复方决明子口服液的制备工艺研究

目的 :用正交法优选复方决明子口服液的最佳工艺条件。方法 :以决明子中蒽醌的含量及浸出物的含量为指标 ,应用L9(3′)正交试验法优选复方决明子口服液的最佳工艺条件。结果 :最佳提取条件为 :加 1 0倍量水 ,煎煮 3次 ,每次 1 .5h。结论 :优越工艺验证表明 ,最佳提取工艺为A1 B2 C1 。说明优选工艺稳定可靠。     

大黄-黄芪组分自微乳的制备及在体肠吸收特性研究

目的 研究大黄-黄芪多组分自微乳的处方与制备工艺,评价制剂质量,并考察其大鼠肠吸收特性。方法 通过溶解度实验、油相与乳化剂和助乳化剂配伍实验及伪三元相图的绘制,筛选出最优处方组成;并从自微乳的外观、形态、粒径、稳定性等方面对自微乳进行评价。通过大鼠在体单向肠灌流实验考察自微乳的肠吸收特性。结果 自微乳处方中油相为辛酸癸酸单双甘油酯、乳化剂为聚氧乙烯蓖麻油35、助乳化剂为乙二醇。在微乳形成区选择各辅料用量,采用适宜方法加入大黄总蒽醌及黄芪总皂苷制得的组分自微乳,外观均一透明,加水分散后形成黄色乳光的微乳液,透射电镜显微镜（transmission electron microscopy,TEM）下观察到微乳分散均匀,无黏连,呈大小均一圆球形乳滴;平均粒径为（33.01±0.12）nm、多分散指数（polydispersion index,PDI）为0.10±0.02、电位为（-10.10±1.00）m V;自微乳中大黄总蒽醌和黄芪总皂苷质量分数分别为6.29、8.80 mg/g。自微乳中大黄总蒽醌在十二指肠、空肠段的吸收速率常数（Ka）及表观吸收系数（Papp）较回肠段均有显著提高;黄芪...     

炮制对何首乌中有效成分含量的影响

目的 :测定何首乌炮制前后蒽醌类和二苯乙烯苷的含量变化。方法 :大黄素对照品溶液与 0 .5 %Mg(AC) 2 显色 ,在5 10nm处以 0 .5 %Mg(AC) 2 为空白 ,测其吸收度 ;二苯乙烯苷对照溶液以 95 %乙醇稀释定容 ,在 310nm处测其吸收度。结果 :大黄素和二苯乙烯苷测定回归方程分别为Y =2 9.70X +7.95× 10 -3 ,r =0 .9993和Y =73.0 0X +0 .0 4 2 0 ,r =0 .99992。结论 :制何首乌中游离蒽醌的含量略高于生何首乌 ,而结合蒽醌的含量生何首乌则明显高于制何首乌 ;二苯乙烯苷的含量生何首乌要高于制何首乌     

虎杖提取工艺初探

对乙肝康君虎杖进行单方水提、复方水提及７０％醇提工艺比较，结果７０％醇提，总蒽酯提取率为９６．７％，大黄素提取率为９６．１％，但经回收酒精，浓缩，干燥后，总蒽酯保留率为６８．９％，大黄素保留率为６５．６％。     

不同碳源对掌叶大黄毛状根生物量和蒽醌产量的影响

目的研究不同碳源对掌叶大黄毛状根生物量和蒽醌产量的影响。方法选取3个克隆的掌叶大黄毛状根和非转化根,采用统计分析方法,对7种糖作为培养基碳源时对大黄根生物量的积累和5种蒽醌类化合物的产量的影响进行了研究。结果不同糖作为碳源对大黄根生物量积累和蒽醌产量有极显著影响。大黄根类型与糖种类互作分析显示,DH 7a与麦芽糖对于蒽醌产量来说是优势组合,而DH 5a和DH 5c在蔗糖和果糖差异不显著,非转化根在蔗糖作碳源的培养基中蒽醌产量极显著地高于其他6种糖。结论果糖作为碳源最利于大黄根培养的生物量的积累,蔗糖作为碳源时大黄根蒽醌产量最高。     

生大黄与酒炙大黄不同溶剂提取液中游离蒽醌、结合蒽醌的含量比较

目的:通过大黄不同炮制品的水煎液和甲醇提取液中结合蒽醌类化合物的含量比较研究,探索酒炙大黄泻下力缓与结合蒽醌含量的关系.方法:采用分光光度法分别测定不同炮制品水煎液、甲醇提取液中游离蒽醌、结合蒽醌的含量.结果:水煎液中,游离蒽醌生品与炮制品相差不大,但是结合蒽醌酒炙品比生品高的多;而甲醇提取液中,生品的游离蒽醌、结合蒽醌均较酒炙品高.结论:临床汤方,多为水煎,用结合蒽醌含量减少来解释酒炙大黄缓泻作用可能并不完全,酒炙大黄缓泻的真正原因可能需要从多个层次上进行探讨.     

RP-HPLC同时测定苦黄注射液中4种大黄蒽醌类成分含量

目的 :建立同时测定苦黄注射液中大黄素、大黄酸、大黄酚和大黄素甲醚 4种大黄蒽醌类成分含量的反相高效液相色谱分析方法。方法 :采用汉邦LichrospherC₁₈柱 ,流动相组成为A :1%醋酸水溶液 ,B :含 1%醋酸的80%乙腈水溶液 ,梯度洗脱 ,流速 0.8mL·min^-1,柱温 35℃ ,检测波长 254nm ,以外标法定量。结果 :苦黄注射液中 4种蒽醌类成分的平均加样回收率分别为大黄酸 98.9%、大黄素 100.5 %、大黄酚 102.5 %和大黄素甲醚 99.0 % ,线性范围分别为大黄酸 0.0875～175 μg ,大黄素 0.0825～165μg ,大黄酚 0.15 9～ 3.17μg和大黄素甲醚 0.0525～1.05μg。 结论 :本法准确可靠 ,重现性好 ,结果稳定 ,适合于苦黄注射液中这 4种蒽醌含量的分析。     

Anthraquinones As Pharmacological Tools and Drugs

Anthraquinones (9,10‐dioxoanthracenes) constitute an important class of natural and synthetic compounds with a wide range of applications. Besides their utilization as colorants, anthraquinone derivatives have been used since centuries for medical applications, for example, as laxatives and antimicrobial and antiinflammatory agents. Current therapeutic indications include constipation, arthritis, multiple sclerosis, and cancer. Moreover, biologically active anthraquinones derived from Reactive Blue 2 have been utilized as valuable tool compounds for biochemical and pharmacological studies. They may serve as lead structures for the development of future drugs. However, the presence of the quinone moiety in the structure of anthraquinones raises safety concerns, and anthraquinone laxatives have therefore been under critical reassessment. This review article provides an overview of the chemistry, biology, and toxicology of anthraquinones focusing on their application as drugs.     

HPLC测定决明子中6种游离蒽醌含量

目的建立决明子中6种游离蒽醌类成分的HPLC含量测定方法,为决明子的质量评价提供参考方法。方法采用HPLC法同时测定决明子中6种游离蒽醌类成分的含量,分别为橙黄决明素,大黄酸,决明蒽醌,大黄素,大黄酚,大黄素甲醚。色谱柱为DiamonsilTMC18色谱柱(5μm,250 mm×4.6mm);乙腈(B)-0.1%磷酸(A)梯度洗脱;流速1.0 m L/min;检测波长285 nm;柱温为室温。结果 6种游离蒽醌类成分在相应的线性范围内均呈良好的线性关系。平均回收率均在98.0%~99.6%范围内,RSD<2.0%。结论该方法准确、灵敏、高效,可用于决明子中游离蒽醌类成分的含量测定。     

Trichomonicidal activity of a new anthraquinone isolated from the roots of Morinda panamensis Seem

Trichomoniasis, caused by the protozoan parasite Trichomonas vaginalis, is the most common nonviral sexually transmitted infection worldwide. Although drug treatment is available, unpleasant side effects and increased resistance to the nitroimidazole family have been documented. Hence, there is a need for the identification of new and safe therapeutic agents against T. vaginalis. Antimicrobial activity of anthraquinone compounds has been reported by a number of authors. The genus Morinda is well known for the diversity of anthraquinones with numerous biological activities. A new anthraquinone, lucidin-ω-isopropyl ether, was isolated from the roots of Morinda panamensis Seem. The structure of the compound was determined by ¹H and ¹³C Nuclear Magnetic Resonance (NMR) analyses, in addition to comparison with literature reports. Using in vitro susceptibility assay, the half inhibitory concentration (IC₅₀) of lucidin-ω-isopropyl ether for T. vaginalis (1.32 μg/mL) was found similar to that of metronidazole concentration tested (6 μM = 1.03 μg/mL). In addition, this anthraquinone was capable of inhibiting the parasite's ability to kill HeLa cells and decreased proteolytic activity of the proteinase TvMP50 from T. vaginalis. This was associated with the decreased expression of the mp50 gene. These results demonstrate the trichomonicidal potential by lucidin-ω-isopropyl ether. Further action-mode studies are necessary to elucidate the antiparasitic mechanism of this new anthraquinone to develop a more potent antitrichomonal agent.