone triptolide derivatives are extracted from the woody vines of the genus Tripterygium in the family Euonymus. The woody vines of the genus Tripterygium in the family Euonymus are distributed in the south of the Yangtze River Basin and the southwest region. [0003] Studies in the past two decades have shown that diterpenoid lactone triptolide derivatives have anti-tumor, anti-inflammatory, immunosuppressive, anti-fertility, antibacterial and other activities, especially in terms of immunosuppressive effects, diterpenoids Triptolide has strong pharmacological activity. [0004] Diterpenoid lacto...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/585A61P35/00A61P37/00A61P37/06A61P35/02
Inventor 秦继红
Owner SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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