CN1058609C - 化合物摩鲁新(morusin)的医药用途 - Google Patents
化合物摩鲁新(morusin)的医药用途 Download PDFInfo
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- CN1058609C CN1058609C CN 94101625 CN94101625A CN1058609C CN 1058609 C CN1058609 C CN 1058609C CN 94101625 CN94101625 CN 94101625 CN 94101625 A CN94101625 A CN 94101625A CN 1058609 C CN1058609 C CN 1058609C
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- aids
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- hiv
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 22
- 208000030507 AIDS Diseases 0.000 title claims abstract description 15
- 230000005764 inhibitory process Effects 0.000 title claims description 5
- HDHRTQZSBFUBMJ-UHFFFAOYSA-N Artonin E Natural products O1C2=C3C=CC(C)(C)OC3=CC(O)=C2C(=O)C(CC=C(C)C)=C1C1=CC(O)=C(O)C=C1O HDHRTQZSBFUBMJ-UHFFFAOYSA-N 0.000 claims description 9
- XFFOMNJIDRDDLQ-UHFFFAOYSA-N morusin Chemical compound O1C2=C3C=CC(C)(C)OC3=CC(O)=C2C(=O)C(CC=C(C)C)=C1C1=CC=C(O)C=C1O XFFOMNJIDRDDLQ-UHFFFAOYSA-N 0.000 claims description 9
- WUBUWBUVAKMGCO-UHFFFAOYSA-N morusin Natural products CC(=CCC1=C(Cc2c3C=CC(C)(C)Oc3cc(O)c2C1=O)c4ccc(O)cc4O)C WUBUWBUVAKMGCO-UHFFFAOYSA-N 0.000 claims description 9
- 229930187056 morusignin Natural products 0.000 claims description 7
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 239000013078 crystal Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 abstract description 20
- 208000015181 infectious disease Diseases 0.000 abstract description 5
- 241000196324 Embryophyta Species 0.000 abstract description 3
- 240000000249 Morus alba Species 0.000 abstract description 2
- 235000008708 Morus alba Nutrition 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- DKBPTKFKCCNXNH-YWUCGUBVSA-N Kuwanon H Natural products CC(C)=CCC1=C(O)C=CC(C(=O)[C@@H]2[C@@H](C=C(C)C[C@H]2C=2C(=CC(O)=CC=2)O)C=2C3=C(C(C(CC=C(C)C)=C(O3)C=3C(=CC(O)=CC=3)O)=O)C(O)=CC=2O)=C1O DKBPTKFKCCNXNH-YWUCGUBVSA-N 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- DKBPTKFKCCNXNH-QXGWMLRCSA-N kuwanone H Chemical compound CC(C)=CCC1=C(O)C=CC(C(=O)[C@@H]2[C@H](C=C(C)C[C@H]2C=2C(=CC(O)=CC=2)O)C=2C3=C(C(C(CC=C(C)C)=C(O3)C=3C(=CC(O)=CC=3)O)=O)C(O)=CC=2O)=C1O DKBPTKFKCCNXNH-QXGWMLRCSA-N 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
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- 230000004083 survival effect Effects 0.000 description 10
- 210000004366 CD4-positive T-lymphocyte Anatomy 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 4
- 239000003085 diluting agent Substances 0.000 description 4
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- 230000003612 virological effect Effects 0.000 description 2
- 101710169336 5'-deoxyadenosine deaminase Chemical class 0.000 description 1
- 102000055025 Adenosine deaminases Human genes 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
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- -1 coumarin, pelargonin class Chemical class 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
人爱滋病(AIDS)是一种HIV病毒感染的免疫系统疾病，死亡率极高。
本发明提供的化合物可抑制人爱滋病病毒HIV的活性，以预防或治疗由爱滋病病毒HIV引起的感染，治疗爱滋病。本发明的化合物系从中药植物桑白皮中提取的化合物摩鲁新，为人爱滋病病毒HIV提供了新的抑制剂。
Description
本发明是关于化合物摩鲁新(morusin)的医药用途，特别是从中药植物桑白皮中提取的化合物摩鲁新，可抑制人爱滋病病毒HIV的活性。
为了预防或治疗由人爱滋病病毒HIV引起的感染，治疗爱滋病，曾使用过化学化合物嘧啶、吲哚类、激素化合物、腺苷脱氨基酶、AZT、肽类，植物提取物香豆素，天竺葵素类。日本曾研究过桑白皮morus alba L.的化学成分，提取、分离、鉴定过摩鲁新(morusin)，(Chem·Pharm·Bull·24(11)·1976·P2898--2900)。但用桑白皮提取物摩鲁新(morusin)抑制人爱滋病病毒HIV，预防或治疗由HIV引起的感染，治疗爱滋病则未见报导。
本发明旨在将桑白皮的提取物摩鲁新(morusin)用于抑制人爱滋病(AIDS)病毒HIV，以预防或治疗由HIV引起的感染，治疗爱滋病。
本发明的化合物摩鲁新(morusin)是从中药植物桑白皮中提取的，其分子式为C25H24O6，分子量为420，结构式为
该化合物为黄色晶体，熔点为166～168℃。易熔于氯仿、甲醇、乙酸乙酯、不熔于水。
实施例
将化合物摩鲁新(morusin)用二甲基亚砜(DMSO)溶解，配成浓度为2mg/ml的溶液A，将A液用水分别稀释成浓度不1μg/ml～1mg/ml的多组稀释液，用其浓度的10g值在图2上作横座标，取9组不同浓度的稀释液进行毒性实验。取人体淋巴T4细胞分成9组，分别加入上述9组不同浓度的稀释液培养7天，观察这9组细胞的成活率，用0～100％在图2上作纵座标，得到9个实验点，将各点连成曲线，由该曲线可以看到该化合物对细胞的毒性(图2中粗线所示)。当细胞成活率为50％时，该点的化合物浓度称为IC50。
取人体淋巴T4细胞，用人爱滋病(AIDS)病毒HIV进行感染后，分成9组，进行该化合物对HIV的抑制实验。分别加入上述9组不同浓度的稀释液培养7天，观察这9组细胞的成活率，用0～100％在图2上作纵座标，得到9个实验点，将各点连成曲线。由该曲线可以看到被HIV感染的细胞在不同浓度的化合物作用下的成活率(图2中细线所示)，当成活率为50％时，该点的化合物浓度称为EC50。意即被HIV感染的人体淋巴T4细胞在该浓度的化合物作用下的成活率为50％(未加化合物的对照组的HTV感染细胞的成活率为0％)。
表1所示数据为上述二组实验的原始数据，用该数据作出曲线图1。图1中横座标为实验化合物浓度μg/ml的10g值。值0为1μg/ml，值1为10μg/ml，值2为100μg/ml，值3为1000μg/ml。纵座标为人体淋巴T4细胞的成活率。值0表示细胞全部死亡，值50表示细胞成活率为50％，值100表示细胞成活率为100％。由粗线可以看出该化合物对细胞的毒性，由细线可以看出该化合物对爱滋病病毒HIV的抑制作用。IC/EC＝TI，表示该化合物的治疗指数。
由图1可以看出，本发明的化合物摩鲁新(morusin)的浓度在9μg/ml左右就可抑制50％的爱滋病病毒HIV。
Claims (1)
1、具有下述结构式的化合物摩鲁新(morusin)在制备抑制人爱滋病病毒HIV活性的药物中的应用，其特征是：分子式为C25H24O6，分子量为420，结构式为
为黄色晶体，熔点为166～168℃，易溶于氯仿、甲醇、乙酸乙酯，不溶于水。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 94101625 CN1058609C (zh) | 1994-02-15 | 1994-02-15 | 化合物摩鲁新(morusin)的医药用途 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 94101625 CN1058609C (zh) | 1994-02-15 | 1994-02-15 | 化合物摩鲁新(morusin)的医药用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1107152A CN1107152A (zh) | 1995-08-23 |
| CN1058609C true CN1058609C (zh) | 2000-11-22 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 94101625 Expired - Fee Related CN1058609C (zh) | 1994-02-15 | 1994-02-15 | 化合物摩鲁新(morusin)的医药用途 |
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| CN (1) | CN1058609C (zh) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101787030A (zh) * | 2010-03-09 | 2010-07-28 | 周英 | 一种抗hiv的化合物摩鲁新l的制备与应用方法 |
| CN105566340A (zh) * | 2016-01-20 | 2016-05-11 | 贵州大学 | 一种桑白皮活性成分Morusin衍生物及其应用与制备方法 |
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1994
- 1994-02-15 CN CN 94101625 patent/CN1058609C/zh not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN1107152A (zh) | 1995-08-23 |
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Owner name: WANG LIHONG Free format text: FORMER NAME OR ADDRESS: LUO SHIDE; NING BINGMEI |
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Address after: Baiyun road 650024 Yunnan city of Kunming province (No. 525 Beijing Road, Huayuan 6-3-202) Patentee after: Wang Lihong Address before: 650031 Yunnan city of Kunming province Tianjun Dian Xiang Lin Street five building 1 unit 303 Co-patentee before: Ning Bingmei Patentee before: Luo Shide |
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Granted publication date: 20001122 Termination date: 20120215 |