对羟基苯甲酸通过抑制NF-κB/caspase-1信号通路抗类风湿性关节炎的研究

目的 探讨天然酚酸类化合物对羟基苯甲酸（p-hydroxybenzoic acid，HA）对完全弗氏佐剂（complete Freund’s adjuvant，CFA）诱导的佐剂性关节炎（adjuvant arthritis，AA）模型的治疗作用，并对HA的作用机制进行初步分析。方法 除正常组外，向大鼠足跖皮内注射CFA 0.1 mL诱导AA大鼠模型。将AA模型大鼠随机分为模型组，HA低、中、高剂量组（2.5，5，10 mg·kg^-1）和阳性药物组（吲哚美辛，5 mg·kg^-1），灌胃给予药物进行治疗干预，记录每组大鼠足肿胀体积、足肿胀厚度并进行关节肿胀评分；通过ELISA和qPCR检测不同剂量HA对炎症因子（TNF-α、IL-1β、IL-6）表达的影响；采用X-射线和HE染色观察足爪组织形态学和病理学变化；Western blotting检测caspase-1和NF-κB的表达。结果 HA能减轻AA大鼠关节肿胀（P<0.05）；从蛋白质和mRNA水平显著抑制炎症因子（TNF-α、IL-1β、IL-6）的产生（P<0.05），并显著降低caspase-1和NF-κB蛋白表达水平；X-射线显示HA能减轻大鼠踝关节损伤，HE染色结果显示HA能显著抑制炎症细胞的浸润和软骨表层破坏等情况（P<0.05），且这些结果均呈剂量依赖性。结论 HA可能通过抑制NF-κB/caspase-1信号通路缓解关节炎症状。     

茵连痛风颗粒对佐剂性关节炎大鼠的抗炎镇痛作用研究

目的 考察茵连痛风颗粒对佐剂性关节炎大鼠的缓解作用。方法 建立弗氏完全佐剂模型,48只大鼠随机分为正常组、模型组、茵连痛风颗粒高、中、低剂量组（15.4、7.7、3.8 g/kg）,用药物干预后,测定大鼠关节炎指数、踝关节肿胀率、甲醛致痛分值,用ELISA检测IL-4、IL-10、前动力蛋白（PK1,PK2）含量。观察大鼠足趾肉垫病理变化。结果 与模型组比较,茵连痛风颗粒组可显著抑制大鼠踝关节肿胀,降低甲醛致痛反应（P<0.01）,明显升高抑炎因子IL-4、IL-10 含量（P<0.01）,降低PK1、PK2含量（P<0.01）;缓解足趾水肿和淋巴细胞浸润。结论 茵连痛风颗粒对佐剂关节炎具有明显抑制作用,暗示其对类风湿关节炎具有一定的治疗前景。     

伸筋草生物碱对佐剂性关节炎大鼠的抗炎作用及机制研究

目的 探讨伸筋草生物碱对完全弗氏佐剂（CFA）诱导大鼠关节炎的治疗作用及机制。方法 健康SD大鼠48只,随机分为6组,每组8只,即对照组、模型组、依托考昔片（阳性药,1 mg/kg）组及伸筋草生物碱低、中、高剂量（30、60、120 mg/kg）组,除对照组外,其余40只大鼠sc 0.1 mL CFA造模,致炎15 d后,连续ig给药30 d。测定大鼠足趾肿胀率、HE染色后观察造模测踝关节滑膜病理改变;致炎45 d,ELISA法测定血清中白介素-1β（IL-1β）、肿瘤坏死因子-α（TNF-α）水平。结果 与模型组比较,依托考昔片及伸筋草生物碱低、中、高剂量组足趾肿胀率均显著下降（P<0.05、0.01）;中、高剂量伸筋草生物碱明显改善滑膜细胞、巨噬细胞、纤维细胞增生与炎症细胞浸润;与模型组比较,依托考昔片及伸筋草生物碱高剂量组大鼠血清TNF-α水平显著下降（P<0.05）,依托考昔片及伸筋草生物碱各剂量组IL-1β水平均显著降低（P<0.01）。结论 伸筋草生物碱显著抑制CFA诱导关节炎大鼠关节肿胀,改善大鼠踝关节滑膜病变,其作用机制可能与降低体内IL-1β、TNF-α水平有关。     

蜂毒肽通过Th1/Th2途径对胶原诱导关节炎大鼠模型免疫调节的影响

目的 探讨蜂毒肽对胶原诱导关节炎大鼠模型免疫调节的影响。方法 成功建立胶原诱导关节炎大鼠模型，随机分为模型组、蜂毒肽（0.5 mg/kg）组、甲氨蝶呤（1 mg/只）组，每组6只，另选取未造模大鼠为对照组；造模第14天起，隔日1次ip蜂毒肽，每周1次ip甲氨蝶呤，对照组、模型组ip等量生理盐水，给药21 d。观察关节肿胀程度、进行关节炎指数（AI）评分；给药结束后，收集血清，ELISA法检测血清中免疫球蛋白G （IgG）、IgG1、IgG2a、干扰素-γ（IFN-γ）、白细胞介素-4（IL-4）水平；分离大鼠脾脏，提取淋巴细胞，流式细胞术检测Th1、Th2细胞比例。结果 蜂毒肽组大鼠关节皮肤发红，关节肿胀明显减轻；与模型组比较，蜂毒肽显著抑制AI评分（P<0.05）；显著降低血清中IgG、IgG2a、IFN-γ浓度（P<0.05），升高IgG1、IL-4浓度（P<0.05）；显著下调Th1细胞比例、Th1/Th2比值（P<0.05），上调Th2细胞比例（P<0.05）。结论 蜂毒肽能通过调节Th1/Th2平衡抑制胶原诱导关节炎大鼠的炎症。     

痹痛合剂对佐剂性关节炎大鼠滑膜组织的影响

目的 考察痹痛合剂通过NF-κB信号通路对佐剂性关节炎大鼠关节滑膜炎症的调节。方法 将40只SD大鼠随机分成5组,分别为：空白组,模型组,双氯芬酸钠组,痹痛合剂高剂量组（高剂量组）、痹痛合剂低剂量组（低剂量组）,除正常组外,其余大鼠采用0.2 mL弗氏完全佐剂皮内注射右后足趾,形成佐剂性关节炎大鼠模型。正常组注射等体积的生理盐水在相同部位注射。致炎后,每组大鼠根据设定剂量连续灌胃给药21 d,双氯芬酸钠组每天剂量为0.5 mg·(100 g)^-1双氯芬酸钠,痹痛合剂高剂量组每天剂量为0.6 mL·(100 g)^-1痹痛合剂,低剂量组每天剂量为0.3 mL·(100 g)^-1痹痛合剂。分别给予空白组、模型组等体积的蒸馏水。检测大鼠滑膜组织病理组织学改变,炎症因子核因子-κB （NF-κB）、白细胞介素-1β（IL-1β）、白细胞介素-6（IL-6）、肿瘤坏死因子α（TNF-α）的表达水平改变及核因子-κB信号通路相关蛋白的相对表达水平改变。结果 各给药组在以上各检测指标上较模型组有显著改变（P＜0.01）,痹痛合剂高剂量组的治疗作用优于低剂量组和双氯芬酸钠组（P＜0.05）。结论 痹痛合剂具有抑制关节滑膜组织中炎症因子的表达,可有效减轻佐剂性关节炎大鼠的关节炎症表现。     

雷公藤柱层析各段组分对胶原诱导性关节炎模型大鼠细胞因子表达的影响

目的 比较雷公藤柱层析各段组分对Ⅱ型胶原诱导性关节炎（collagen-induced arthritis,CIA）模型大鼠血清中肿瘤坏死因子-α（TNF-α）、白细胞介素-1β（IL-1β）表达的影响,初步探讨各段组分中有效成分与药效的关系。方法 HPLC测定各段组分中6个有效成分的含量。在SD大鼠背、尾根及左后足跖多点皮内注射牛Ⅱ型胶原蛋白（BCⅡ）乳液,建立CIA大鼠模型。选取80只成模大鼠随机分为模型对照组、阳性对照组和各段组分组,每组各8只。免疫20 d后,连续灌胃给药3周,记录大鼠关节炎指数（arthrits index,AI）,通过酶联免疫法检测血清中TNF-α、IL-1β的表达,原位末端转移酶标记技术（TUNEL染色法）检测各段组分对肝细胞凋亡的影响,Western-blot检测大鼠肝组织中caspase-3蛋白表达。结果 中段和末段组分中有效成分的含量差异较大。与模型对照组比较,中段组分的高、低剂量组和末段组分的高剂量组给药3周后均能明显降低AI值（P<0.01）,能明显抑制大鼠血清中TNF-α、IL-1β表达（P<0.01）,也能明显诱导肝细胞凋亡（P<0.01）,明显升高caspase-3活性（P<0.01）。结论 雷公藤柱层析各段组分治疗CIA可能与降低血清中TNF-α和IL-1β表达有关,灌胃后会诱导大鼠肝细胞发生凋亡,上调caspase-3活性,有效成分与药效存在量效关系。     

红花黄色素对佐剂型关节炎大鼠的抗炎作用研究

目的 观察红花黄色素对佐剂型关节炎大鼠的抗炎作用并探讨其机制。方法 用弗氏完全佐剂建立佐剂型关节炎大鼠模型,分为正常组、模型组、红花黄色素100,50,25 mg·kg^-1组,每组10只。排水法检测大鼠足趾肿胀度,Elisa法检测炎症因子IL-1β及TNF-α的水平,western blot法检测滑膜组织中IL-1β和TNF-α蛋白的表达。结果 与模型组相比,红花黄色素各组能显著降低佐剂型关节炎大鼠的足趾肿胀度（p<0.01或P<0.05）,降低血清中IL-1β及TNF-α含量水平（p<0.01或p<0.05）,还能降低滑膜组织中IL-1β及TNF-α蛋白的表达（p<0.01或p<0.05）。结论 红花黄色素能显著缓解佐剂型关节炎大鼠的关节炎症,其机制与下调炎症因子IL-1β及TNF-α的表达有关。     

杜仲醇提取物通过NF-kB信号通路改善大鼠牙周组织病的作用研究

目的 探讨杜仲醇提取物通过NF-kB信号通路作用于牙周病破骨细胞活化因子（IL-1β）改善大鼠牙周组织病的疗效。方法 选取SPF级Wistar大鼠60只,♂,随机数字表法分成4组,正常组,模型组,杜仲醇提取物低、高剂量组,各15只。除正常组外,其他大鼠制备牙周病模型,造模1周后杜仲醇提取物低、高剂量组分别在大鼠上颌右侧第一、第二磨牙间腭、颊侧的龈沟底内注入0.2 mL 0.1,1.0 mg·mL^-1的杜仲醇提取物,正常组与模型组大鼠注入等剂量生理盐水,连续注入5 d。Western-blot、荧光定量PCR检测大鼠牙周膜成纤维细胞内破骨细胞活化因子（IL-1β）蛋白、mRNA表达状况。结果 与正常组相比,模型组大鼠成纤维细胞内IL-1β、NF-kB mRNA相对表达量显著上升（P<0.05）;与模型组相比,杜仲醇提取物低、高剂量组大鼠成纤维细胞内IL-1β、NF-kB mRNA相对表达量显著下降（P<0.05）。与正常组相比,模型组大鼠血清IL-6、IL-1β及TNF-α含量显著上升（P<0.05）;与模型组相比,杜仲醇提取物低、高剂量组大鼠血清IL-6、IL-1β及TNF-α含量显著下降（P<0.05）。与正常组相比,模型组大鼠上颌组织内NF-kB、IL-1β蛋白表达显著上升（P<0.05）;与模型组相比,杜仲醇提取物低、高剂量组大鼠上颌组织内NF-kB、IL-1β蛋白表达下降（P<0.05）。结论 杜仲醇提取通过NF-kB信号路径对牙周病破骨细胞活化因子（IL-1β）产生作用,降低牙周组织内炎症因子含量,对牙周病起到治疗作用。     

愈风宁心片对偏头痛大鼠模型的镇痛作用研究

目的 探讨愈风宁心片对偏头痛大鼠模型的镇痛作用及机制。方法 SD大鼠随机分成6组：对照组、模型组、苯甲酸利扎曲普坦片（阳性药,0.9 mg·kg^-1）组和愈风宁心片低、中、高剂量（378、756、1 512 mg·kg^-1）组,每天ig给药1次,连续10 d。末次给药后1 h,除对照组外,其余各组大鼠在头颈处sc 10 mg·kg^-1硝酸甘油建立偏头痛大鼠模型,观察疼痛行为学指标,试剂盒法检测血清中疼痛相关因子缩胆囊素（CCK）、白细胞介素-1β （IL-1β）、前列腺素E（2 PGE₂）含量;利用小鼠醋酸扭体实验、小鼠右后足跖部福尔马林致痛实验观察愈风宁心片低、中、高剂量（546、1 092、2 184 mg·kg^-1）对小鼠扭体反应和舔足时长的影响。结果 偏头痛实验结果表明,与模型组比较,愈风宁心片各剂量组和苯甲酸利扎曲普坦片组的挠头、甩头次数和行为学评分显著降低（P<0.05、0.01）;愈风宁心片中、高剂量组血清CCK水平显著降低（P<0.05、0.01）,低、中、高剂量组血清PGE₂、IL-1β水平显著降低（P<0.05、0.01）。醋酸扭体实验结果表明,与模型组比较,愈风宁心片中、高剂量组小鼠扭体次数显著降低（P<0.05、0.01）,高剂量组小鼠扭体反应潜伏期显著延长（P<0.01）。福尔马林致痛实验结果表明,与模型组比较,各给药组均能显著缩短小鼠的舔足时长（P<0.01）。结论 愈风宁心片对偏头痛模型具有镇痛作用,其机制可能与调节中枢及外周神经系统、改善疼痛相关因子含量有关。     

乳香没药精油自微乳的制备与抗炎镇痛作用评价

目的 制备乳香没药精油（FMO）自微乳化给药系统（FMO-SMEDDSs）,并评价其抗炎镇痛效果。方法 水蒸气蒸馏法提取FMO,考察FMO与不同种类油相、乳化剂和助乳化剂的配伍相容性并确定了FMO-SMEDDSs的处方组成,最终根据伪三元相图法得到其处方配比;以热力学稳定性、动态光散射、透射电镜等实验手段评价FMO-SMEDDSs的理化性质。将 SD 大鼠随机分为 5 组 ：对照组、模型组、布洛芬（阳性药 ,20 mg·kg^-1）组、FMO（生药剂量 90 mg·kg^-1）组、FMOSMEDDSs （90 mg·kg^-1）组,每天ig给药2次,连续给药7 d,对照组与模型组ig生理盐水;除对照组外,其余4组大鼠均在右后足跖sc 40.0%甲醛溶液0.1 mL,6 h后用千分尺测量大鼠右后足厚度,并计算肿胀度和肿胀抑制率;ELISA试剂盒法分别检测致炎足足底组织中前列腺素E₂（PGE₂）水平,血清白细胞介素-6（IL-6）、肿瘤坏死因子-α（TNF-α）水平。通过小鼠扭体法评价布洛芬（40 mg·kg^-1）组、FMO（180 mg·kg^-1）组、FMO-SMEDDSs（180 mg·kg^-1）的镇痛效果。结果 根据配伍相容性及伪三元相图结果,分别选择肉豆蔻酸异丙酯（IPM）、聚山梨酯 80 和异丙醇作为 FMO-SMEDDSs 的油相、乳化剂和助乳化剂,配比为 4∶4∶2;FMO-SMEDDSs形成的微乳平均粒径为（57.8±1.1）nm,PDI为（0.216±0.014）,Zeta电位为（-11.5±0.05）mV,在透射电镜下可观察到微乳呈球状,FMO-SMEDDSs热力学稳定性良好。与模型组比较,布洛芬、FMO、FMOSMEDDSs组大鼠的致炎足肿胀度及肿胀率均显著降低（P＜0.05）,PGE₂、TNF-α和IL-6水平显著降低（P＜0.05）;与FMO组比较,FMO-SMEDDSs组大鼠致炎足肿胀度及肿胀率进一步显著降低（P＜0.05）,PGE₂、TNF-α和IL-6水平进一步显著降低（P＜0.05）。与模型组比较,ig布洛芬、FMO以及FMO-SMEDDSs后均能显著延长小鼠扭体反应潜伏期,显著减少15 min内的扭体次数（P＜0.05）;相对于FMO组,FMO-SMEDDSs抑制小鼠扭体反应作用更明显。结论 成功制备FMO-SMEDDSs,其具有良好的抗炎镇痛的作用。     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

EFFECT OF POLICOSANOL SUCCESSIVE DOSE INCREASES ON PLATELET AGGREGATION IN HEALTHY VOLUNTEERS

Policosanol is a cholesterol-lowering drug with hypocholesterolemic effects demonstrated in experimental models, healthy volunteers and type II hypercholesterolemic patients. In addition, antiplatelet effects of policosanol have been shown in experimental models and healthy volunteers. The effect of successively increasing doses of policosanol on platelet aggregation was investigated in a randomized, placebo-controlled, double-blind study conducted in 37 healthy volunteers. The volunteers were on a placebo-baseline period (two tablets per day) for 7 days and thereafter they received randomly, under double-blind conditions, placebo or policosanol (10mgday⁻¹) for 7 days. After this period dosage was doubled to 20mgday⁻¹for the next 7 days and then again doubled to 40mgday⁻¹, while the control group received placebo tablets all the time. Platelet aggregation as well as coagulation time was measured at baseline and after each dosing step. Results showed that antiplatelet effects of policosanol were successfully enhanced throughout the study, thus suggesting a dose-dependent relationship. No significant effect was reached during the first dosing period, but significant reductions of epinephrine and ADP-induced platelet aggregation were observed after the second one. Finally, a significant inhibition of platelet aggregation induced by all the agonists was observed at the last dosing step. Coagulation time remained unchanged during the trial.     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

鼻渊净胶囊的HPLC指纹图谱研究

目的 建立鼻渊净胶囊的高效液相色谱（HPLC）指纹图谱。方法 采用Agilent SB-C₁₈（4.6 mm×250 mm,5 μm）色谱柱,乙腈-水为流动相、以1.0 ml/min流速行梯度洗脱,检测波长210 nm,柱温30 ℃,洗脱时间为80 min。采用中药色谱指纹图谱相似度评价系统（2004A版）对检测出色谱进行指纹图谱相似度评价。结果 建立了鼻渊净胶囊的HPLC指纹图谱,确定了20个共有峰,15个峰归属到各药材,其中5个峰确认了化学成分;10批样品的指纹图谱的整体相似度与对照图谱比较,均在90%以上。结论 所建立的鼻渊净胶囊指纹图谱有助于从整体上控制该制剂的质量。     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF THE CLASS III ANTIARRHYTHMIC SUBSTANCE / -SOTALOLIN VITRO: REVERSIBLE INHIBITION OF CHOLINESTERASE ISOENZYMES FROM BLOOD AND THE HUMAN CENTRAL NERVOUS SYSTEM

Inhibitory effects of the class III antiarrhythmic compound / -sotalol on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and the human caudate nucleus and on serum cholinesterase (ChE; EC 3.1.1.8) were studiedin vitrousing a spectrophotometric kinetic assay with acetylthiocholine (ASCh) as substrate. Sotalol concentrations in the assays varied from 0.32 to 3.2m . All isoenzymes studied were inhibited by / -sotalol in a reversible and concentration-dependent manner. Double reciprocal plots of the reaction velocity against varying ASCh concentrations revealed that / -sotalol reduced substrate affinity (apparent Michaelis constant, KM, increased) of serum ChE, but did not change the enzyme's maximal rate of ASCh hydrolysis (V_max). Thus, / -sotalol inhibition of serum ChE was of the competitive type (rate constant for reversible competitive inhibition: K_i=0.51m ). In contrast, / sotalol reduced the maximal reaction velocity of the AChE isoenzyme from the central nervous system (caudate nucleus), but had no influence on substrate affinity of the enzyme (K_Mwith ASCh unchanged) indicating purely non-competitive inhibition kinetics (rate constant of reversible non-competitive inhibition: K_i′=0.44m ). / -sotalol inhibition of erythrocyte AChE was of mixed competitive/non-competitive type (K_i=0.31m , K_i′=0.49m ). Non-competitive / -sotalol inhibition of caudate nucleus AChE and the non-competitive component of erythrocyte AChE inhibition cannot be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Peak / -sotalol plasma levels as described in the literature for both humans (15μ ) and experimental animals (dogs: 18μ ; rats: 260μ ) as well as maximal myocardial concentrations of the substance (dogs: 46μ ; rats: 478μ ) are in the range of about 2% to 100% of the sotalol inhibition rate constants determined in the present paper for cholinesterase isoenzymesin vitro. Thus, / -sotalol inhibition of ACh hydrolysisin vivomay contribute to both the well known antiarrhythmic potential and proarrhythmic side effects of the compound.     

喙果黑面神化学成分研究

目的研究大戟科植物喙果黑面神(Breynia rostrata Merr.)的化学成分。方法利用硅胶、凝胶等色谱技术分离纯化化学成分,根据化合物的理化性质和光谱数据进行结构鉴定。结果从喙果黑面神的正丁醇萃取部分分离得到4个化合物,分别鉴定为6-O-甲基丙酰基-α-D-吡喃葡糖(6-O-methylpropanoyl-α-D-glucopyranose,1);4″-苯酚基-6-O-甲基丙酰基-β-D-吡喃葡糖苷(4″-phenolic-6-O-methylpropanoyl-β-D-glucopyranoside,2);1-O-没食子酰基-β-D-吡喃葡糖苷(1-O-galloyl-β-D-glucopyranoside,3);熊果苷(arbutin,4)。结论化合物1和2为新化合物,3和4均为首次从该种植物分离得到。     

AMELIORIATION OF CHEMICALLY-INDUCED HEPATOCYTE INJURY BY CYCLOSPORINE A

Cyclosporine A, beside its current applications, possesses potential hepatoprotective effects. This study was directed to investigate the effect of Cyclosporine A pretreatment on hepatic injury due to carbon tetrachloride (CCl₄) and -galactosamine. Rats were injected by two successive doses of Cyclosporine A (5mgkg⁻¹day⁻¹). Six hours after the second dose, 1mlkg⁻¹of CCl₄was administered i.p. Effects associated with Cyclosporine A pretreatment were examined by using isolated hepatocytes and hepatocytes that were immobilized and continuously perfused. -Galactosamine (5m ) was added directly to the perfusion medium. After isolation, hepatocytes were examined histologically by light and electron microscopy, immobilized and perfused for further metabolic functional activity evaluation. Cyclosporine A pretreatmentin vivoproduced hepatoameliorative effects of various degrees which were statistically significant as manifested by: (1) an increased trypan blue exclusion after CCl₄; (2) an improved ureagenesis after CCl₄; (3) a reduction in the lipid droplets accumulation in the cytoplasm produced by CCl₄administration; (4) well preserved cytoplasmic organelles as mitochondria, endoplasmic reticulum ER, nuclear chromatin structures that were altered by CCl₄; and (5) an increased hepatocytes survival in the agarose gel matrix, reduction of LD leakage and improvement of ureagenesis after -galactosamine addition to the perfusion medium. The beneficial effect of Cyclosporine A pretreatment in modifying hepatotoxicity of chemical insults merits further studies.     

EFFECTS OF 2-GUANIDINE-4-METHYLQUINAZOLINE ON GASTRIC ACID SECRETION IN RATS

In this study 2-guanidine-4-methylquinazoline (2-GMQ) appeared to decrease basal and stimulated gastric acid secretion, while structurally related compounds as dimethyl- biguanide, cyanoguanidine and 2-cyanoamino-4-methylpyrymidine did not. Thus, there is an antisecretory effect when the biguanide group is associated with a lipophilic structure. The antisecretive effects exerted by 2-GMQ are associated with anti H₂-histamine activity.The anti H₂-histamine nature of the effects of 2-GMQ was confirmed by the capacity of this compound of depressing the chronotropic activity of the isolated guinea pig auricle increased by histamine, as well as relaxant activity in rat uterus contracted by histamine, since both preparations are rich in H₂-histamine receptors.     

栝楼不同药用部位质量控制的研究进展

瓜蒌子、瓜蒌皮、瓜蒌、天花粉来源于栝楼的不同药用部位,4味药材均为常用的大宗药材,现行版《中国药典》对其制定的质量标准过于简单,无法科学合理地控制其质量。本文对瓜蒌子、瓜蒌皮、瓜蒌、天花粉安全性和有效组分的研究进行综述,明确了相关研究存在的问题并针对问题提出建议,为科学全面的药材及饮片标准的制定提供参考依据。