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Pharmaceutical use of diacetyl diphenyl sulphone heptane in preventing and controlling chronic marrow-derived leukocythemia

A technology of diacetyl and leukemia, which is applied in the field of natural medicinal chemistry and pharmacology, and can solve the problems of single target, poor adverse reaction reversal effect, etc.

Inactive Publication Date: 2008-10-29
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] In recent years, researchers have discovered a variety of chemical reversal agents, such as verapamil (VRP), cyclosporin A (CsA), tamoxifen, etc., but most of these chemical reversal agents have a single target, and in vivo application can cause different effects. The degree of adverse reactions or poor reversal effects and other issues limit its clinical application

Method used

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  • Pharmaceutical use of diacetyl diphenyl sulphone heptane in preventing and controlling chronic marrow-derived leukocythemia

Examples

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preparation example Construction

[0016] The phenolic diphenylheptane compound 3,5-diacetyl-1-(3-methoxyl-4,5-dihydroxyphenyl)-7-(4-hydroxyl-3-methyl) involved in the present invention The extraction and preparation methods of oxyphenyl)heptane include: ultrasonic extraction of the rhizomes, tubers, leaves, and flowers of Zingiberaceae plants through alcohol water or ketone water, macroporous resin enrichment, normal phase and reverse phase silica gel column chromatography purification made. Extraction method of the present invention comprises the following steps:

[0017] (a) The rhizomes, tubers, leaves, and flowers of Zingiberaceae plants that are dried and ground by cold immersion or ultrasonic extraction with alcohol water or ketone water, and evaporate the solvent under reduced pressure to obtain an extract;

[0018] (b) Dissolve with ethanol or methanol, then go through macroporous resin column chromatography, wash with water to remove impurities, and then use alcohol-water system gradient elution to o...

Embodiment 1

[0024] Example 1 : Separation and preparation of 3,5-diacetyl-1-(3-methoxy-4,5-dihydroxyphenyl)-7-(4-hydroxyl-3-methoxyphenyl)heptane in ginger and purification method

[0025] The crude drug of ginger was collected from Luoping County, Yunnan Province, and the crude drug specimen was identified by Professor Zhang Rongping of Kunming Medical College. Dried ginger rhizomes (5.5 kg) are ground and soaked with 10 times the amount of 95% ethanol, and extracted with ultrasound for 3 hours each time. After the solvent was evaporated under reduced pressure, the macroporous resin column was chromatographed, and ethanol-water (0:100-100:0) gradient elution was used. According to the detection results of thin-layer chromatography, the fractions of the same components were combined. The fractions eluting with ethanol-water (65:35) were collected, and the solvent was evaporated under reduced pressure to obtain 3.3 g of a brown solid. They were then subjected to column chromatography on...

Embodiment 2

[0027] Example 2 : Separation and preparation of 3,5-diacetyl-1-(3-methoxy-4,5-dihydroxyphenyl)-7-(4-hydroxyl-3-methoxyphenyl)heptane in Wenyujin and purification method

[0028] The rhizome of Wenyujin is collected from the south of Ruian, Zhejiang Province, and the crude drug is identified by Professor Huang Kexin of Wenzhou Medical College.

[0029] Dried warm turmeric rhizomes (6.0 kg) are ground and soaked with 10 times the amount of 95% ethanol, and extracted with ultrasound for 3 hours each time. After the solvent was evaporated under reduced pressure, the macroporous resin column was chromatographed, and ethanol-water (0:100-100:0) gradient elution was used. According to the detection results of thin-layer chromatography, the fractions of the same components were combined. The fractions eluting with ethanol-water (65:35) were collected, and the solvent was evaporated under reduced pressure to obtain 5.1 g of a brown solid. They were then subjected to column chromat...

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Abstract

The invention relates to a drug use of diacetyl-diphenyl-heptane to prevent and cure chronic Bone marrow-derived leukemia. Specifically, the invention relates to the drug use of 3, 5-diacetyl group-1-(3- methoxyl group-4, 5-dihydroxy phenyl)-7-(4-hydroxy-3- methoxyl group phenyl) heptane and the medicinal salt thereof in the preparation of prevention and treatment of chronic Bone marrow-derived leukemia. The compound is extracted mainly from ginger, curcuma wenyujin, zedoary and other zingiberaceae plants. Pharmacological experiments are proved that the compound has potent inhibitory effect on chronic Bone marrow-derived leukemia cell strain (K562) of human and the adriamycin-resistant strain (K562 / ADR) proliferatione in vitro thereof, wherein, the value of IC50 is 34.9 plus or minus 0.6 and 50.6 plus or minus 23.5 Mum respectively.

Description

technical field [0001] The present invention relates to the fields of natural medicinal chemistry and pharmacology, in particular, the present invention relates to 3,5-diacetyl-1-(3-methoxy-4,5-dihydroxyphenyl)-7-(4- Hydroxy-3-methoxyphenyl)heptane and its pharmaceutically acceptable salts are used in the preparation of drugs for preventing and treating human chronic myelogenous leukemia. The compound was found to be effective against human chronic myelogenous leukemia cell line (K562) The drug and its adriamycin-resistant strain (K562 / ADR) have a strong inhibitory effect on in vitro proliferation, and can be expected to be used in the preparation of medicines for treating related human chronic myelogenous leukemia. Background technique [0002] Tumor multidrug resistance (MDR) refers to the fact that after a drug acts on the tumor to make it resistant, it also has cross-resistance to a variety of anti-tumor drugs that it has not been exposed to, with irrelevant structures a...

Claims

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Application Information

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IPC IPC(8): A61K31/222A61K36/9068A61P35/02C07C69/157C07C67/48
Inventor 黄可新杨雷香于荣敏宋丽艳巫秀美李校堃赵昱瞿佳
Owner WENZHOU MEDICAL UNIV
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