银杏内酯B柔性纳米脂质体的制备及体外透皮研究

目的：制备银杏内酯B(GB)柔性纳米脂质体，并对其体外透皮规律进行研究。方法：采用薄膜分散法制备银杏内酯B柔性纳米脂质体，并对其形态及粒径大小进行分析；采用改良的 Franz 扩散池进行体外透皮吸收试验，比较银杏内酯B醇溶液、银杏内酯B柔性纳米脂质体及普通银杏内酯B纳米脂质体的经皮累积渗透量及渗透速率。结果：此方法制得的脂质体平均包封率为(89.52±1.76)%，平均粒径为(208.3±25.49) nm，Zata电位为-49.2 mV。柔性纳米脂质体8 h的累积透过量为189.97 μg·cm^-2，8 h的渗透速率为23.75 μg·cm^-2·h^-1。结论：柔性纳米脂质体包封率较高，稳定性良好，可显著促进银杏内酯B的透皮吸收。     

补肾抗衰片对实验性动脉粥样硬化家兔的NF-κB及炎症因子的影响

目的 探讨补肾抗衰片对家兔动脉粥样硬化的干预作用及作用机制。     

Suppression of lipopolysaccharide-induced inflammatory responses in RAW 264.7 murine macrophages by aqueous extract of Clinopodium vulgare L. (Lamiaceae)

Ethnopharmacological relevance

The wild basil Clinopodium vulgare L. is commonly used in Bulgarian folk medicine for treatment of irritated skin, mastitis- and prostatitis-related swelling, as well as for some disorders accompanied with significant degree of inflammation (e.g. gastric ulcers, diabetes, and cancer).

Aim of study

To determine the effect of aqueous extract of Clinopodium vulgare L. on LPS-induced inflammatory responses of murine RAW 264.7 macrophages.

Materials and methods

Cell cytotoxicity was evaluated by MTT assay. Protein expression levels were monitored by Western blot analysis. Production of NO and PGE₂ was measured by the Griess colorimetric method and enzyme immunoassay, respectively. Activation of MMP-9 was visualized by gelatin zymography. Cytokine levels were determined by BioPlex assay. Intracellular ROS and free radical scavenging potential were measured by DCFH-DA and DPPH method, respectively. Xanthine oxidase activity was evaluated spectrophotometrically.

Results

The extract suppresses NF-κB activation by preventing Iκ-B phosphorylation and inhibits the phosphorylation of p38 and SAPK/JNK MAPKs. It down-regulates iNOS expression which manifests as a drastic decrease of NO production, inhibits MMP-9 activation, but does not affect COX-2 protein levels and reduces only slightly the released PGE₂. Secretion of IL-1β and Il-10 is greatly reduced, whereas suppression of TNF-α and GM-CSF production is less dramatic. The extract has strong free radical scavenging properties and exerts inhibitory effect on xanthine oxidase activity, which lowers the levels of intracellular ROS.

Conclusion

The study provides evidence for the anti-inflammatory potential of Clinopodium vulgare L. aqueous extract.     

荞麦花叶黄酮对2型糖尿病大鼠胰岛素抵抗及肝组织PTP1B的影响

目的:探讨荞麦花叶黄酮(FBFL)对2型糖尿病大鼠降血糖、改善胰岛素抵抗的作用及其机制.方法:雄性健康Wistar大鼠70只,随机抽取10只作为正常对照组,其余60只大鼠每天灌胃脂肪乳,第14天开始腹腔注射小剂量四氧嘧啶,隔日1次,共3次,同时继续灌胃脂肪乳.末次腹腔注射四氧嘧啶72 h后,用血糖仪测定空腹血糖和用K_(IPT)值判定胰岛素抵抗性.K_(IPT)＜正常组的60%作为2型糖尿病胰岛素抵抗大鼠.将成模大鼠随机分为模型组,阳性药物组,FBFL低、中、高剂量组,连续4周.末次给药后禁食,用血糖仪测空腹血糖(FBG),用正糖钳技术判定胰岛素抵抗性,用生化分析仪测定游离脂肪酸(FFA),放免法测定血浆胰岛素(INS),免疫组织化学法检测肝组织蛋白酪氨酸磷酸酶1B(PTP1B)表达.结果:与正常组比较,模型组大鼠FBG,INS,FFA含量明显升高(P＜0.135,P＜0.01);大鼠葡萄糖输注速率(GIR)明显下降;肝组织PTP1B表达增加.各剂量FBFL能不同程度的改善上述指标的变化,明显改善胰岛素抵抗性,增加胰岛素敏感性,使肝组织PTP1B表达下调,并呈一定剂量依赖性.结论:FBFL对四氧嘧啶加脂肪乳所致2型糖尿病大鼠胰岛素抵抗具有明显的改善作用,并呈一定剂量依赖性.     

丙泊酚对大鼠缺血再灌注肾NF-κB、TNF-α表达的影响

目的 研究丙泊酚对大鼠肢体缺血再灌注损伤后肾组织中肿瘤坏死因子-α（tumornecrosisfactor-α，TNF-α）、核因子-κB（nuclear factor-κxB，NF-κB）表达的影响。方法 24只SD雄性大鼠，随机分为假手术对照组（A组），肢体缺血再灌注组（B组）和丙泊酚干预组（C组），每组8只。采用免疫组织化学方法检测TNF-α、NF-κB的表达，行图像分析半定量。结果 B组大鼠肾组织中TNF-α、NF-κB的表达明显高于A组（P〈0．05），C组明显低于B组（P〈0．05）。结论 肢体缺血再灌注后有明显肾损伤，丙泊酚对肢体缺血再灌注肾损伤有一定程度的保护作用，其机制可能与下调大鼠肢体缺血再灌注损伤肾组织中TNF-α、NF-κB的过度表达有关。     

慢性乙型肝炎患者病毒e系统状态与肝纤维化关系的研究

目的:观察慢性乙型肝炎患者乙型肝炎病毒e系统状态和复制指标在肝纤维化发生过程中的变化及其与血清纤维化标志的关系,探讨它们在肝纤维化发生过程中的作用及其可能的临床意义.方法:188例慢性乙型肝炎患者根据肝纤维化程度分为S0～S4期等5组,分别用定量PCR及放免法检测患者血清中HBV-DNA及肝纤维化标志透明质酸、Ⅳ型胶原、Ⅲ型前胶原和层粘连蛋白的含量;HBeAg和抗-HBe采用酶联免疫吸附法(ELISA)检测,并观察其在不同肝病理纤维化分期时的变化.结果:随着肝纤维化程度加重,血清HBV-DNA含量逐渐升高,从S1期开始显著增加(P＜0.01);而HBeAg阳性率逐渐降低,S3、S4期较S0显著减少(P＜0.05和P＜0.01);抗-HBe阳性率呈相反的变化趋势,在S3和S4期的阳性率明显高于S0期(P＜0.05和P＜0.01).血清HBV-DNA( )HBeAg( )组血清纤维化标志最低,HBV-DNA(-)抗-HBe( )组最高,两者差异有显著性(P＜0.01).结论:HBV复制和e系统状态的改变与肝纤维化程度密切相关,肝内病毒复制标志与血清纤维化标志联合检测,对于判断肝纤维化程度和指导抗病毒治疗有重要的价值.     

尔肾康对肾病综合征大鼠模型系膜增殖的影响

目的：观察中药尔肾康对肾病综合征大鼠模型系膜增殖的影响，探讨其治疗机制。方法：选取Wistar大鼠，采用阿霉素慢性肾病模型，分别用强的松和中药合强的松进行治疗，并设对照组，连续给药12周，测定24h尿蛋白定量、血生化及血、尿TNF—α，观察肾脏病理变化。结果：中药合激素组24h尿蛋白定量呈明显低值，与模型组相比有极显著性差异（P〈0．01），与激素组相比较有明显差异（P〈0．05）；中药合激素组明显降低大鼠血、尿TNF—α浓度，与激素组比较也有明显差异（P〈0．05）；中药合激素组同激素组比较有显著升高白蛋白作用（P〈0．05）；病理切片发现，中药合激素组与模型组、激素组比较，肾小球轮廓清晰，系膜细胞和系膜基质增生不明显，肾小管内未见有蛋白管型。结论：尔肾康有明显抑制系膜增殖的作用，机理可能是促进白蛋白的合成，减少白蛋白在肾小管处的分解，抑制TNF—α的分泌。     

Flavocoxid is as effective as naproxen for managing the signs and symptoms of osteoarthritis of the knee in humans: a short-term randomized,double-blind pilot study

Flavocoxid (Limbrel), a proprietary mixture of flavonoid molecules (baicalin and catechin), was tested against a traditional nonsteroidal anti-inflammatory drug, naproxen, for the management of the signs and symptoms of moderate osteoarthritis (OA) in humans. Discomfort and global disease activity were used as the primary end points, and safety assessments were also taken for both treatments as a secondary endpoint. In this double-blind study, 103 subjects were randomly assigned to receive either flavocoxid [500 mg twice daily (BID)] or naproxen (500 mg BID) in a 1-month onset of action trial. Outcome measures included the short Western Ontario and McMaster University Osteoarthritis Index, subject Visual Analogue Scale for discomfort and global response, and investigator Visual Analogue Scale for global response and fecal occult blood. Both flavocoxid and naproxen showed significant reduction in the signs and symptoms of knee OA (P ≤ .001). There were no statistically detectable differences between the flavocoxid and naproxen groups with respect to any of the outcome variables. Similarly, there were no statistically detectable differences between the groups with respect to any adverse event, although there was a trend toward a higher incidence of edema and nonspecific musculoskeletal discomfort in the naproxen group. In this short-term pilot study, flavocoxid was as effective as naproxen in controlling the signs and symptoms of OA of the knee and would present a safe and effective option for those individuals on traditional nonsteroidal anti-inflammatory drugs or cyclooxygenase-2 inhibitors. A low incidence of adverse events was reported for both groups.     

血清和精浆抑制素B在无精子症诊断中的应用研究

目的:评价血清和精浆抑制素B浓度在诊断梗阻性和非梗阻性无精子症中的应用价值。方法:测定25例正常生育者(正常对照组),37例梗阻性无精子症以及33例非梗阻性无精子症者的血清卵泡刺激素(FSH)、血清和精浆抑制素B浓度,对无精子症者行睾丸病理Johnsen评分。结果:精浆和血清抑制素B浓度比值在正常对照组和非梗阻性无精子组分别为2.17和3.63,差异无显著性(P=0.29);在梗阻性无精子症组两者比值为0.18,与正常对照组和非梗阻性无精子症组比较显著降低(P<0.01)。结论:精浆和血清抑制素B浓度比值可用于临床诊断梗阻性和非梗阻性无精子症。     

体外短波热疗联合前列腺灸及哈乐治疗非细菌性前列腺炎和前列腺痛疗效观察

目的 探讨慢性非细菌性前列腺炎（CNP）和前列腺痛（PD）的治疗方法。方法 应用体外短波热疗联合前列腺灸及α1A-肾上腺素能受体阻滞剂哈乐治疗CNP和PD患者26例，疗程8周。观察治疗前后前列腺炎症状评分（CPSI）与最大尿流率（MFR）变化。结果 有效率为80．8％。治疗前后CPSI和MFR均有显著改善（P〈0．05）。结论 体外短波热疗联合前列腺灸及哈乐治疗CNP和PD安全有效。