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加味塔布森-2提取工艺优化及其对破骨细胞分化的抑制作用                                                                  Δ


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        郭 姝 ,宋清翔,董 睿,封千喜,薛培凤,董 馨(内蒙古医科大学药学院,呼和浩特 010110)
        中图分类号 R965;R283          文献标志码 A          文章编号     1001-0408(2022)16-1943-07
        DOI  10.6039/j.issn.1001-0408.2022.16.05

        摘  要   目的 优化蒙药加味塔布森-2(MT-2)的提取工艺,并考察按最优工艺所制提取物对破骨细胞分化的抑制作用。方法 采用
        网络药理学方法筛选MT-2工艺优化的指标性成分;以上述指标性成分的度值和含量计算综合评分,在单因素实验的基础上,使用
        Box-Behnken设计-响应面法优化MT-2的提取工艺并验证。以核因子κB受体激活蛋白配体(100 ng/mL)诱导RAW264.7细胞以制
        备破骨细胞分化模型,考察按最优工艺所制MT-2提取物(18.6、37.2、74.4 ng/mL)对破骨细胞分化的抑制作用。结果 网络药理学
        筛选所得指标性成分包括绿原酸、松脂醇二葡萄糖苷、异绿原酸A、1,5-二咖啡酰奎宁酸、羟基红花黄色素A、人参皂苷Rg1、人参皂
        苷Rb1。MT-2最优提取工艺为乙醇体积分数60%,料液比1 ∶ 14(g/mL),提取时间94 min,提取2次;3次验证实验所得平均综合评
        分为95.50,与预测值(95.75)的相对误差为-0.26%。与破骨分化模型细胞比较,经最优工艺所制MT-2提取物处理后的细胞多为
        单核圆形细胞,破骨细胞数量均显著减少(P<0.05),且这种抑制作用有随药物质量浓度增加而增强的趋势。结论 优化的MT-2
        提取工艺稳定、可行;所得提取物可抑制破骨细胞分化。
        关键词 加味塔布森-2;蒙药;提取工艺;Box-Behnken设计-响应面法;破骨细胞分化;抑制作用

        Optimization of the extraction technology of modified Tabusen-2 and its inhibitory effects on osteoclast
        differentiation
        GUO Shu,SONG Qingxiang,DONG Rui,FENG Qianxi,XUE Peifeng,DONG Xin(School of Pharmacy,Inner
        Mongolia Medical University,Hohhot 010110,China)

        ABSTRACT    OBJECTIVE To optimize the extraction technology of modified Tabusen-2(MT-2),and to investigate inhibitory
        effects of the extract obtained by the optimal technology on osteoclast differentiation. METHODS The index components of MT-2
        process optimization were selected by using network pharmacology. Based on single factor tests,the extraction technology of MT-2
        was optimized by Box-Behnken design-response surface methodology according to the comprehensive score of contents of above
        index components,and then validated. RAW264.7 cells were induced by receptor activator of nuclear factor-κB ligand(100 ng/mL)
        to prepare osteoclast differentiation model. Inhibitory effects of MT-2 extract(18.6,37.2,74.4 ng/mL)obtained by the optimal
        technology on osteoclast differentiation were investigated. RESULTS The index components screened by network pharmacology
        included chlorogenic acid,terpineol diglucoside,isochlorogenic acid A,1,5-dicaffeoylquinic acid,hydroxysafflower yellow A,
        ginsenoside Rg1 and ginsenoside Rb1. The optimal extraction technology of MT-2 was ethanol volume fraction of 60% ,the
        solid-liquid ratio of 1 ∶ 14(g/mL),extraction time of 94 min and extraction times of twice. The average comprehensive score
        obtained by the three validation experiments was 95.50,and the relative error with the predicted value(95.75)was -0.26%.
        Compared with osteoclastic differentiation model cells,the cells treated with MT-2 extract prepared by the optimal technology were
        mostly mononuclear round cells,and the number of osteoclasts decreased significantly(P<0.05),its inhibitory effects tended to
        strengthen with the increase of drug concentration. CONCLUSIONS The optimal extraction technology of MT-2 is stable and
        feasible. Obtained extract can inhibit osteoclast differentiation.
        KEYWORDS     modified Tarbson-2; Mongolian medicine; extraction technology; Box-Behnken design-response surface
        methodology;osteoclast differentiation;inhibitory effect


            蒙药加味塔布森-2(modified Tabusen-2,MT-2)是我           材打粉混合而成的散剂,患者用药依从性差,加之方中
        国蒙古族治疗骨科疾病的传统验方,由蓝刺头、杜仲、红                          各味药材未经提取,不利于有效成分的吸收。复方制剂
        花、三七、珍珠5味药材构成,用于治疗骨质疏松、软组织                         所含成分复杂,且具有多成分、多靶点协同起效的特
        挫伤等,具有良好的临床疗效             [1-2] 。MT-2 原剂型是以药       点 [3-4] 。既往关于复方提取工艺优化的研究大多未能将
           Δ 基金项目 国家自然科学基金资助项目(No.81960758);国家大            有效成分含量与药效关联起来,对提取工艺优劣的评价
                                                                                       [5]
        学生创新创业训练计划项目(No.202010132003);内蒙古自治区大学             过于片面,造成成分与疗效脱节 。因此,开展 MT-2 成
        生创新创业训练计划项目(No.202110132029)                       分、疗效、提取工艺的关联研究,对阐明 MT-2 的治疗作
           *第一作者 硕士研究生。研究方向:中蒙药物质基础及质量控
                                                           用至关重要。为此,本研究拟借助网络药理学方法,挖
        制。E-mail:54257065@qq.com
                                                           掘MT-2方中的有效成分,并以此作为MT-2提取工艺优
           # 通信作者 实验师,硕士生导师,硕士。研究方向:中蒙药物质基
        础及质量控制。电话:0471-6653162。E-mail:dongx1128@163.com    劣的评价指标,采用Box-Behnken设计-响应面法考察各


        中国药房    2022年第33卷第16期                                            China Pharmacy 2022 Vol. 33 No. 16  ·1943 ·
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