Antifungal activity of magnolol and honokiol

Two neolignan compounds, magnolol (5,5'-diallyl-2,2'-dihydroxybiphenyl, 1) and honokiol (5,5'-diallyl-2,4'-dihydroxybiphenyl, 2), were isolated from the stem bark of Magnolia obovata and evaluated for antifungal activity against various human pathogenic fungi. Compound 1 and 2 showed significant inhibitory activities against Trichophyton mentagrophytes, Microsporium gypseum, Epidermophyton floccosum, Aspergillus niger, Cryptococcus neoformans, and Candida albicans with minimum inhibitory concentrations (MIC) in a range of 25-100 microg/ml. Therefore, compound 1 and 2 could be used as lead compounds for the development of novel antifungal agents.     

HPLC法测定藿香正气片厚朴酚、和厚朴酚含量

目的:建立藿香正气片的含量测定方法。方法:采用高效液相色谱法,以甲醇-水(75:25)为流动相;流速1．0 ml·min-1;检测波长294 nm。结果:厚朴酚平均回收率为99．48％,RSD为0．6％;和厚朴酚平均回收率为99．41％,RSD为0．8％。结论:该方法简便易行,结果准确可靠,适用于本品的含量测定。     

HPLC法测定胃肠舒胶囊中葛根素、橙皮苷、丁香酚、和厚朴酚、厚朴酚的含量

目的建立复方制剂胃肠舒胶囊中多种有效成分的含量测定方法.方法采用 HPLC法, Phenomenex luna C18(2)色谱柱,甲醇-水梯度洗脱分离制剂中葛根素、橙皮苷、丁香酚、和厚朴酚、厚朴酚等有效成分,并对其进行含量测定,流速 1 mL· min-1,检测波长 283 nm,柱温 25 ℃.结果葛根素、橙皮苷、丁香酚、和厚朴酚、厚朴酚的线性范围分别为 0.125～ 2.000 μ g、 0.031～ 1.020 μ g、 0.117～ 2.340 μ g、 0.142～ 2.280 μ g、 0.117～ 1.880 μ g;平均回收率分别为 100.43 %、 99.44 %、 100.37 %、 100.01 %、 99.64 %.结论该测定方法简便可行、重复性好,可用于胃肠舒胶囊中各有效成分的含量测定.     

超声辅助提取厚朴叶中厚朴酚及和厚朴酚的研究

目的研究超声辅助提取厚朴叶中厚朴酚及和厚朴酚的方法。方法采用正交实验进行提取方法的研究，用HPLC法测定厚朴酚及和厚朴酚的含量，流动相为甲醇-水-冰醋酸（85：15：0．25），流速为1．0ml／min，检测波长为294nm，柱温为23℃。结果用超声强度中等、酒精浓度100％、提取时间为24h以及料液比1：40的提取条件可很好地提取厚朴叶中的厚朴酚及和厚朴酚，和厚朴酚、厚朴酚以及总酚的提取率分别为92．15％，70．83％和85．27％；RP-HPLC方法较好，结果理想。结论研究得到了很好的超声辅助提取厚朴叶中厚朴酚及和厚朴酚的方法。     

Magnolol induces apoptosis in vascular smooth muscle

Magnolol, an active component extracted from Magnolia officinalis, has various pharmacological effects, including potent antioxidant activity. In the present study, we investigated the effect of magnolol on apoptosis in rat vascular smooth muscle cells (VSMCs), using terminal-deoxynucleotidyl-transferase-mediated deoxyuridine triphosphate nick end labelling (TUNEL) and flow cytometric analysis. Magnolol (5–20 µM) concentration-dependently induced significant VSMC apoptosis, this effect being blocked by the caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone (z-VAD-fmk, 50 µM). To study the molecular mechanism, the mitochondrial death pathway was examined. Magnolol increased caspase-3 and caspase-9 activities significantly and reduced the mitochondrial potential (_m). The levels of B-cell leukaemia/lymphoma-2 (Bcl-2), but not those of Bcl-2-associated X protein (Bax) or Bcl-x_L, were down-regulated concentration dependently by magnolol. In an animal model, balloon angioplasty-induced neointima formation was inhibited significantly by magnolol and Bcl-2 protein levels were reduced. Taken together, these results show that magnolol induces apoptosis in VSMCs via the mitochondrial death pathway. This effect is mediated through down-regulation of Bcl-2 protein levels, both in vivo and in vitro. Magnolol thus shows potential as a novel therapeutic agent for the treatment of atherosclerosis and re-stenosis.     

高效液相色谱梯度洗脱法同时测定调气丸中6个主要成分含量

目的 建立调气丸中和厚朴酚、厚朴酚、牡荆素葡萄糖苷、牡荆素鼠李糖苷、牡荆素和金丝桃苷含量的测定方法。 方法采用Venusil MP C₁₈色谱柱(200 mm×4.6 mm,5 μm),流动相:乙腈—1.0%冰醋酸溶液,梯度洗脱,流速:0.9 mL/min,柱温30 ℃。结果 和厚朴酚、厚朴酚、牡荆素葡萄糖苷、牡荆素鼠李糖苷、牡荆素和金丝桃苷分别在2.97~59.40、4.26~85.20、3.59~71.80、20.68~413.60、2.66~53.20、1.84~36.80 mg/L范围内线性关系良好;平均回收率分别为97.95%(RSD=0.98%)、98.27%(RSD=1.26%)、 98.19%(RSD=1.15%)、99.96%(RSD=0.68%)、 97.88%(RSD=1.68%)、96.93%(RSD=1.24%);精密度和重复性良好;供试品溶液在室温条件下12 h内稳定。结论 该方法操作简便,精密度、稳定性、重复性好,可同时用于调气丸中6种主要成分的含量测定。     

Ionic liquids functionalized β-cyclodextrin polymer for separation/analysis of magnolol

Ionic liquids functionalized β-cyclodextrin polymer, a mono-6-deoxy-6-(1,2-dimethylimidazolium)-β-cyclodextrin iodide polymer (ILs-β-CDCP), was synthesized as a solid-phase adsorbent coupled with high-performance liquid chromatography for separating or analyzing magnolol in drug samples. The results showed that magnolol was adsorbed rapidly on ILs-β-CDCP and eluted with methanol. Under the optimum conditions, preconcentration factor of the proposed method was 12. The linear range, limit of detection (LOD), correlation coefficient (R) and relative standard deviation (RSD) were found to be 0.02–8.00 μg/mL, 1.9 ng/mL, 0.9992 and 2.76% (n=3, c=2.00 μg/mL), respectively. The interaction between ILs-β-CDCP and magnolol was studied through the inclusion constant, FTIR and TGA analysis. This proposed method has been successfully applied to the determination of magnolol in real samples.     

正交试验优选健脾化食口服液提取工艺

目的:优选健脾化食口服液的提取工艺。方法:以干浸膏收率及和厚朴酚、厚朴酚含量为定量指标,以加水量、提取时间、醇沉浓度和提取次数为考察因素,用正交试验优选最佳提取工艺。结果:最佳提取工艺为加入药材30倍量的水,提取2次,每次1h,醇沉浓度为70%。结论:优选的最佳提取工艺稳定、可行。     

HPLC法测定厚朴温中汤不同煎液中厚朴酚的含量

目的考察用合煎、分煎方法制备的厚朴温中汤汤剂中厚朴酚含量的变化。方法建立HPLC法,采用Diamonisl C18柱;流动相为甲醇-水(70∶30);流速1mL.min-1;检测波长为294nm,分析厚朴温中汤合煎液和分煎液样品中厚朴酚的含量变化。结果厚朴温中汤分煎液中厚朴酚的平均含量等于合煎液中厚朴酚的平均含量。结论分煎液与合煎液比较,两种煎液中厚朴酚的含量无差异性。     

厚术胶囊质量标准研究

目的:建立厚术胶囊的质量标准。方法:采用薄层色谱(TLC)法对方中苍术、三七、白芍和山楂药材进行定性鉴别;采用高效液相色谱法测定厚朴中厚朴酚、和厚朴酚的含量。结果:TLC斑点清晰,阴性对照无干扰。厚朴酚与和厚朴酚的进样量分别在0.080～0.400μg(r=0.9999)、0.048～0.240μg(r=0.9999)范围内与各自峰面积积分值呈良好的线性关系;平均回收率分别为98.42%、98.34%,RSD分别为0.63%、0.90%(n=6)。结论:所建标准可有效控制厚术胶囊的质量。