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CN111298074A - 一种预防和改善冠心病的心脏保护类的植物草药制剂 - Google Patents

一种预防和改善冠心病的心脏保护类的植物草药制剂 Download PDF

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CN111298074A
CN111298074A CN201811510367.2A CN201811510367A CN111298074A CN 111298074 A CN111298074 A CN 111298074A CN 201811510367 A CN201811510367 A CN 201811510367A CN 111298074 A CN111298074 A CN 111298074A
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heart disease
coronary heart
dried pulp
walnut
stone
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宋元达
赛德侯赛因
李少琦
杨武
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Shandong University of Technology
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Priority to PCT/CN2019/121061 priority patent/WO2020119453A1/zh
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Abstract

本发明提供了一种新的天然植物草药制剂，基于20种植物部分提取物的协同作用。它可以预防和治疗各种冠心病风险因子，包括引起心血管事件的血管炎症过程。植物提取物为以下部分：丹参鼠尾草、胡桃草、欧洲七叶树和姜的根，中国肉桂的树皮，芝麻、番木瓜、黑种草、石榴的种子，欧矢车菊的叶子，乳香黄连木树脂，椰子树的核果，可可豆，海枣的干果肉和核，油橄榄、无花果、核桃、蓝莓的干果肉，蒜瓣和蔷薇花瓣。本发明用70％乙醇在70‑80℃下处理上述植物部分并保持溶液的pH值在7‑10之间，使用色谱法和光谱法分离活性化合物并检测植物提取物的分子表征。该配方已经过试验证明具有降血脂、抗肥胖、抗动脉粥样硬化、抗氧化、抗焦虑和降低半胱氨酸的作用。该试验药物还可以改善内皮功能障碍，因此建议将其作为预防/减少不良心脏疾病的有效补救措施。

Description

一种预防和改善冠心病的心脏保护类的植物草药制剂
技术领域
本发明涉及新型天然植物草药制剂。具体涉及一种预防和改善诱发冠心病或中风的各种危险因子的方法。
背景技术
心血管疾病是发展中国家和发达国家死亡的主要原因。据世界卫生组织报告，到2020年，心脏病将成为导致残疾和死亡的主要原因。最常见的心血管疾病是冠心病，每年造成358,000多人死亡，每年花费1089亿美元。心血管疾病的诱因包括高血压，焦虑，压力，吸烟，高低密度脂蛋白胆固醇，糖尿病，超重/肥胖，不良饮食，缺乏运动和过量饮酒。尽管人们对心血管健康的补充替代医学越来越关注，但关于心血管疾病的补充替代医学的使用模式的文献较少。过去的许多研究证明，通过降低血脂水平和控制高血压，可以最大限度地减少冠心病的发病。
有大量证据证明高胆固醇血症和高甘油三酯血症会导致动脉粥样硬化，冠心病和中风。高血清胆固醇，低密度脂蛋白胆固醇和较低的高密度脂蛋白胆固醇都是导致冠心病和动脉粥样硬化发生的重要因素。高浓度的甘油三酯，小密度低密度脂蛋白胆固醇和低水平的高密度脂蛋白胆固醇被称为血脂异常，并且该过程会导致胰岛素抵抗。胰岛素抵抗综合征的特征包括许多心血管疾病诱因，如中心性肥胖，高血糖，高血压，血脂异常以及促凝血因子和炎症标志物。研究表明，通过适当管理高胆固醇血症，糖尿病患者的冠心病发生率显着减少。
急性期反应物循环细胞因子，高敏C反应蛋白，血清白蛋白和纤维蛋白原是冠心病发作和复发性急性心肌梗死的预测因子。一些研究表明，同型半胱氨酸升高在心血管疾病患者中很常见，并且极大可能会导致心脏疾病的发生。
叶酸缺乏会引起同型半胱氨酸的升高，而同型半胱氨酸的升高与心血管疾病的风险增加有关。其中一项实验研究表明，叶酸耗竭引起的高同型半胱氨酸血症会增加动脉通透性和僵硬度。升高的同型半胱氨酸水平的位置效应导致血管内皮细胞的氧化损伤，平滑肌细胞的增殖增加和动脉粥样硬化的低密度脂蛋白胆固醇高氧化。因此，它导致内皮功能障碍。同样，增加的高敏C反应蛋白在动脉粥样硬化的发病机理中起主要作用。高敏C反应蛋白和其他炎症敏感蛋白主要与斑块形态的变化和破裂和急性血栓形成有关。
研究人员已经在心力衰竭患者中证实了循环细胞因子水平升高。白细胞介素-6浓度与左心室功能障碍的严重程度和交感神经和肾素 - 血管紧张素系统的活化程度有关。因此，白细胞介素-1，IL-6和肿瘤坏死因子α的细胞因子会引起冠心病。白细胞介素-6是遗传决定的，它的水平决定了动脉粥样硬化，血栓形成和冠心病的风险。
脂联素也与血压，心率，总胆固醇，低密度脂蛋白胆固醇和甘油三酯呈负相关，与HDL-c呈正相关。研究人员认为高敏C反应蛋白，纤维蛋白原，脂蛋白和同型半胱氨酸是用于评估冠心病风险的重要生物标志物，即使在具有冠心病常规危险因素的强家族史的无症状个体中也是如此。
最近，一些生物标志物正在出现用于诊断和治疗心脏病如心肌肌钙蛋白的病理生理学，β型利钠肽是一种会引起心脏舒张的32-氨基酸反调节肽释放的物质。β型利钠肽值与年龄和急性冠状动脉综合征病例有很强的相关性。β型利钠肽升高是造成中风、阻塞性睡眠呼吸暂停、糖尿病、左侧房室性肥厚的原因。 3CD40是一种信号蛋白，它会在急性冠状动脉综合征中显着升高。
心理社会压力也在动脉高血压，心绞痛和心肌梗塞沉淀的发生中起重要作用。抑郁症是冠心病发展的独立危险因素。因此，压力管理有助于预防不良心脏事件。减少肥胖指数也有助于降低冠心病的发病率。
许多合成的常规药物疗法被用于诸如抗高血压药，抗心律失常药，降血脂药，抗糖尿病药，抗肥胖药，但它们的应用受到限制，长期使用会对生物系统产生不利影响。
发明内容
本发明提供了一种新的天然植物草药制剂，它可以预防和控制各种冠心病风险因子，包括引起心血管事件的血管炎症过程，包括70％乙醇提取植物的下列部分; 即，丹参鼠尾草、胡桃草、欧洲七叶树和姜的根，中国肉桂的树皮，芝麻、番木瓜、黑种草、石榴的种子，欧矢车菊的叶子，乳香黄连木树脂，椰子树的核果，可可豆，海枣的干果肉和核，油橄榄、无花果、核桃、蓝莓的干果肉，蒜瓣和蔷薇花瓣。
本发明还提供了一种制备植物制剂的新方法，该方法包括以下步骤：用70％乙醇在70-80℃下处理上述植物部分（表1）并保持溶液的pH值在7-10之间，使用波层色谱法，高效液相色谱法分离活性化合物，使用红外光谱和核磁共振检测植物提取物的分子表征。预防和控制各种冠心病风险因子。
表1：
<i>序列</i> 学名 组织部位 mg
<i>1</i> 丹参鼠尾草 根 20
<i>2</i> 欧矢车菊 叶 20
<i>3</i> 中国肉桂 树皮 10
<i>4</i> 胡桃草 根 10
<i>5</i> 欧洲七叶树 根 20
<i>6</i> 芝麻 种子 10
<i>7</i> 乳香黄连木 树脂 10
<i>8</i> 椰子树 核果 10
<i>9</i> 番木瓜 种子 10
<i>10</i> 黑种草 种子 20
<i>11</i> 海枣 干果肉和核 各10
<i>12</i> 核桃木 干果 10
<i>13</i> 可可 豆子 10
<i>14</i> 油橄榄 干果肉 10
<i>15</i> 无花果 干果 10
<i>16</i> 蓝莓 干果肉 10
<i>17</i> 石榴 种子 10
<i>18</i> 大蒜 蒜瓣 10
<i>19</i> 姜 根 10
<i>20</i> 突厥蔷薇 花瓣 10
[有益效果]
本发明的有益效果：本发明涉及新型植物制剂及其治疗和控制诱发冠心病或中风的各种诱因的方法。本发明的制剂用于治疗和控制血脂异常，肥胖，高血压，葡萄糖耐受不良，高半胱氨酸血症，血管炎症以及焦虑和压力。
【具体实施方式】
1提取
用去离子水彻底洗涤样品以除去任何污染物，在液氮的帮助下研磨制备粗粉末，然后用单独的乙醇，甲醇，丙酮和水提取。溶剂的选择基于它们的极性，从高到低（即水>甲醇>乙醇>丙酮），因为不同类别的生物活性化合物对不同极性的溶剂具有不同的亲和力。
为了提取，将等份的粗粉末（5g）精确称量到四个250mL烧瓶中，并与50ml乙醇，甲醇，丙酮和水一起以1:10的比例摇动过夜（16-20h）。室内温度。过夜摇动后，将所有样品以4000rpm离心10分钟，然后通过定性滤纸真空过滤上清液。然后将残余物分别再重浮于另外50ml乙醇甲醇，丙酮和水中。该过程重复两次。将合并的滤液转移到预先称重的玻璃板中，通过在40℃的热空气烘箱中放置4小时来蒸发有机溶剂，之后使用冷冻干燥装置进行滤液的冷冻干燥。冷冻干燥后，记录样品的干重并储存在-80℃下以备进一步使用。
2受试者
共有112名具有心血管病症的符合条件的受试者，随机分为两组：PHF治疗组（n = 78）和安慰剂组（n = 34） - 每日一次，含500 mg（一粒胶囊）持续12周。
3入选标准
纳入标准为35-72岁，肥胖（BMI×30 kg m-2），诊断为2型糖尿病，缺血性心脏病或高血压或高胆固醇血症或血管炎症的心血管诱因之一。
4排除标准
排除标准是对危及生命的合并症的诊断; 甲状腺疾病; 冠状动脉旁路移植术6周内;1个月内心肌梗死; 6个月内血管成形术; 左冠状动脉主干狭窄> 50％; 反应迟钝的充血性心力衰竭; 恶性不受控制的心律失常; 纯合高胆固醇血症; 严重的精神疾病; 目前酒精或药物滥用; 目前吸烟; 目前孕妇或哺乳期妇女，既往减肥手术，其他直接影响体重的病症（如铅毒性，恶性肿瘤）。
5结果
Figure 341793DEST_PATH_IMAGE002

Claims (3)

1.一种新的可以预防和控制各种冠心病风险因子的植物制剂。
2.本发明包括乙醇提取植物的下列部分：丹参鼠尾草、胡桃草、欧洲七叶树和姜的根，中国肉桂的树皮，芝麻、番木瓜、黑种草、石榴的种子，欧矢车菊的叶子，乳香黄连木树脂，椰子树的核果，可可豆，海枣的干果肉和核，油橄榄、无花果、核桃、蓝莓的干果肉，蒜瓣和蔷薇花瓣，且不局限于上述植物的各种组合搭配和提取办法。
3.根据权利要求1所述的应用，其特征在于所述的预防和控制冠心病和中风风险因子的新型天然植物草药制剂包括上述提取物。
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