CN115364147B - 具有抗氧化活性和α-葡萄糖苷酶抑制活性的大果枣提取物和其应用 - Google Patents
具有抗氧化活性和α-葡萄糖苷酶抑制活性的大果枣提取物和其应用 Download PDFInfo
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Abstract
提供大果枣[Ziziphus mairei Dode]果肉和种仁的植物提取物及其制备方法，以及该提取物的药物组合物，和它们在制备治疗糖尿病的药物中的应用。属于医药技术领域。本发明将干燥的大果枣果肉和种仁，分别用溶剂提取，制备得到PXS137、PXS138。经过体外DPPH清除实验和α‑葡萄糖苷酶抑制试验研究表明，大果枣果肉提取物PXS137和大果枣种仁提取物PXS138均具有很强的抗氧化活性；同时，大果枣果肉提取物PXS137对α‑葡萄糖苷酶具显著的抑制活性。本发明的大果枣提取物PXS137和PXS138为制备抗氧化、抗衰老化妆品或药物或治疗或预防糖尿病的药物或降血糖保健品提供了新的选择。
Description
技术领域：
本发明属于医药技术领域，具体地，涉及植物药技术领域，更具体地，涉及大果枣提取物及其药物组合物与其制备方法和其在制备抗氧化、抗衰老化妆品或药物或治疗或预防糖尿病的药物或降血糖保健品中的应用。
背景技术：
糖尿病是一种以高血糖为特征的临床常见代谢疾病，α-葡萄糖苷酶的活性对机体血糖水平的调节具有重要意义。α-葡萄糖苷酶属于低聚糖水解酶类，其抑制剂通过竞争性抑制小肠上皮绒毛膜上的糖苷酶的作用来减少糖类的降解，延缓糖类的消化和吸收，从而有效地降低糖尿病人餐后血糖浓度的峰值，达到控制血糖的目的。α-葡萄糖苷酶抑制剂(如阿卡波糖，付格列波糖等)是临床上广泛应用的一类口服降糖药物，现有药物易导致腹胀、腹泻、腹痛等不良反应[郅丽超,张琳依,梁馨元,夏青,程晶,任丹丹,何云海,汪秋宽.天然活性成分对α-葡萄糖苷酶抑制作用的研究进展.食品安全质量检测学报,2021,12(6):2276-2282.]。因此，新降糖药的研发是有必要的。
大果枣[Ziziphus mairei Dode]为鼠李科枣属植物，主要分布在云南的中部至西北部。迄今为止，现有技术中未见有大果枣和其提取物具有抗氧化和α-葡萄糖苷酶抑制活性的报道。
发明内容：
本发明的目的是提供大果枣提取物，其制备方法或其在制备抗氧化、抗衰老化妆品或药物或治疗或预防糖尿病的药物或降血糖保健品中的应用。
为了实现本发明的上述目的，本发明提供了如下的技术方案：
具有抗氧化活性和α-葡萄糖苷酶抑制活性的大果枣提取物，所述的大果枣提取物是由大果枣果肉和种仁提取的，包括大果枣果肉提取物PXS137和/或大果枣种仁提取物PXS138，大果枣果肉提取物PXS137是90％乙醇提取物，大果枣种仁提取物PXS138是90％乙醇提取物；其由下述方法制备而得：(a)大果枣干燥的果肉，粉碎后用90％的乙醇，60℃水浴超声提取60min，合并过滤，回收溶剂，得浸膏大果枣果肉提取物PXS137；(b)大果枣干燥的种仁，粉碎后用90％乙醇，60℃水浴超声提取60min，合并过滤，回收溶剂，得大果枣种仁提取物浸膏PXS138。
所述的大果枣提取物的制备方法，该方法包括下述步骤：(a)取大果枣干燥的果肉，粉碎后用90％的乙醇，60℃水浴超声提取60min，合并过滤，回收溶剂，得浸膏大果枣果肉提取物浸膏PXS137；(b)取大果枣干燥的种仁，粉碎后用90％乙醇，60℃水浴超声提取60min，合并过滤，回收溶剂，得大果枣种仁提取物浸膏PXS138。
药物组合物，其含有治疗有效量的所述的大果枣提取物PXS137和PXS138任其一或其组合，以及药学上可接受的载体。
所述的大果枣提取物或药物组合物在制备抗氧化、抗衰老的药物中的应用。
所述的大果枣提取物或药物组合物在制备治疗糖尿病的药物或降血糖保健品中的应用。
所述的大果枣提取物所述的药物组合物在制备抗氧化、抗衰老的化妆品中的应用。
一种抗氧化、抗衰老的化妆品，其含有所述的大果枣提取物和化妆品常用载体。
一种改善或治疗糖尿病的植物药，其含有治疗有效量的所述的大果枣提取物和药学上可接收的载体。
本发明将干燥的大果枣果肉和种仁用溶剂提取，制备得到PXS137和PXS138。PXS137和PXS138对DPPH清除实验表明，PXS137和PXS138具有较强的抗氧化活性，IC50值分别为20.9μg/mL和16.4μg/mL。PXS137和PXS138及其组合，提供了新的抗氧化、抗衰老化妆品或药物。PXS137和PXS138对α-葡萄糖苷酶抑制实验表明，PXS137具有较强的α-葡萄糖苷酶抑制活性，其IC50值为6.4μg/mL。PXS137提供了新的治疗或预防糖尿病的药物或降血糖保健品。
在本发明中，所述药物组合物中本发明提取物PXS137和PXS138的质量百分含量优选为0.1～99％，更优选为0.5～90％；所述药物组合物中药用载体和/或赋形剂的总质量百分含量优选为1～99.9％，更优选为10～99.5％。
本发明对于所述药用载体或所述赋形剂没有特殊限定，采用本领域熟知的药用载体或赋形剂即可，具体如固体、半固体或液体稀释剂，填料或药物制品辅剂中的一种或多种。在本发明中，所述药物组合物的制剂种类优选包括液体制剂、固体制剂、喷剂或雾剂；所述液体制剂优选包括注射剂、混悬剂、乳剂、溶液剂或糖浆剂；所述固体制剂优选包括片剂、胶囊剂、颗粒剂或冲剂。本发明中对于所述药物组合物的制备方法没有特殊限定，采用本领域熟知的制备方法即可。对于所述化妆品的剂型和制备方法没有特殊既定，采用本领域熟知的剂型和制备方法即可。
在本发明中，所述药物组合物的给药方式优选为注射、口服、舌下给药或粘膜透析；所述注射优选包括静脉注射、静脉滴注、肌肉注射、腹腔注射或皮下注射。
在本发明中，所述药物组合物优选以单位体重服用量的形式使用。在本发明中，所述药物组合物优选以单位体重服用量的形式使用。在本发明中，所述单位体重服用量优选为0.5～20mg/kg。
与现有技术相比，本发明具有下述的优益效果：首次对大果枣提取物开展了抗氧化活性和α-葡萄糖苷酶抑制活性评价，活性评价结果显示大果枣果肉和种仁提取物PXS137和PXS138具有较强的抗氧化活性；大果枣果肉提取物PXS137具有较强的α-葡萄糖苷酶抑制活性。本发明所述的大果枣及其提取物为原料制备抗氧化、抗衰老化妆品或药物以及制备预防和治疗糖尿病的药物和保健品，是在现有技术的基础上，采用中药制剂常规方法制备成任何药用的制剂。例如，将大果枣果肉提取物制成散剂冲服；将提取物制成片剂、胶囊剂、颗粒剂、丸剂，但这并不限制本发明的保护范围。
具体实施方式：
下面用本发明的实施例来进一步说明本发明的实质性内容，但并不以此来限定本发明。
实施例1：
PXS137的制备。
取大果枣[Ziziphus mairei Dode]干燥后的果肉样品10.8g，粉碎后用90％乙醇(0.05L)，60℃水浴超声提取60min，过滤，滤液60℃减压回收溶剂，得得浸膏(编号PXS137)0.3g。
实施例2：
PXS138的制备。
取大果枣[Ziziphus mairei Dode]干燥后的种仁样品23.1g，粉碎后用90％乙醇(0.05L)，60℃水浴超声提取60min，过滤，滤液60℃减压回收溶剂，得浸膏(编号PXS139)1.4g。
实施例3：
PXS137和PXS138体外抗氧化作用(DPPH清除实验)。
1、实验材料
DPPH、水溶性维生素E(Trolox)均购自Sigma公司。
2、实验方法
体外抗氧化作用采用DPPH自由基清除实验，将待测样品与DPPH(终浓度为100μM)混合反应，设定3个重复孔，同时设置不含药物的空白对照和水溶性维生素E(Trolox)阳性对照孔，30℃，1h，酶标仪测定OD值，检测波长为515nm，计算得到抗氧化率。
抗氧化率(％)＝(1–样品孔OD515 nm/实验对照孔OD515 nm)×100％
IC50(50％inhibitory concentration)按Reed&Muench法计算。
3、实验结果
体外抗氧化活性测试结果见表1。结果显示，PXS137和PXS138有很强的DPPH自由基清除活性，IC50值分别为20.9μg/mL和16.4μg/mL。
表1 PXS137和PXS138体外抗氧化作用
实施例4：
PXS137和PXS138对α-葡萄糖苷酶的抑制实验。
1、实验材料
α-葡萄糖苷酶、底物4-Nitrophenylα-D-glucopyranoside和阳性对照槲皮素均购自Sigma公司。
2、实验方法
将样品(终浓度50μg/mL开始梯度稀释)与酶溶液(终浓度0.025U/mL)、缓冲液、底物(终浓度1mM)顺序加入96孔酶标板，充分混匀，设置三孔重复。同时设置不含药物的空白对照和槲皮素阳性对照。37℃孵育50min，酶标仪测定405nm处的OD值，计算得出α-葡萄糖苷酶活性的抑制率。
抑制率(％)＝(1-实验孔OD405nm/空白孔OD405nm)×100％
IC50(50％concentration of inhibition)按Reed&Muench法计算。
3、实验结果
α-葡萄糖苷酶的抑制测试结果见表2。结果显示，PXS137具有较强的α-葡萄糖苷酶抑制活性，其IC50值为6.42μg/mL；PXS138无α-葡萄糖苷酶抑制活性。
表2 PXS137对α-葡萄糖苷酶酶活性抑制的IC50值
制剂实施例：
在以下制剂实施例中，选择常规试剂，并按照现有常规方法进行制剂制备，本应用例仅体现本发明所述提取物PXS137和PXS138中的至少一种能够制备成不同的制剂，对具体试剂和操作不作具体限定：
1.本发明提取物PXS137和PXS138制备成片剂：
片剂原料：取提取物PXS137和PXS138其中一种或混合10mg，乳糖180mg，淀粉55mg，硬脂酸镁5mg；
制备方法：将化合物、乳糖和淀粉混合，用丙二醇均匀湿润，把湿润后的混合物过筛并干燥，再过筛，加入硬脂酸镁，然后将混合物压片，每片重250mg，化合物含量为10mg。
2.本发明提取物PXS137和PXS138制备成胶囊剂：
胶囊剂原料：取提取物PXS137和PXS138其中一种或混合10mg，乳糖187mg，硬脂酸镁3mg；
制备方法：将提取物PXS137和PXS138与助剂混合，过筛，均匀混合，把得到的混合物装入硬明胶胶囊，每个胶囊重200mg，活性成分含量为10mg。
3.取提取物PXS137和PXS138其中一种或其混合溶于无菌注射用水中，搅拌至化合物溶解，经无菌抽滤漏斗过滤和无菌精滤后分装于安瓿中，然后低温冷冻干燥后无菌熔封，得到药物组合物粉针剂。
4.取提取物PXS137和PXS138其中一种或其混合与赋形剂按照质量比为5:1～9:1混合均匀，进行低温冷冻干燥和灭菌，得到药物组合物粉剂。
5.将提取物PXS137和PXS138中的至少一种，用DMSO溶解后，按常规方法加注射用水，精滤，灌封灭菌制成注射液，所述注射液的浓度为0.5～5mg/mL。
6.将提取物PXS137和PXS138中的至少一种，用DMSO溶解后，将其溶于无菌注射用水中，搅拌使其溶解，用无菌抽滤漏斗过滤，再无菌精滤，分装于安瓿中，低温冷冻干燥后无菌熔封，得粉针剂。
7.将提取物PXS137和PXS138中的至少一种，按常规口服液制备方法制成口服液。
制备方法：搅拌下于适当体积的重蒸馏水中每次加入一种成分，直至完全深解，然后再加入另一种成分。加水至2ml后，将该溶液在无菌过滤器上过滤，装入瓶中并按照适当的剂量分隔。
9.滴丸：提取物PXS137和PXS138 1g
聚乙二醇6000 9g
制法：提取物PXS137和PXS138 6000熔融液的制备：按上述处方量称取提取物PXS137和PXS138，加入适量无水乙醇，微热溶解后，加入处方量的聚乙二醇熔融液中(60℃水浴保温)，搅拌混合均匀，直至乙醇挥尽为止，静置于60℃水浴中保温30分钟，待气泡除尽，然后将除尽气泡的上述混匀熔融液转入贮液筒内，在保温80-85℃的条件下，控制滴速，一滴滴地滴入冷凝液中，等冷凝完全，倾去冷凝液，收集滴丸，沥净和用滤纸除去丸上的冷凝液，放置硅胶干燥器中或自然干燥即可。
10.含有提取物PXS137和PXS138的美白霜配方(W％)：
按常规制作化妆品的方法制得本发明上述配方的化妆品。
11.含有提取物PXS137和PXS138的乳剂配方(W％)：
按常规制作化妆品的方法制得本发明上述配方的化妆品。
以上所述仅是本发明的优选实施方式，应当指出，对于本技术领域的普通技术人员来说，在不脱离本发明原理的前提下，还可以做出若干改进和润饰，这些改进和润饰也应视为本发明的保护范围。
Claims (8)
1. 具有抗氧化活性和α-葡萄糖苷酶抑制活性的大果枣提取物，其特征在于所述的大果枣提取物是由大果枣果肉和种仁提取的，包括大果枣果肉提取物PXS137和/或大果枣种仁提取物PXS138，大果枣果肉提取物PXS137是90%乙醇提取物，大果枣种仁提取物PXS138是90%乙醇提取物；其由下述方法制备而得：（a）大果枣干燥的果肉，粉碎后用90%的乙醇，60℃水浴超声提取60 min，合并过滤，回收溶剂，得浸膏大果枣果肉提取物PXS137；（b）大果枣干燥的种仁，粉碎后用90%乙醇，60 ℃水浴超声提取60 min，合并过滤，回收溶剂，得大果枣种仁提取物浸膏PXS138。
2. 权利要求1所述的大果枣提取物的制备方法，其特征在于该方法包括下述步骤：（a）取大果枣干燥的果肉，粉碎后用90%的乙醇，60℃水浴超声提取60 min，合并过滤，回收溶剂，得浸膏大果枣果肉提取物浸膏PXS137；（b）取大果枣干燥的种仁，粉碎后用90%乙醇，60℃水浴超声提取60 min，合并过滤，回收溶剂，得大果枣种仁提取物浸膏PXS138。
3.药物组合物，其含有治疗有效量的权利要求1所述的大果枣提取物PXS137和PXS138任其一或其组合，以及药学上可接受的载体。
4.权利要求1所述的大果枣提取物或权利要求3所述的药物组合物在制备抗氧化、抗衰老的药物中的应用。
5.权利要求1所述的大果枣提取物或权利要求3所述的药物组合物在制备治疗糖尿病的药物中的应用。
6.权利要求1所述的大果枣提取物或权利要求3所述的药物组合物在制备抗氧化、抗衰老的化妆品中的应用。
7.一种抗氧化、抗衰老的化妆品，其含有权利要求1所述的大果枣提取物和化妆品常用载体。
8.一种改善或治疗糖尿病的植物药，其含有治疗有效量的权利要求1所述的大果枣提取物和药学上可接收的载体。
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| KR20200053016A (ko) * | 2018-11-07 | 2020-05-18 | 이효준 | 붓기 제거에 효과가 있는 식물성 천연물의 혼합 추출물을 포함하는 당뇨병의 예방 또는 치료용 약학적 조성물 및 건강 기능 식품 |
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