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Reversing agent for drug-fast during treating tumor with multiple medicines

A tumor cell, multi-drug resistance technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of research reports and patent disclosures that have not been seen in reversing tumor multi-drug resistance by pregnane compounds , to achieve the effect of wide application prospects

Inactive Publication Date: 2007-02-14
广州中医药大学热带医学研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There are no research reports and patent publications on the reversal of tumor multidrug resistance by pregnane compounds at home and abroad

Method used

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  • Reversing agent for drug-fast during treating tumor with multiple medicines
  • Reversing agent for drug-fast during treating tumor with multiple medicines
  • Reversing agent for drug-fast during treating tumor with multiple medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 extraction and separation

[0040] 5.0 kg of Tongguangsan coarse powder was added with 80% ethanol by volume, heated and refluxed for extraction 3 times, each time for 2 hours. The extract was collected, ethanol was evaporated under reduced pressure, water was added to form a suspension, petroleum ether was added to degrease, the liquid was separated, the aqueous phase was extracted with ethyl acetate, the organic phase was separated and concentrated under reduced pressure to obtain 146.5 g of ethyl acetate extract. Take the ethyl acetate fraction (80 g), add chloroform-methanol mixture to dissolve, perform silica gel column (particle size 200-300 mesh) chromatography, and use chloroform:methanol (100:0-0:100, volume ratio) gradient elution, The eluate was collected, the separation results were detected by TLC, similar fractions were combined, and repeated silica gel column chromatography, C-18 alkylated silica gel reverse phase column chromatography and pr...

Embodiment 2

[0042] The structure identification of embodiment 2 compound MT-1 (structural formula sees accompanying drawing, the same below)

[0043] MT-1: 17βH, R = Pachbiosyl, R 1 =Tig,R 2 = Ac

[0044] Compound MT-1, C 42 h 64 o 14 . White amorphous powder, easily soluble in chloroform, methanol, acetone and other organic solvents, insoluble in water. [α] D 25 -26.3 (c0.076, CH 3 OH), the molecular formula is C 42 h 64 o 14 , ESI-MS: m / z 815.2 ([M+Na]+), 1HNMR (400MHz, CDCl 3 , δin ppm) and 13C NMR data are shown in Table 1 and Table 3. The Liebermann reaction and Keller-Kiliani reaction of MT-1 were both positive, indicating that it may be a steroidal glycoside containing 2-deoxysugar. 13 The C NMR (DEPT) spectrum shows that it contains 42 carbon atoms, including 10 methyl groups, 8 methylene groups, 16 methine groups and 8 quaternary carbons. Combined with the analysis of the biogenic characteristics of the plant containing 21-carbon steroidal ester glycosides, the che...

Embodiment 3

[0046] The structural identification of embodiment 3 compound MT-9, MT-10

[0047] MT-9: 17βH, R=H, R 1 = Bu, R 2 = Ac

[0048] MT-10: 17βH, R=H, R 1 =Bz,R 2 = Ac

[0049] MT-9,C 28 h 42 o 7 . White powder, easily soluble in chloroform, methanol, acetone and other organic solvents, insoluble in water. [α] D 25 -9.6 (c 0.052, CH 3 OH), ESI-MS: m / z 513.1 ([M+Na] + ), 1H NMR (400MHz, CDCl 3 , δin ppm) and 13 See Table 1 and Table 3 for CNMR data. Compound MT-9 13 C NMR (DEPT) spectrum shows 28 carbon atoms, including all features of MT-8 aglycone moiety: C 21 Pregnant + Acetate + 2-Methyl-2-Butenoate. Including the C-20 keto group (δ C 210.8); Acetyl (δ C 170.7 / 20.5), 2-methyl-2-butenoate (Tiglic acid) (δ C 167.2, 138.0, 128.6, 14.4, 12.6); 8β, 14β epoxy (δ66.7 and δ71.8), etc. MT-9 1 In the H NMR spectrum, δ5.330 (1H, t, J=10.0Hz) and 5.013 (1H, d, J=10.0Hz) are 11α-, 12β-ester-substituted C 21 Steroidal 11β-H, 12α-H features; 2.988 (1H, d, J = 7.6Hz) for...

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Abstract

A pregnane compound for reversing the resistance of cancer cells to multiple medicines is a pregnane derivative, that is, the derivative of tenacigenin B or C and the derivative of dihydrosarcostin.

Description

technical field [0001] The invention relates to a new tumor cell multidrug resistance reversing agent capable of producing medicine. Specifically, it relates to a derivative of Tenacigenin B (also known as Tongguang Scattering Aglycone B, or Tongguang Scattering Aglycone B, English name Tenacigenin B), and dihydroscarptinin ( Also known as Dihydrosarcosarginin, English name Dihydrosarcostin) derivatives and Tongguang scatter aglycon C (also known as Tongguang scatter aglycon C, or Tongguang scatter aglycon C, English name Tenacigenin C) derivatives The application of natural or semi-synthetic derivatives of steroid structure in the preparation of tumor cell multidrug resistance reversal agents. Background technique [0002] Multidrug resistance (MDR) of tumor cells means that after tumor cells develop resistance to one anticancer drug, they can simultaneously develop cross-resistance to other anticancer drugs that have not been exposed to each other with different chemical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/57A61K31/704A61P35/00
Inventor 胡英杰沈小玲卢鸿龙符林春
Owner 广州中医药大学热带医学研究所
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