CN107456451A - 虾青素酯作为胰脂肪酶抑制剂的用途 - Google Patents

虾青素酯作为胰脂肪酶抑制剂的用途 Download PDF

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CN107456451A
CN107456451A CN201710799589.XA CN201710799589A CN107456451A CN 107456451 A CN107456451 A CN 107456451A CN 201710799589 A CN201710799589 A CN 201710799589A CN 107456451 A CN107456451 A CN 107456451A
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pancreatic lipase
astaxanthin ester
ester
astaxanthin
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杜希萍
邓思
黄莹
杨秋明
姜泽东
倪辉
杨远帆
黄高凌
李利君
朱艳冰
肖安风
吴昌正
蔡慧农
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Jimei University
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Jimei University
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids

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Abstract

本发明公开了虾青素酯对胰脂肪酶的抑制作用，提供了虾青素酯的一种新用途。虾青素酯作为胰脂肪酶抑制剂的用途，其特征是虾青素酯在减肥药物中的应用。

Description

虾青素酯作为胰脂肪酶抑制剂的用途
技术领域
本发明公开了虾青素酯对胰脂肪酶的抑制作用，提供了虾青素酯的一种新用途，属于医药技术领域。
背景技术
胰脂肪酶是脂肪消化所必需的酶，食物中的脂肪在胰脂肪酶的作用下发生水解，被肠道吸收后，在人体内又重新合成脂肪，作为能量储备。若胰脂肪酶的活性较高，脂肪摄入过多，容易导致人体内脂肪堆积而造成肥胖，从而引发与肥胖相关的疾病如高血脂、糖尿病等。因此，目前市场上出现了针对胰脂肪酶活性抑制的减肥药，其原理是利用胰脂肪酶抑制剂抑制胰脂肪酶的活性，降低肠道中胰脂肪酶对脂肪的催化分解作用，以减少人体对脂肪的吸收，从而达到减肥的目的。但目前市场上许多胰脂肪酶抑制剂存在副作用，如奥利司他对胰脂肪酶有着良好的抑制效果，在临床上作为抗肥胖药物已经被广泛应用，但奥利司他作为一种半合成药物，长期使用会出现胀气、腹泻、脂肪便秘等副作用。
虾青素是一种酮式类胡萝卜素，在末端环状结构中各有一个羟基(-OH)，这种自由羟基可与脂肪酸形成酯，称为虾青素酯，其疏水性和亲脂性增强。如果其中一个羟基与脂肪酸成酯，称虾青素单酯；如果两个羟基都与脂肪酸成酯，则称为虾青素双酯。关于虾青素酯作为减肥保健品的开发利用还没有相关文献报道。
发明内容
本发明的目的是提供虾青素酯作为胰脂肪酶抑制剂在制备减肥药物中的新用途。
虾青素酯作为胰脂肪酶抑制剂的用途，其特征是虾青素酯作为胰脂肪酶抑制剂在减肥药物的应用。
其中，虾青素酯对胰脂肪酶具有抑制作用。
申请人在研究虾青素酯的作用机制的过程中，发现虾青素酯对胰脂肪酶具有明显的抑制作用，而胰脂肪酶作为人体肠道中脂肪分解的催化剂，可促进脂肪的分解，分解产物在人体内重新合成脂肪而堆积，虾青素酯通过抑制胰脂肪酶的活性，可以减少人体对脂肪的摄入而达到减肥的目的。
附图说明
图1为本发明虾青素酯对胰脂肪酶的抑制作用。
具体实施方式
为了使本发明的目的、技术方案及优点更加清楚明白，以下结合附图及实施例，对本发明进行进一步详细说明。应当理解，此处所描述的具体实施例仅仅用以解释本发明，并不用于限定本发明。
实施例虾青素酯对胰脂肪酶活性的抑制率的测定
1、试剂的准备：
Buffer A的配制：准确称量12.10g Tris碱，加入900mL蒸馏水溶解，用浓盐酸缓慢滴定至pH 7.0，再加入5.55g CaCl2并搅拌均匀使其充分溶解，待溶液冷却至室温，用蒸馏水定容到1L。
Buffer B的配制：准确称量0.105g MOPS(3-(N-玛琳代)丙磺酸)，加入45mL蒸馏水使其充分溶解，再加入100μL 0.5mol/L的EDTA的NaOH(0.05mol/L)溶液，100μLNaOH(0.05mol/L)溶液，用盐酸滴定至pH 6.8，放置待溶液冷却后用蒸馏水定容至50mL。
胰脂肪酶液的配制：胰脂肪酶固体以buffer B配制成10U/mL的酶液，高速离心5min，准确称取胰脂肪酶固体0.09g充分溶解于100mL的buffer B溶液中，配制成10U/mL的酶液，冷冻离心5min，取上清液，现配现用。
底物4-硝基苯丁酸酯溶液(p-NPB溶液)的配制：准确称量12.55mg p-NPB，加入10mL二甲基亚砜溶解，配成6mmol/L的p-NPB溶液，于-20℃条件下避光保存备用。
本实施例所用的虾青素酯是从雨生红球藻中分离制备而得。
2、虾青素酯对胰脂肪酶的抑制率的测定
在6支10mL离心管中依次加入60μL的胰脂肪酶酶液、1.7mL buffer A，再分别加入系列浓度为70、50、40、30、10、5μg/mL的虾青素酯二甲亚砜溶液200μL，37℃保温15min后加入40μL底物p-NPB溶液，37℃继续反应15min后，在405nm处测定吸光值A1。
用buffer B替代酶液，在同一波长下测定其吸光值A2，用二甲基亚砜替代虾青素酯溶液，测定吸光值A3，用buffer B和二甲基亚砜分别替代酶液和虾青素酯溶液，测定吸光值A4。
以奥利司他作为阳性对照，儿茶素作为阴性对照，每组实验均测定三次平行。
抑制率按如下公式计算：
通过测定，我们得到如图1所示的结果，纵坐标表示抑制率，横坐标表示虾青素酯的质量浓度。从图中可以看出，虾青素酯对胰脂肪酶有一定的抑制作用，且随着虾青素酯浓度的增大，抑制率也随之增大。阳性对照奥利司他对胰脂肪酶的抑制活性极强，其IC50值为0.058μg/mL，是一种常见的胰脂肪酶抑制剂。阴性对照儿茶素对胰脂肪酶没有抑制作用。当虾青素酯浓度为32μg/mL时，它对胰脂肪酶的抑制率达到94.29％。通过回归曲线计算得虾青素酯对胰脂肪酶的IC50值为：4.173μg/mL。可见，虾青素酯对胰脂肪酶有较好的抑制作用，而本发明所述的测定方法能够准确的测出虾青素酯对胰脂肪酶的抑制率。
以上所述，仅为本发明较佳的具体实施方式，但本发明的保护范围并不局限于此，任何熟悉本技术领域的技术人员在本发明揭露的技术范围内，可轻易想到的变化或替换，都应涵盖在本发明的保护范围之内。因此，本发明的保护范围应该以权利要求的保护范围为准。

Claims (2)

1.虾青素酯作为胰脂肪酶抑制剂的用途，其特征在于：虾青素酯作为胰脂肪酶抑制剂在减肥药物的应用。
2.如权利要求1所述的虾青素酯作为胰脂肪酶抑制剂的用途，其特征在于：虾青素酯对胰脂肪酶具有抑制作用。
CN201710799589.XA 2017-09-07 2017-09-07 虾青素酯作为胰脂肪酶抑制剂的用途 Pending CN107456451A (zh)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101111239A (zh) * 2004-12-03 2008-01-23 富士化学工业株式会社 用于减少体内脂肪的组合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101111239A (zh) * 2004-12-03 2008-01-23 富士化学工业株式会社 用于减少体内脂肪的组合物

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