羊脂油对淫羊藿炮制品提取物中宝藿苷Ⅰ在大鼠体内药动学特征的影响

目的 研究炮制辅料羊脂油对淫羊藿炮制品提取物中主要活性成分宝藿苷Ⅰ在大鼠体内药动学特征的影响.方法 大鼠分别ig给予相同剂量(15 g/kg)的淫羊藿生品提取液、加热品提取液、羊脂油炙品提取液,HPLC-ESI-MS法测定大鼠宝藿苷Ⅰ血药浓度,经DAS 2.0程序处理数据,比较宝藿苷Ⅰ药动学参数.结果 3种淫羊藿炮制品提取物在血液中的达峰浓度(Cmax)、药时曲线下面积(AUC)等药动学参数大小为油炙品＞加热品＞生品,均具有统计学差异.结论 羊脂油能促进淫羊藿提取物中宝藿苷Ⅰ的口服吸收,提高其生物利用度.     

生、炙品淫羊藿不同溶剂提取物对前列腺增生小鼠干预作用的比较

目的比较淫羊藿生品和炙品的不同溶剂提取物对良性前列腺增生(BHP)小鼠模型的治疗作用。方法测定灌服淫羊藿不同提取物及羊脂油后BHP小鼠的前列腺系数,制作前列腺病理切片进行观察。同时测定不同提取物中淫羊藿苷的含有量,探究其与疗效的关系。结果与模型组相比,淫羊藿炙品水提物可显著降低前列腺增生小鼠的前列腺系数,而淫羊藿生品50%和75%乙醇提取物及羊脂油可显著增加前列腺增生小鼠的前列腺系数。病理切片显示,与模型组相比,生品水提取物和炙品水提取物可使腺上皮乳头状突起明显减少,腺上皮细胞层明显变薄;其他用药组与模型组相比无明显差异。含有量测定结果显示,淫羊藿生品水提取物中淫羊藿苷的含有量较高;淫羊藿炙品水及50%、75%乙醇提取物中的淫羊藿苷含有量相近,95%乙醇提取物中含有量较低。结论炙淫羊藿水提取物可显著降低前列腺增生小鼠模型的前列腺系数,淫羊藿苷可能为其活性成分之一。同时,羊脂油可促进小鼠前列腺增生。     

巫山淫羊藿不同炮制品中脂肪酸成分的气相色谱-质谱联用分析

目的比较巫山淫羊藿不同炮制品及辅料羊脂油中的脂肪酸成分组成和相对含量变化。方法采用索氏提取法提取脂肪酸成分,用KOH-MeOH溶液甲酯化后,用气相色谱-质谱联用技术分析脂肪酸成分的组成,面积归一化法计算成分相对含量。结果巫山淫羊藿生品、清炒品、油拌品、油炙品和羊脂油中分别检测出16、14、17、19、18种化合物,油炙品与生品比较,含量升高的组分有6个,占油炙品脂肪酸成分总量的53.10%;降低的有4个组分,占总量的34.36%。结论巫山淫羊藿不同炮制品中脂肪酸成分的组成和相对含量有较大差异,成分变化与加入羊脂油和加热均有关。     

淫羊藿生品及羊脂炙品中主成分淫羊藿苷的吸收差异比较

目的:考察淫羊藿生品与炮制品中主成分淫羊藿苷的吸收差异。方法:采用Caco-2细胞模型,用高效液相色谱法测定药物浓度,计算其表观渗透系数,研究淫羊藿生品与羊脂炙品中淫羊藿苷及单体在模型中的双向转运。结果:在淫羊藿苷浓度相同的条件下,羊脂炙品所含淫羊藿苷的吸收渗透系数明显大于生品及单体化合物。结论:初步说明淫羊藿经过羊脂加热炮制以后,能促进有效成分淫羊藿苷的吸收,这可能和炮制时加入的羊脂有关。     

淫羊藿炮制前后对正常和肾阳虚小鼠肾上腺V_C水平的影响

目的比较淫羊藿炮制前后降低正常和肾阳虚小鼠肾上腺维生素C(VC)的作用。方法采用氢化可的松建立肾阳虚模型,比较淫羊藿炮制前后对正常和肾阳虚小鼠肾上腺VC水平的影响。结果淫羊藿生品对正常小鼠未表现出显著的降低肾上腺VC水平作用,对肾阳虚小鼠仅在高剂量(3.33 g/kg)时有降低肾上腺VC水平的作用(P<0.05);淫羊藿羊脂油制品对正常小鼠在高剂量(3.33 g/kg)时表现降低肾上腺VC水平的作用(P<0.05),对肾阳虚小鼠在中剂量(1.67 g/kg)表现出降低肾上腺VC水平的作用(P<0.05),在高剂量(3.33 g/kg)时表现出显著的降低肾上腺VC水平的作用(P<0.01)。结论淫羊藿经过羊脂油炮制后其降低肾上腺VC水平作用不仅起效剂量降低,且作用强于生品。     

不同品种淫羊藿生品与炮制品中5种黄酮类成分的含量比较

目的:对不同品种淫羊藿生品与炮制品中5种主要黄酮类成分的含量进行比较。方法:采用反相高效液相色谱(RP-HPLC)方法,选取5个不同品种淫羊藿药材,同时测定羊脂炙品与生品中淫羊藿苷、朝藿定A、朝藿定B、朝藿定C、宝藿苷I的含量。结果:不同品种淫羊藿炮制品与生品比较,淫羊藿苷、宝藿苷Ⅰ的含量炮制品比生品要高,其中朝鲜淫羊藿炮制品中淫羊藿苷、宝藿苷Ⅰ的含量增加的最多,淫羊藿苷的含量增加了32.93%,宝藿苷Ⅰ的含量增加了11.50%,而朝藿定A、朝藿定B、朝藿定C的含量炮制品比生品要低。结论:淫羊藿经炮制后所含5种黄酮类成分的含量都发生了变化,提议应分别建立生品与炮制品的多黄酮成分测定质量控制标准,以完善淫羊藿生品与炮制品的质量控制。     

不同炼制温度和用量的羊脂油制淫羊藿对肾阳虚大鼠的影响

目的:考察不同炼制温度和用量的羊脂油制淫羊藿对肾阳虚大鼠的影响.方法:采用皮下注射皮质酮(CORT)建立肾阳虚大鼠模型,以淫羊藿总黄酮为阳性对照,以症状体征、动物抓力、组织病理学检查、血清睾酮含量等为评价指标,3种制淫羊藿(羊脂油炼制温度与加入量分别为250℃,30％;120℃,30％;120℃,20％)和生淫羊藿经水提取灌胃给药,考察不同样品对肾阳虚大鼠的药理作用.结果:3个炮制品均能不同程度地增强生品的温肾壮阳作用,其中以120℃,30％的制淫羊藿增强效果最佳.其作用机制可能与改善肾阳虚证大鼠下丘脑-垂体-肾上腺-胸腺(HPAT)轴病理改变和功能抑制状态有关.结论:辅料羊脂油的炼制温度影响辅料质量,进而影响饮片药效.本试验结果为进一步阐明制淫羊藿炮制原理及建立炮制辅料的国家标准提供实验数据.     

箭叶淫羊藿炮制前后对小鼠副性器官的影响

目的:观察箭叶淫羊藿炮制前后补益作用的强弱.方法:观察箭叶淫羊藿炮制前后不同提取液对去势雄性小鼠副性器官发育的影响.结果:生品和炮制品箭叶淫羊藿的水提取液和醇提液对去势小鼠副性器官的萎缩有明显的抑制作用,且生品和炮制品的作用强度无显著性差异.结论:生品和炮制品箭叶淫羊藿均具有补益作用,且作用强度无明显差异.     

淫羊藿炮制前后对小鼠血浆睾酮及附性器官的影响

对淫羊藿经羊脂油炮制可以增强温肾壮阳作用这一传统概念,用现代药理学方法予以检验。实验结果表明:生品淫羊藿无提高性机能作用,炮制品淫羊藿有明显的增强性机能作用。     

比较以不同品质的羊脂油炙淫羊藿的温肾阳作用

目的: 对比以不同品质的羊脂油炙淫羊藿对肾阳虚证小鼠的温肾阳作用。方法: 采用肌肉注射(im)大剂量氢化可的松建立肾阳虚证小鼠模型。以生品淫羊藿和不同品种(山羊、绵羊)、不同性别(公、母绵羊)、不同部位(绵羊肚子、尾巴油)的6种羊脂油炙淫羊藿为供试品以淫羊藿总黄酮为阳性对照,加设阴性和模型对照。造模同时给药,其中阴性和模型对照组小鼠ig等体积的生理盐水(N.S),阳性对照组小鼠ig淫羊藿总黄酮提取物0.46 g·kg^-1(含淫羊藿总黄酮0.23 g·kg^-1),各供试品组小鼠ig剂量相当于生药18 g·kg^-1,ig容量均为15 mL·kg^-1,1次·d^-1,连续9 d。以肾阳虚小鼠症状体征(体重、体表温度、自主活动次数),动物抓力、凝血时间,血清超氧化物歧化酶(SOD)、丙二醛(MDA)含量为指标,考察各供试品对肾阳虚证小鼠的影响。结果: 与阴性对照组比较,模型对照组小鼠体重、体表温度、自主活动、血清SOD 含量显著下降,MDA含量升高,差异均有显著性(均P<0.01),此外,抓力和凝血时间亦呈降低趋势,提示造模是成功的。与模型对照组比较,各供试品明显延缓或抑制小鼠体重下降(惟山羊油炙淫羊藿对体重减轻的抑制作用不明显),提高小鼠体表温度,增加小鼠自主活动次数,差异均有显著性(P<0.01或P<0.05);各供试品均可提高小鼠血清SOD水平、降低MDA含量,其中,以山羊油、绵羊油、肚子油、尾巴油炙淫羊藿作用显著(P<0.01或P<0.05);各供试药组小鼠抓力呈增强趋势,但无统计学显著性;除绵羊油炙淫羊藿具有延长模型小鼠凝血时间的作用趋势外,其余各组未见明显影响。与生品比,6种不同品质的羊脂油炙淫羊藿均可不同程度地改善肾阳虚证(如体重下降、自主活动减少、抓力下降)的虚弱状态,差异多具有显著性;而各炙品之间在温肾阳作用上有一定差异,但是差异多不具有显著性。结论: 炙淫羊藿炮制品温肾阳作用优于生品淫羊藿;不同品质的羊脂油对炙淫羊藿的温肾阳药效有一定影响,但差异多不具有显著性。     

榼藤子生品和炮制品总皂苷体内抗肿瘤作用

目的:考察榼藤子生品和炮制品总皂苷体内抗肿瘤作用.方法:荷瘤小鼠随机分为8组,接种后第2天给药,连续10 d,模型对照组ig以等量生理盐水,阳性对照组腹腔注射顺铂3 mg· kg -1,低、中、高剂量榼藤子生品、炮制品总皂苷组分别ig 0.25,0.5,1 g·kg-1剂量.观察榼藤子总皂苷的肿瘤抑制作用;计算抑瘤率、胸腺指数、脾指数、肝脏指数;测定血清超氧化物歧化酶(SOD)、丙二醛(MDA)水平.结果:榼藤子生品高、中、低剂量组的抑瘤率分别为58.86％,49.52％,43.45％,榼藤子炮制品高、中、低剂量组的抑瘤率分别为59.41％,48.81％,44.59％,榼藤子生品及炮制品总皂苷还能提升荷瘤小鼠血清SOD的活力,降低MDA水平.结论:榼藤子生品和炮制品总皂苷具有抗小鼠肿瘤作用,并可增强抗氧化能力.     

Pharmacokinetics-based elucidation on disparity in clinical effectiveness between varieties of Zhi Zhu Wan,a Traditional Chinese Medical formula

Aim

Zhi Zhu Wan (ZZW) is a classical Chinese medical formulation used for the treatment of functional dyspepsia that attributed to Spleen-deficiency Syndrome. ZZW contains Atractylodes Rhizome and Fructus Citrus Immaturus, the later originates from both Citrus aurantium L. (BZZW) and Citrus sinensis Osbeck (RZZW). The present study is designed to elucidate disparities in the clinical efficacy of two ZZW varieties based on the pharmacokinetics of naringenin and hesperetin.

Mehtod

After oral administration of ZZWs, blood sample was collected from healthy volunteers at designed time points. Naringenin and hesperetin were detected in plasma by RP-HPLC, pharmacokinetic parameters were processed using mode-independent methods with WINNONLIN.

Results

After oral administration of BZZW, both naringenin and hesperetin were detected in plasma, and demonstrated similar pharmacokinetic parameters. Ka was 0.384 ± 0.165 and 0.401 ± 0.159, T_1/2(ke)(h) was 5.491 ± 3.926 and 5.824 ± 3.067, the AUC (mg/L h) was 34.886 ± 22.199 and 39.407 ± 19.535 for naringenin and hesperetin, respectively. However, in the case of RZZW, only hesperetin was found in plasma, but the pharmacokinetic properties for hesperetin in RZZW was different from that in BZZW. T_max for hesperetin in RZZW is about 8.515 h, and its C_max is much larger than that of BZZW. Moreover, it was eliminated slowly as it possessed a much larger AUC value.

Conclusion

The distinct therapeutic orientations of the Chinese medical formula ZZWs with different Fructus Citrus Immaturus could be elucidated based on the pharmacokinetic parameters of constituents after oral administration.     

The effects of wine-processing on ascending and descending: The distribution of flavonoids in rat tissues after oral administration of crude and wine-processed Radix scutellariae

Ethnopharmacological relevance

Ascending and descending theory is a core principle of traditional Chinese medicine (TCM) theories. It plays an essential role in TCM clinical applications. Some TCM medicine has specific properties, which could alter the inclination and direction of their actions. The properties of the ascending and floating process of one herbal medicine are affected by means of herb processing. Wine-processing, which is sautéing with rice wine, is one of the most popular technologies of herb processing. Wine-processing increases the inclination and direction of its actions, thereby producing or strengthening their efficacy in cleaning the upper-energizer heat.Radix scutellariae, the dried roots of Scutellaria baicalensis Georgi, is a well-known TCM used for the treatment of inflammation, pyrexia, jaundice, etc. Recently, wine-processed Radix scutellariae was normally applied in clinical studies for the treatment of upper-energizer syndrome. In order to investigate the effects of wine-processing on ascending and descending of Radix scutellariae, the comparative study of distribution of flavonoids in rat tissues of triple energizers (SanJiao-upper, middle, lower jiao) after oral administration of crude and wine-processed Radix scutellariae aqueous extracts was carried out.

Materials and methods

The rats were randomly assigned to two groups and orally administered with crude and wine-processed Radix scutellariae aqueous extracts, respectively. At different pre-determined time points after administration, the concentrations of compounds in rat tissue homogenate were determined, and the main tissue pharmacokinetic parameters were investigated. Tissue pharmacokinetic parameters including AUC_0–t, t_1/2, T_max and C_max were calculated using DAS 2.0. An unpaired Student t-test was used to compare the differences in tissue pharmacokinetic parameters between the two groups. All the results were expressed as arithmetic mean±S.D.

Results

The parameters of C_max and AUC_0–t of some flavonoids in wine-processed Radix scutellariae were remarkably increased (p<0.05, p<0.01, p<0.001) in the rat upper-energizer tissues (lung and heart) compared with those of the crude group. However, in the rat middle- and lower-energizer tissues (spleen, liver and kidney), the C_max and AUC_0–t of some flavonoids were significantly decreased (p<0.05, p<0.01) compared with the crude group. The main explanation for these differences seems to the effects of wine-processing on ascending and descending theory.

Conclusions

All of these differences in the distribution of triple energizers after oral administration of crude and wine-processed Radix scutellariae aqueous extracts may lead to the increase of efficacy on the upper-energizer tissues and were in compliance with the ascending and descending theory. Therefore, wine-processing was recommended when Radix scutellariae was used for cleaning the upper-energizer heat and humidity. The obtained knowledge can be used to evaluate the impact of these differences on the efficacy of both the drugs in clinical applications and might be helpful in explaining the effects of wine-processing on ascending and descending theory.     

Comparative pharmacokinetics of swertiamarin in rats after oral administration of swertiamarin alone,Qing Ye Dan tablets and co-administration of swertiamarin and oleanolic acid

Ethnopharmacological relevance

Qing Ye Dan is a well-known herbal drug that is widely used to treat viral hepatitis in the Yi and Hani minority regions in the Yunnan province of China.

Materials and methods

An LC–MS/MS method was developed to determine the levels of swertiamarin in rat plasma. Swertiamarin and naringin (internal standard, IS) were extracted from rat plasma using solid-phase extraction (SPE) to purify the samples. The pharmacokinetics of the following different administration methods of swertiamarin in rats were studied: oral administration of swertiamarin alone, a Qing Ye Dan tablet (QYDT) and co-administration of swertiamarin and oleanolic acid, with each method delivering approximately 20 mg/kg of swertiamarin. Non-compartmental pharmacokinetic profiles were constructed by using the software DAS (version 2.1.1), and the pharmacokinetic parameters were compared using an unpaired Student's t-test.

Results

The results showed that the pharmacokinetic parameters C_max, AUC_0–∞, V_z/F and CL_z/F were significantly different (P<0.05) among the three types of swertiamarin administration.

Conclusions

The data indicate that oleanolic acid and the other ingredients present in QYDT could affect the pharmacokinetic behaviour of swertiamarin in rats.     

Pharmacokinetics of aconitine as the targeted marker of Fuzi (Aconitum carmichaeli) following single and multiple oral administrations of Fuzi extracts in rat by UPLC/MS/MS

Ethnopharmacological relevance

Fuzi, which is the processed lateral roots of Aconitum Carmichaeli. Debx and is widely distributed over the southwest provinces of China, is recognised for its anti-inflammatory and analgesic effects.

Aim of the study

The pharmacokinetic properties of Fuzi are inadequately understood. Aconitine, the primary highly toxic ingredient of Fuzi, is well known as the target marker of Fuzi. The purpose of the present study is to investigate the pharmacokinetic behaviours of aconitine in vivo following single and multiple administrations of processed Fuzi extracts and to compare the pharmacokinetic characteristics of aconitine after administrations of pure aconitine or Fuzi extracts as well as compare the difference at single dose and multiple doses. The in vitro aconitine protein binding in plasma through equilibrium dialysis was also examined.

Methods

A high performance liquid chromatography (HPLC) method was developed for the determination of aconitine in Fuzi crude extracts and a fast ultra performance liquid chromatography-tandem mass spectrometry (UPLC/MS/MS) was developed to investigate the pharmacokinetic behaviour of aconitine as the targeted marker of Fuzi.

Results

The absolute bioavailability (F %) after the administration of 0.5 mg/kg aconitine and Fuzi extract (0.118 mg/kg aconitine) in rat was 8.24 ± 2.52% and 4.72 ± 2.66%, respectively. Aconitine absorption was very fast at the t_max 30.08 ± 9.73 min for pure aconitine and 58.00 ± 21.68 min for Fuzi extract administration. Aconitine was also eliminated rapidly with a short half-life (i.v., 80.98 ± 6.40 min) and a low rate of protein bounding (23.9–31.9%). No significance was observed on all the pharmacokinetics parameters following the single and multiple doses of pure aconitine (ANOVA, p > 0.05). However, the absorption of aconitine after multiple administrations of Fuzi extract was much faster than that of a single dose (t_max: 58.00 ± 21.68 vs. 20.00 ± 8.66 min, p < 0.05), and the area under the plasma concentration–time curve (AUC) was higher than that of a single dose.

Conclusions

The pharmacokinetic behaviour of processed Fuzi was determined in this paper. The aconitine has low bioavailability. No variation in the pharmacokinetic behaviours of pure aconitine was observed after single and multiple administrations. In contrast, multiple administrations of processed Fuzi extract could result in variations in its pharmacokinetic behaviour in AUC and t_max indicating that multiple dose might increase the bioavailability of aconitine, which may result in its toxicity. In addition, aconitine has a low protein bounding (23.9–31.9%), resulting in its rapid elimination.     

苍耳子4种提取物小鼠急性毒性比较研究

目的:研究苍耳子生品和炒品的水提、醇提4种提取物对小鼠的急性毒性。方法:观察小鼠灌胃给药后的毒性反应,并计算半数致死量(LD50)。结果:苍耳子水提取物组毒性反应为静卧、竖毛、尾足发绀、震颤、呼吸抑制、间歇性惊厥、翻正反射消失、后腿抽搐等,乙醇提取物组则表现为静卧、腹式呼吸、部分竖毛、震颤、严重间歇性惊厥、跳跃、后腿抽搐,部分动物出现大小便失禁等。苍耳子炒品水提取物、炒品乙醇提取物、生品水提取物、生品乙醇提取物的小鼠灌胃给药的LD50分别为生药155.93,317.80,167.60,275.41 g.kg-1。结论:苍耳子水提取物的急性毒性明显大于乙醇提取物,而炒品和生品的毒性差异不明显。     

商陆提取物醋制前后毒性作用的比较研究

目的:提取分离获得商陆的毒性成分,并比较其醋制前后毒性的变化.方法:采用黏膜刺激性反应、小鼠腹腔炎症模型及离体巨噬细胞释放NO模型,比较商陆毒性成分醋制前后的致炎毒性变化.结果:商陆毒性成分具有显著的致炎毒性,可导致家兔眼结膜水肿、小鼠腹腔渗出液中PGE2含量升高以及巨噬细胞释放NO含量升高;经醋制后,对家兔眼结膜刺激性减弱,使小鼠腹腔渗出液中PGE2含量降低、巨噬细胞释放NO含量降低.结论:醋制法能够降低商陆毒性成分的毒性作用.     

Interactions of pharmacokinetic profile of different parts from Ginkgo biloba extract in rats

Ethnopharmacological relevance

Extracts from Ginkgo biloba L. leaves confer their therapeutic effects through the synergistic actions of flavonoid and terpenoid components, but some non-flavonoid and non-terpenoid components also exist in this extract. In the study of this paper, an investigation was carried out to compare the pharmacokinetic parameters of fourteen compounds to clarify the influences of non-flavonoid and non-terpenoid fraction (WEF) on the pharmacokinetics profile of the flavonoid fraction (FF) and the terpene lactone fraction (TLF) from Ginkgo biloba extracts.

Materials and methods

A selective and sensitive UPLC–MS/MS method was established to determine the plasma concentrations of the fourteen compounds to compare the pharmacokinetic parameters after orally administration of FF, TLF, FF–WEF, FF–TLF, TLF–WEF and FF–TLF–WEF with approximately the same dose. At different time points, the concentration of rutin (1), isoquercitrin (2), quercetin 3-O-[4-O-(-β-D-glucosyl)-α-L-rhamnoside] (3), ginkgolide C (4), bilobalide (5), quercitrin (6), ginkgolide B (7), ginkgolide A (8), luteolin (9), quercetin (10), apigenin (11), kaempferol (12), isorhamnetin (13), genkwanin (14) in rat plasma were determined and main pharmacokinetic parameters including T_1/2, T_max, C_max and AUC were calculated using the DAS 3.2 software package. The statistical analysis was performed using the Student?s t-test with P<0.05 as the level of significance.

Results

FF and WEF had no effect on the pharmacokinetic behaviors and parameters of the four terpene lactones, but the pharmacokinetic profiles and parameters of flavonoids changed while co-administered with non-flavonoid components. It was found that C_max and AUC of six flavonoid aglycones in group FF–WEF, FF–TLF and FF–TLF–WEF had varying degrees of reduction in comparison with group FF, especially in group FF–TLF–WEF. On the contrary, the values of C_max, T_max and AUC of four flavonoid glycosides in group FF–TLF–WEF were significantly increased compared with those in group FF.

Conclusions

These results indicate that non-flavonoid components in Ginkgo biloba extracts could increase the absorption and improve the bioavailability of flavonoid glycosides but decrease the absorption and reduce the bioavailability of flavonoid aglycones.     

对叶百部生品及蜜炙品不同极性部位止咳化痰作用比较

目的: 比较对叶百部生、炙品不同极性部位止咳化痰作用差异性,为百部作为止咳类药物发挥传统功效时生熟用药提供实验支持,为进一步揭示百部蜜炙原理奠定基础。方法: 清洁级昆明种小鼠200 只, 随机分为20 组, 10 只/组, 雌雄各半。第1组为空白对照组,ig 给予生理盐水;第2 组为阳性对照组,ig 给予可待因6 mg ·kg^-1;其他组为给药组,给药容积为10 mL ·kg^-1。给药小鼠给药前禁食8 h,禁水2 h,连续给药2 d,末次给药后1 h,采用小鼠氨水引咳法,对对叶百部生品及蜜炙品的不同部位,包括水煎液、总生物碱提取物及非生物碱提取液(各设3个剂量,按生药量计均为20,10,5 g ·kg^-1)的止咳作用进行比较。取昆明种小鼠200 只, 随机分为20 组, 10只/组, 雌雄各半。第1组为空白对照组,ig 给予生理盐水;第2 组为阳性对照组,ig 给予氯化氨 40 mg ·kg^-1;其他组为给药组,给药剂量为10 mL ·kg^-1。给药小鼠给药前禁食8 h,禁水2 h,连续给药2 d,末次给药后0.5 h,采用气管酚红法,研究生、炙品不同极性部位化痰效果。结果: 与空白组对比,对叶百部生品不同部位均具有显著的止咳作用(P<0.05, P<0.01, 或P<0.001),而炙品的水煎液及总生物碱提取物有显著的止咳作用(P<0.05, P<0.01, 或P<0.001),但其非碱部分只有高剂量有显著的止咳作用(P<0.001)。对于对叶百部生、炙品相同极性部位比较,发现生、炙品水煎液中剂量及高剂量之间均有显著差异(P<0.05),而总碱提取物低剂量和中剂量有显著性差异(P<0.05),非生物碱提取液仅高剂量有显著性差异(P<0.05), 均显示炙品止咳活性强于生品。化痰实验仅生品水煎液高剂量和炙品水煎液高剂量有显著的效果(P<0.05),其他均和空白组之间无显著差异。结论: 对叶百部蜜炙后止咳作用增强的主要部位为总生物碱提取物部位及水煎液部位,而其化痰作用生、炙品均较弱, 说明百部不是通过化痰起到止咳功效。     

不同炮制法对广西五月艾总黄酮含量及镇痛作用的影响

目的:探讨不同炮制方法对广西五月艾总黄酮含量及镇痛作用的影响.方法:采用紫外分光光度法测定总黄酮含量;采用热板法、扭体法观察不同五月艾炮制品对小鼠的镇痛作用.结果:不同炮制品中广西五月艾总黄酮含量大小为酒炙品＞醋炙品＞生品.醋炙品中总黄酮含量较生品提高6.60％,酒炙品则提高7.46％;扭体法中,醋炙组镇痛率较生品提高27.11％,酒炙组则提高29.11％;热板法中,广西五月艾醋炙品和酒炙品较生品对热板致痛能大幅提高止痛作用.结论:广西五月艾生品、醋炙品、酒炙品对冰乙酸所致的小鼠扭体反应有明显的抑制作用,均能提高对小鼠不同时段热板致痛的痛阈.