CN114469935B - 母菊内酯酮的应用 - Google Patents
母菊内酯酮的应用 Download PDFInfo
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- 239000003814 drug Substances 0.000 claims abstract description 11
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- 235000015459 Lycium barbarum Nutrition 0.000 claims abstract description 9
- 239000008280 blood Substances 0.000 abstract description 5
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- 230000003285 pharmacodynamic effect Effects 0.000 abstract description 2
- 210000004027 cell Anatomy 0.000 description 14
- 238000011282 treatment Methods 0.000 description 9
- QONYNSMAVSRIRD-UPQAZBFISA-N Matricarin Chemical compound [C@@H]1([C@H](CC(C)=C2C(=O)C=C(C)[C@@H]22)OC(C)=O)[C@@H]2OC(=O)[C@H]1C QONYNSMAVSRIRD-UPQAZBFISA-N 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 6
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 5
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 5
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 5
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 5
- 239000005642 Oleic acid Substances 0.000 description 5
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 5
- 150000002632 lipids Chemical class 0.000 description 5
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 5
- FXEJLRKTIPQDPO-UHFFFAOYSA-N 8alpha-Acetoxyachillin Natural products CC1C2C(CC(=C3C(=O)C=C(C)C3(C)C2OC1=O)C)OC(=O)C FXEJLRKTIPQDPO-UHFFFAOYSA-N 0.000 description 4
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- 108010023302 HDL Cholesterol Proteins 0.000 description 3
- 108010028554 LDL Cholesterol Proteins 0.000 description 3
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- HATRDXDCPOXQJX-UHFFFAOYSA-N Thapsigargin Natural products CCCCCCCC(=O)OC1C(OC(O)C(=C/C)C)C(=C2C3OC(=O)C(C)(O)C3(O)C(CC(C)(OC(=O)C)C12)OC(=O)CCC)C HATRDXDCPOXQJX-UHFFFAOYSA-N 0.000 description 2
- 239000013592 cell lysate Substances 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 208000029078 coronary artery disease Diseases 0.000 description 2
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- 206010003211 Arteriosclerosis coronary artery Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 235000007866 Chamaemelum nobile Nutrition 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010067125 Liver injury Diseases 0.000 description 1
- 244000042664 Matricaria chamomilla Species 0.000 description 1
- 235000007232 Matricaria chamomilla Nutrition 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
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- 208000016097 disease of metabolism Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
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- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 229940125753 fibrate Drugs 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 231100000753 hepatic injury Toxicity 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
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- 230000004054 inflammatory process Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 230000006371 metabolic abnormality Effects 0.000 description 1
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
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- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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Abstract
本发明公开了母菊内酯酮在制备治疗或预防高血脂症药物或在制备改善高血脂症保健品上的应用。本发明提供了母菊内酯酮在降血脂、治疗脂质堆积和改善脂质代谢紊乱方面的药效活性,开发了母菊内酯酮在医药方面的新用途。同时母菊内酯酮的植物来源广泛,拓展了高血脂症的用药来源。
Description
技术领域
本发明涉及母菊内酯酮的医药新用途。
背景技术
高脂血症是一种以多种脂质代谢异常为特征的代谢性疾病,主要表现为甘油三酯(Triacylglycerol,TG)、总胆固醇(Total cholesterol,TC)、低密度脂蛋白胆固醇(Lowdensity lipoprotein cholesterol,LDL-C)水平的异常升高,和/或伴随高密度脂蛋白胆固醇(High density lipoprotein cholesterol,HDL-C)水平的降低。高脂血症是诱发冠心病、动脉粥样硬化等心脑血管疾病的主要危险因素,严重威胁人民健康。西医治疗高脂血症的药物主要包括他汀类、贝特类,具有较多不良反应,如引起肝损伤、消化道反应、皮肤瘙痒等。因此寻找安全、有效副作用小的高脂血症治疗药物,具有重要的临床意义和社会价值。
菊科植物分布广泛,是主要的药用植物来源,在我国的菊科植物中,大约有300种可为药用,具有治疗肥胖、降糖、降脂、抗炎、抗氧化等药理活性。菊科植物中所含有的倍半萜内酯类化合物具有降脂、强心、抗癌、镇痛等作用,是主要的活性成分。母菊内酯酮(Matricarin)是一种天然来源的倍半萜内酯化合物,主要存在于菊科的一些可食用或药用的植物中,如洋甘菊、白花蒿和蒙古蒿。目前关于母菊内酯酮生物学活性的研究较少,且仅仅集中在抗炎和抗氧化方面,尚无文献证明母菊内酯酮的降脂活性。
发明内容
本发明拓展了母菊内酯酮的医药用途,开拓了高血脂症的用药来源。
为了达到上述目的,本发明提供的技术方案如下:
母菊内酯酮在制备治疗或预防高血脂症药物或在制备改善高血脂症保健品上的应用。
本发明提供了母菊内酯酮在降血脂、治疗脂质堆积和改善脂质代谢紊乱方面的药效活性,开发了母菊内酯酮在医药方面的新用途。同时母菊内酯酮的植物来源广泛,拓展了高血脂症的用药来源。
附图说明
图1为不同处理后HepG2细胞油红染色图;
图2为不同处理对HepG2细胞中TC的影响;
图3为不同处理对HepG2细胞中TG的影响;
图4为不同处理对HepG2细胞中HDL的影响;
图5为不同处理对HepG2细胞中LDL的影响。
具体实施方式
下面结合附图对本发明进行详细说明。
实施例1
治疗脂质堆积药效研究
HepG2细胞复苏后,采用25mL培养瓶传代,培养至80%密度,加入含有1mM OA(Oleic Acid,油酸)的培养基,培养12h,构建高脂细胞模型(Model)。成功建立模型后,加入不同剂量的母菊内酯酮(低剂量为50μM,高剂量为100μM)继续培养12小时。空白组(CON)加入等体积的DMSO作为溶剂对照。培养结束后,所有细胞均采用PBS洗涤细胞3次。采用油红对各组细胞进行染色,显微镜下观察细胞中脂滴变化情况(放大倍数×100)。结果显示,OA处理可诱导肝细胞脂质堆积,油红染色后呈现明显的红色脂滴,给予母菊内酯酮处理后(低剂量Matricarin 50μM,高剂量Matricarin 100μM),细胞内脂质堆积显著减轻,油红染色的区域显著减少。
实施例2
改善脂质代谢紊乱药效研究
HepG2细胞复苏后,采用25mL培养瓶传代,培养至80%密度,加入含有1mM OA的培养基,培养12h,构建高脂细胞模型(Model)。成功建立模型后,加入不同剂量的母菊内酯酮(低剂量为50μM,高剂量为100μM)继续培养12小时。空白组(CON)加入等体积的DMSO作为溶剂对照。培养结束后,所有细胞均采用PBS洗涤细胞3次,吸干水分后采用细胞裂解液将细胞裂解。进一步检测细胞裂解液中TC,TG,HDL和LDL的含量。结果显示,与空白组(CON)相比,OA处理后(Model)可显著诱导脂质代谢紊乱,TC、TG、LDL显著升高,HDL显著降低(P<0.05),给予不同浓度母菊内酯酮治疗后(低剂量Matricarin50μM,高剂量Matricarin 100μM),TC、TG、LDL显著降低,HDL显著增高(P<0.05)。
Claims (1)
1.母菊内酯酮在制备治疗或预防高血脂症药物上的应用,所述母菊内酯酮为治疗或预防高血脂症药物中的唯一活性成分。
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Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
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CN103977015A (zh) * | 2014-05-05 | 2014-08-13 | 南京瑞菁医药科技有限责任公司 | 中药毛菊苣降脂活性成分配伍组合物 |
CN110327323A (zh) * | 2019-08-14 | 2019-10-15 | 江苏省中国科学院植物研究所 | 菊苣酸在制备治疗肥胖症或其并发症药物上的应用 |
CN111588708A (zh) * | 2020-06-28 | 2020-08-28 | 河北中医学院 | 野艾蒿酮a在制备降糖降脂药物中的应用 |
CN111603463A (zh) * | 2020-06-28 | 2020-09-01 | 河北中医学院 | 脱氢去乙酰氧母菊素或去乙酰母菊酮素在制备降糖降脂药物中的应用 |
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CN103977015A (zh) * | 2014-05-05 | 2014-08-13 | 南京瑞菁医药科技有限责任公司 | 中药毛菊苣降脂活性成分配伍组合物 |
CN110327323A (zh) * | 2019-08-14 | 2019-10-15 | 江苏省中国科学院植物研究所 | 菊苣酸在制备治疗肥胖症或其并发症药物上的应用 |
CN111588708A (zh) * | 2020-06-28 | 2020-08-28 | 河北中医学院 | 野艾蒿酮a在制备降糖降脂药物中的应用 |
CN111603463A (zh) * | 2020-06-28 | 2020-09-01 | 河北中医学院 | 脱氢去乙酰氧母菊素或去乙酰母菊酮素在制备降糖降脂药物中的应用 |
Non-Patent Citations (1)
Title |
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CHAMOMILE AS A POTENTIAL REMEDY FOR OBESITY AND METABOLIC SYNDROME;Maria M. Bayliak等;《EXCLI Journal》;第20卷;1261-1286 * |
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