Effect of Rubus Occidentalis Extract on Metabolic Parameters in Subjects with Prediabetes: A Proof‐of‐concept,Randomized, Double‐blind,Placebo‐controlled Clinical Trial

Rubus occidentalis (RO) has beneficial effects on glucose and lipid profiles in vitro. The aim of the study was to investigate RO extract effect on metabolic parameters in prediabetic patients, adopting a 12‐week, randomized, double‐blind, placebo‐controlled trial. Forty‐four patients (age 59.0 ± 8.2 years, 70.5% females, HbA1c 5.8 ± 0.4%) were divided into placebo (n = 13), low‐dose RO extract (LRE; n = 14), or high‐dose RO extract (HRE; n = 17) groups. Either 900 or 1800 mg per day of RO extract was administered orally. Area under the curve for glucose obtained 2 h after a 75‐g oral glucose tolerance test was significantly decreased in the HRE group, compared with the placebo group (?28.1 ± 42.4 vs. +13.4 ± 52.6 mg/dL, p < 0.05). Homoeostasis model assessment‐B was increased (+17.11 ± 10.69, +5.24 ± 4.10, and +0.86 ± 6.01 in HRE, LRE, and placebo, respectively, p < 0.05). Serum levels of monocyte chemoattractant protein‐1 and oxidized low‐density lipoprotein were significantly decreased by treatment in a dose‐dependent manner (monocyte chemoattractant protein‐1: ?35.0 ± 21.2, +8.4 ± 18.1, and +24.2 ± 14.5; oxidized low‐density lipoprotein: ?19.7 ± 8.5, ?13.1 ± 7.2, and ?2.2 ± 11.0 in the HRE, LRE, and placebo, respectively, p < 0.05). The results support the beneficial effects of RO extract on the control of glycemia and vascular inflammation in prediabetic patients. (ClinicalTrials.gov: NCT01964703). Copyright © 2016 John Wiley & Sons, Ltd.     

Different Effects of Some Isoquinoline Alkaloids from Argemone mexicana on Electrically Induced Contractions of Isolated Guinea-pig Ileum

The present study examines the effects of the extracts [petroleum ether, CHCl₃, CHCl₃/MeOH (9:1) and MeOH], partially purified fractions and pure compounds from Argemone mexicana on the electrically induced contractions of the isolated guinea-pig ileum (E.C.I.). The results of the experiments indicate that CHCl₃/MeOH (9:1) and MeOH extracts, tested at a concentration of 400, 200 and 100 μg/mL, dose-dependently reduced the guinea-pig ileum contractions, whereas the petroleum ether and CHCl₃ extracts did not affect it. Furthermore, the partially purified fractions II–V from the MeOH extract, each tested at concentrations of 200, 100 and 50 μg/mL also inhibited E.C.I. Finally the pure compounds 1–2 (5×10⁻⁶–1×10⁻⁵–5×10⁻⁵ M ) isolated and purified from the above fractions significantly reduced, in a dose dependent manner, the electrical contractions of the ileum, whereas compound 3 (5×10⁻⁶–1×10⁻⁵×10⁻⁵ M ) increased them. Since the active compounds 1–3 were respectively identified as protopine, allocryptopine and berberine by NMR, the observed effects could be related mainly to these compounds. © 1997 by John Wiley & Sons, Ltd.     

Inhibiting Activity of Some Glucoindolalkaloids and Iridoids from Sickingia williamsii on Electrically Induced Contractions of Isolated Guinea-pig Ileum

The present study examined the effects of the extracts (petroleum ether, CHCl₃, CHCl₃/MeOH (9:1) and MeOH), partially purified fractions and pure compounds (mainly alkaloids and iridoids) from Sickingia williamsii on the electrically induced contractions of the isolated guinea-pig ileum. The results of our experiments indicate that CHCl₃/MeOH (9:1) and CHCl₃ extracts, tested at concentrations of 300, 150 and 30 μg/mL, dose-dependently reduced the guinea-pig ileum electrical contractions, whereas MeOH and petroleum ether extracts did not affect it. Furthermore, both the partially purified fractions I–IV each tested at concentrations of 500, 250 and 100 μg/mL from the CHCl₃/MeOH (9:1) extract and some pure compounds (10⁻⁴ M , 5×10⁻⁵ M and 2.5×10⁻⁵ M ) isolated and purified from the above fractions significantly reduced, in a dose dependent manner, the electrical contractions of the ileum. As the active pure compounds possess an indole nucleus or/and an iridoid nucleus in their structures, the inhibitory effects appear to depend on these structures.     

固相萃取结合HPLC-MS测定人血浆中佐米曲坦及相对生物利用度

 目的建立人血浆中佐米曲坦的HPLC-MS测定法,研究两种佐米曲坦片的相对生物利用度。方法以舒马曲坦为内标,血浆样品由固相萃取,经Nucleodur C₁₈柱分离后采用质谱检测器检测。18名健康志愿者采用自身对照随机交叉试验设计,分别单剂量口服佐米曲坦片5mg后测定二者相对生物利用度。结果佐米曲坦与内标分离度好,内源性杂质不干扰测定,曲线方程为Y=0.004764X+0.001114,r=0.9995。在0.25～40μg·L^-1内佐米曲坦质量浓度与峰面积比的线性关系良好,最低定量限为0.25μg·L^-1,佐米曲坦萃取回收率为86.7%～96.4%(n=5),内标萃取回收率为79.7%～81.4%(n=15),方法回收率为102.2%～106.0%(n=5),日内精密度(RSD)2.28%～3.42%(n=5);日间精密度(RSD)为3.42%～5.45%(n=5)。单次服用5mg佐米曲坦片试验制剂或参比制剂后的药动学参数AUC_0～16分别为(59.6±24.4)和(56.6±31.2)μg·h·L^-1,AUC_0～∞分别为(62.3±25.9)和(60.2±24.0)μg·h·L^-1,ρ_max分别为(12.4±4.2)和(12.7±4.4)μg·L^-1,t_max(1.9±0.5)和(2.1±0.4)h。相对生物利用度为(107.1±25.7)%。结论该方法简单,准确度高,灵敏度好,可用于佐米曲坦在人体内过程研究。方差分析结果表明,两种制剂的主要药动学参数之间无明显差异,双单侧t检验结果表明,两种制剂为生物等效制剂。     

Effect of Rubia cordifolia extract on acetaminophen and CCl4-induced hepatotoxicity

The hepatoprotective activity of an aqueous-methanol extract of Rubia cordifolia (Rubiaceae) was investigated against acetaminophen and CCl₄-induced hepatic damage. Acetaminophen produced 100% mortality at a dose of 1 g/kg in mice while pretreatment of animals with plant extract (500 mg/kg) reduced the death rate to 30%. Acetaminophen at a dose of 640 mg/kg produced liver damage in rats as manifested by the rise in serum levels of GOT and GPT to 1447±182 and 899±201 IU/L (n = 10) respectively, compared with respective control values of 97±10 and 36±11. Pretreatment of rats with plant extract (500 mg/kg) lowered significantly (p <0.005) the respective serum GOT and GPT levels to 161±48 and 73±29. Similarly, hepatotoxic dose of CCl₄ (1.5 mL/kg; orally) raised the serum transaminases (GOT and GPT) levels to 422±102 and 354±74 IU/L (n = 10) respectively compared with respective control values of 99±15 and 29±08 IU/L. The same dose of plant extract (500 mg/kg) was able to prevent significantly (p <0.01) the CCl₄-induced rise in serum enzymes and the estimated values of GOT and GPT were 95±09 and 33±07 IU/L, respectively. Moreover, it prevented CCl₄-induced prolongation in pentobarbital sleeping time confirming the hepatoprotective effects of the extract.     

Herbal medicine Catuama induces endothelium-dependent and -independent vasorelaxant action on isolated vessels from rats,guinea-pigs and rabbits

The present study was designed to examine the vasorelaxant action of the herbal medicine Catuama and the hydroalcoholic extracts (HE) of each plant present in this product and to compare their effects with that caused by acetylcholine (ACh) in intact (⁺E) or in endothelium-rubbed (⁻E) rings of rat thoracic aorta (RA), guinea-pig pulmonary artery (GPPA), guinea-pig mesenteric artery (GPMA), rabbit pulmonary artery (RPA), rabbit mesenteric artery (RMA) precontracted with noradrenaline (NA) or phenylephrine (PE). The extract of Catuama (1-3000 μg/mL) produced graded relaxation of RA, ⁺E or ⁻E, with mean EC₅₀ of 430 μg/mL and ≊ 3000 μg/mL and E_max of 81 % ± 15 % and 47% ± 4 %, respectively. The nitric oxide (NO) synthase inhibitor, N^ω-nitro-L -arginine (L -NOARG, 100 μM ), inhibited in vasorelaxant action (p < 0.05) in RA (⁺E), while indomethacin (3 μM ), propranolol (1 μM ), glibenclamide (1 μM ), methylene blue (10 μM ) and apamin (0.1 μM ) had no significant effect. ACh (1-1000 μM ) caused graded relaxation in RA with ⁺E, these effects being markedly antagonized by L -NOARG (100 μM ), methylene blue (10 μM ) and partially by apamin (0.1 μM ), but not by indomethacin (3 μM ), glibenclamide (1 μM ) or propranolol (1 μM ). The Catuama extract (1-3000 μg/mL) produces partial relaxations in rings of RMA (mean EC₅₀ of 1073 μg7/ml and E_max of 56 % ± 13 %), an effect which was antagonized by L -NOARG (100 μM ). In RPA (⁺E) the extract produces partial relaxation followed by contraction (E_max 28 % ± 6 %), an effect which was abolished by L -NOARG (100 μM ) or methylene blue (10 μM ). The extract caused graded relaxation in rings of GPPA and GPMA with mean EC₅₀ values of 60 μg/mL and 1148 μg/mL and E_max 96% ± 2% and 88% ± 12%, respectively. L -NOARG (100 μM ) blocked the Catuama extract vasorelaxation in GPPA and only partially in GPMA, but markedly antagonized the vasorelaxations caused by ACh in both GPPA andRMA. The HE Paullinea cupana, Zinziber officinalis and Trichilia catigua (1-3000 μg/mL) caused a graded vasorelaxant effect ⁺E of RA with a mean EC₅₀ of 22, 55 and 1793 μg/mL and E_max 100%, 86% ± 7% 70% ± 2%, respectively. In addition the HE of P. cupana also caused graded relaxation in ⁻E of RA with EC₅₀ and E_max of 233 μg/mL and 100%, respectively, while T. catigua and Z. officinalis produced partial relaxation in RA ⁺E. In contrast the HE of Ptychopetalum olacoides caused little contraction (46% ± 14%). These results demonstrate that the medicinal herb Catuama produces significant vasorelaxation responses in vessels from different animal species, and show that its effects are in great part dependent on the release of NO or NO-derived substances. Our results also demonstrate that the vasorelaxant action of the product Catuama seems to be due to the action of the active principles present mainly in P. cupana; T. catigua and, to a lesser extent, in Z. officinalis. Such results may contribute to the explanation of its beneficial effect of Catuama herbal medicine in the management of cardiovascular disturbances. © 1997 John Wiley & Sons, Ltd.     

HPLC测定白花前胡蜜炙前后3种香豆素类成分的含量

 目的 对前胡蜜炙前后3种香豆素类成分进行比较研究。方法 HPLC同时测定3种香豆素类成分白花前胡甲素、白花前胡乙素、白花前胡E素的含量,Agilent TC-C₁₈ (2)柱,流动相为甲醇-水（3︰1）,检测波长320 nm,流速0.8 mL·min-1,柱温35 ℃。结果 3个成分的线性关系较好（r>0.999 6）,测定范围分别为0.204 4~2.044, 0.077 6~0.776,0.077 2~0.772 μg,平均回收率分别为101.66%,97.45%,97.79%。前胡不同饮片中3种香豆素类成分含量有差异。结论 所建立的方法可用于同时测定前胡不同饮片中3种香豆素的含量,为前胡不同饮片质量评价标准的制定提供了科学依据。     

巯嘌呤甲基转移酶活性对硫唑嘌呤中间代谢物6-巯基嘌呤药动学的影响

 目的通过对硫唑嘌呤中间代谢物6-巯基嘌呤(6-mercaptopurine,6-MP)药动学的研究,初步探讨巯嘌呤甲基转移酶(thiopurine methyltransferase,TPMT)活性对6-MP药动学的影响。方法根据红细胞中TPMT活性,受试者分成高酶活性组[(14.52±2.10)μmol·h^-1·L^-1RBCs,n=16]和低酶活性组[(7.02±2.44)μmol·h^-1·L^-1RBCs,n=4]。受试者早晨空腹口服硫唑嘌呤100 mg,8 h动态采集静脉血,HPLC测定血浆中6-MP浓度,采用WinNonlin程序进行房室模型拟合及药动学参数计算。结果:6-MP药动学符合一室模型特点,6-MP血浆浓度较低,高酶活性组和低酶活性组ρ_max分别是(0.048 3±0.024 3)和(0.039 1±0.010 8)mg·L^-1;两组AUC分别是(0.132 0±0.047 2)和(0.093 2±0.012 5)mg·h·L^-1;6-MP半衰期短,分别是(1.09±0.65)和(1.25±1.05)h;6-MP表观分布容积大,两组Vd/F分别是(625.63±258.82)和(949.83±670.27)L。高酶活性组和低酶活性组在t_max和t_lag存在显著性差异(P<0.05),而K_a,ρ_max,AUC,K_e,t_1/2,Vd/F,CL/F等药动学参数无显著性差异(P>0.05)。结论由于6-MP代谢的复杂性及独特的组织分布特性,使得TPMT活性对6-MP药动学的影响变得不明显,目前还不能借助6-MP药动学来推测硫唑嘌呤的治疗效果和毒性情况。     

国产盐酸托烷司琼片、胶囊与进口片剂人体生物等效性比较

 目的评价国产盐酸托烷司琼片、胶囊与进口参比制剂是否生物等效。方法男性健康受试者24名,随机分成6组,三交叉po受试制剂和参比制剂各20 mg,在一定时间点取静脉血分离血清,用高效液相色谱紫外检测法测定人血清中托烷司琼浓度,所得数据经BECS软件处理得到主要药动学参数。结果国产盐酸托烷司琼片、胶囊与进口参比制剂托烷司琼的t_max均为(1.7±0.4)h,ρ_max分别为:(36.9±8.9),(36.3±8.9)和(36.1±9.3)μg·L^-1,用梯形法计算所得的AUC_0-t分别为(443±176),(448±196)和(443±191)μg·h·L^-1。对经对数转换后的ρ_max,AUC_0-t进行方差分析和双单侧t检验及90%可信限判断,盐酸托烷司琼片、胶囊的ρ_max落在参比制剂的90.7%-116.2%和89.1%-114.2%内,AUC_0-t落在参比制剂的82.8%-124.0%和82.7%-123.8%内,t_max经非参数检验法检验无显著差异,盐酸托烷司琼片、胶囊AUC_0-t的相对生物利用度分别为(102±9)%和(102±10)%。结论3种制剂具有生物等效性。     

Antispasmodic,bronchodilator and blood pressure lowering properties of Hypericum oblongifolium – possible mechanism of action

The crude extract of Hypericum oblongifolium (Ho.Cr), which tested positive for flavonoids, saponins and tannins caused concentration‐dependent (0.1–1.0 mg/mL) relaxation of spontaneous and high K⁺ (80 mM)‐induced contractions in isolated rabbit jejunum preparations, suggesting a Ca⁺⁺ antagonistic effect, which was confirmed when pretreatment of the tissue with Ho.Cr produced a rightward shift in the Ca⁺⁺ concentration‐response curves, like that caused by verapamil. Ho.Cr relaxed carbachol (1 μM) and high K⁺‐induced contractions in guinea pig tracheal preparations. It caused a dose‐dependent (3–100 mg/kg) fall in arterial blood pressure of rats under anesthesia. In isolated guinea pig atria, Ho.Cr caused inhibition of both atrial force and rate of spontaneous contractions. When tested in rabbit aortic rings, Ho.Cr exhibited a vasodilator effect against phenylephrine (1 μM) and high K⁺‐induced contractions. These results indicate that Ho.Cr possesses gastrointestinal, respiratory and cardiovascular inhibitory effects, mediated via a Ca⁺⁺ antagonist mechanism. Copyright © 2009 John Wiley & Sons, Ltd.     

In vitro pharmacological evaluation of the dichloromethanol extract from Schinus molle l.

The pharmacological activity of the dichloromethanol extract of Schinus molle L. (SM-DCM) was analysed in in vitro models. Preincubation of the isolated guinea-pig ileum or rat uterus preparations with the extract (100 μg/mL) abolished the contractile effects of histamine and serotonin respectively. At the same dose, the extract partially reduced the contractile effects of acetylcholine on the isolated rat duodenum. A 10 μg/mL dose showed an inhibitory effect on histamine and serotonin, but not on acetylcholine-induced contractions (NS). No significant effect was found with a 1 μg/mL dose. © 1998 John Wiley & Sons, Ltd.     

Pharmacological studies on hypotensive and spasmolytic activities of pure compounds from Moringa oleifera

Bioassay directed fractionation of an ethanolic extract of Moringa oleifera (MO) leaves resulted in the isolation of four pure compounds, niazinin A (1), niazinin B (2), niazimicin (3) and niaziminin A + B (4 + 5). Intravenous administration of either one of the compounds (1–10 mg/kg) produced hypotensive and bradycardiac effects in anaesthetized rats. Pretreatment of the animals with atropine (1 mg/kg) completely abolished the hypotensive and bradycardiac effects of acetylcholine (ACh), whereas cardiovascular responses to the test compounds remained unaltered, ruling out the possible involvement of muscarinic receptor activation. In isolated guinea-pig atria all the compounds (50–150 μg/mL) produced negative inotropic and chronotropic effects. Each compound inhibited K⁺ -induced contractions in rabbit aorta as well as ileal contractions induced by ACh or histamine at similar concentrations. Spontaneous contractions of rat uterus were also inhibited equally by all compounds. These data indicate that the direct depressant action of these compounds exhibited on all the isolated preparations tested is probably responsible for its hypotensive and bradycardiac effects observed in vivo. Moreover, spasmolytic activity exhibited by the constituents of the plant provides a scientific basis for the traditional uses of the plant in gastrointestinal motility disorders.     

盐酸金刚乙胺颗粒人体生物等效性研究

 目的用高效液相色谱-质谱法(LC-MS)测定受试者口服盐酸金刚乙胺制剂后的血药浓度,估算受试制剂和参比制剂的药动学参数,评价两种制剂的生物等效性和相对生物利用度。方法采用随机二交叉设计试验,20例男性健康志愿受试者,单剂量口服受试制剂盐酸金刚乙胺颗粒和参比制剂盐酸金刚乙胺片。以LC-MS测定血浆中金刚乙胺的浓度。采用BAPP3.0软件处理计算主要药动学参数。结果受试制剂和参比制剂血浆中金刚乙胺的t_1/2分别为(26.46±4.48)和(27.41±4.42)h;ρ_max分别为(84.5±17.7)和(93.1±17.8)μg·L^-1;t_max分别为(4.08±2.86)和(4.70±3.59)h;AUC_0-120h分别为(3204±691)和(3450±724)μg·h·L^-1;AUC_0-∞分别为(3395±767)和(3661±820)μg·h·L^-1;人体相对生物利用度为(93.4±10.8)%。结论2种制剂在健康人体内具有生物等效性。     

Pharmacological studies of Striga senegalensis Benth (Scrophulariaceae) as an abortifacient

The methanol extract of Striga senegalensis Benth (Scrophulariaceae) was investigated on isolated rat uterus. Acetylcholine and the methanol extract of the plant produced dose related contractions of smooth muscle of the isolated rat uterus in vitro. Atropine in doses of 2 × 10⁻² to 32 × 10⁻² μg/mL antagonized dose dependently the contraction of the isolated rat uterus produced by both acetylcholine (1.6 × 10⁻¹ μg/mL) and the methanol extract (160 μg/mL). © 1998 John Wiley & Sons, Ltd.     

β‐secretase inhibitory effects of furanocoumarins from the root of Angelica dahurica

In the course of screening antidementia agents from natural products, five β‐secretase (BACE1) inhibitors were isolated from the root extract of Angelica dahurica (Umbelliferae). They were identified as furanocoumarins, isoimperatorin (1), imperatorin (2), (+)‐oxypeucedanin (3), (+)‐byakangelicol (4) and (+)‐byakangelicin (5). Among them, compounds 2 and 4 showed significant inhibitory activity against β‐secretase (BACE1) with IC₅₀ values of 91.8 ± 7.5 and 104.9 ± 2.4 μM , respectively. Compounds 1‐5 inhibited BACE1 activity in a dose‐dependent manner. Copyright © 2009 John Wiley & Sons, Ltd.     

In vitro and in vivo antimalarial activity of cryptolepine,a plant-derived indoloquinoline

Cryptolepine is an indoloquinoline, high yields of which may be extracted from the roots of the West African shrub Cryptolepis sanguinolenta. The use of this plant as a traditional treatment for malaria is widespread in Ghana and is reported to be clinically effective. We have tested cryptolepine for in vitro antiplasmodial activity against the multidrug resistant (K1) strain of Plasmodium falciparum and found it to be highly active with an IC₅₀ value of 0.031±0.0085 (SE) μg/mL, equivalent to 0.134±0.037 μM (n = 3). In a 4-day suppression test there was, however, no significant reduction in parasitaemia in P. berghei-infected mice treated subcutaneously with cryptolepine (7–113 mg/kg/d×4), when compared with untreated controls. Like 9-aminoacridine, this compound appears to intercalate with DNA and this may explain the high degree of antimalarial activity demonstrated in vitro.     

The Anti‐Osteoporosis and Antioxidant Activities of Chemical Constituents from Chrysanthemum indicum Flowers

Two new compounds, chrysinoneside A (1) and (?)‐trans‐chrysanthenol‐6‐O‐β‐D‐glucopyranoside (2), along with 17 known compounds (3–19) were isolated from Chrysanthemum indicum flowers. The total phenolic and flavonoid contents of various fractions were determined. The EtOAC fraction had the highest total phenolic content (525.84 ± 23.51 mg GAE/g DR) and the total flavonoid content (63.49 ± 3.32 mg QE/g DR). The EtOAc and water fractions showed the greatest peroxyl radical‐scavenging capacity and the ability to reduce Cu(I) ions, with ORAC and CUPRAC values ranging from 24.00 ± 0.44 to 28.06 ± 1.35 and 16.90 ± 0.51 to 49.77 ± 0.97 μM, respectively. Compounds 5–11, 18, and 19 displayed strong effects in both peroxyl radical‐scavenging and reducing capacity assays at a concentration of 10 μM. The anti‐osteoporosis activity of these compounds was also evaluated. Compounds 10, 13, and 19 exhibited the most potent tartrate‐resistant acid phosphatase activity in receptor activator of nuclear factor‐κB ligand‐induced osteoclastic RAW 264.7 cells with values of 105.95 ± 1.18, 110.32 ± 3.95, and 112.58 ± 6.42%, respectively. Copyright © 2015 John Wiley & Sons, Ltd.     

氯沙坦及其代谢物在汉族健康人体内药动学研究

 目的 研究氯沙坦及其代谢产物2-丁基-4-氯-1-[[2’-(1H-四唑-5-基）[1,1‘-联苯基]-4-基]甲基]-lH一咪唑-5-羧酸（E-3174）在中国汉族健康受试者体内的药动学。方法 10名健康受试者,男女各半,口服氯沙坦钾片50 mg,定时采血,用HPLC荧光法测定氯沙坦及其代谢物E-3174血药浓度,DAS2.0软件程序进行数据处理并采用SPSS13.0软件进行统计学分析。结果 氯沙坦和E-3174的主要药动学参数如下：ρ_max分别为( 351±167),( 241±60) μg·L^-1; t_max分别为(1.35±1.06),(3.60±1.68) h;t1/2分别为(0.82±0.40),(4.66±1.10) h;AUC_0-24分别为(498±172),(1 853±194) μg ·h·L^-1;AUC_0-∞分别为(523±184),(1 960±182) μg ·h·L^-1。结论 氯沙坦及其代谢物E-3174的药动学特征和参数在个体间存在较大差异,临床治疗中应实行个体化给药方案。     

环维黄杨星D返针晶结晶体对豚鼠心室肌细胞动作电位的影响

目的:观察环维黄杨星D(Cyclovirobuxine D,CVB-D)返针晶结晶体对豚鼠单个心室肌细胞动作电位的影响。方法:使用Langendorff灌流系统离体灌流心脏,急性酶解法分离获得心肌细胞。全细胞膜片钳技术电流钳模式记录动作电位。Tyrode氏液和药物溶液交替反复灌流单个心室肌细胞。结果:CVB-D中浓度组用药后动作电位0相除极幅度(APA)从(113.3±6.3)mV下降至(110.2±6.4)mV(n=6,P0.01),复极至50%时动作电位时程(APD50)从(616.3±68.0)ms延长至(657.4±79.5)ms(n=6,P0.01),复极至90%时动作电位时程(APD90)从(633.5±71.2)ms延长至(669.2±74.4)ms(n=6,P0.01),复极50%至90%动作电位时程(APD50-90)从(15.9±6.0)ms延长至(20.1±5.2)ms(n=6,P0.01),动作电位3相复极速率(V3)从(-2.6±0.8)V/s减慢至(-2.4±0.7)V/s(n=6,P0.01)。Tyrode氏液和高浓度药物溶液交替反复灌流后APD50-90呈递增趋势而V3呈递减趋势,其他指标的变化趋势与中浓度组一致。CVB-D低浓度组各项指标的变化趋势缺乏统计学意义。结论:体外应用CVB-D返针晶结晶体引起心室肌细胞APA减小,APD50,APD90,APD50-90延长,V3减慢。以上影响可能是其在临床上具有增强心肌收缩力和抗心律失常作用的药理机制。     

复方丹参注射液Ⅱ中丹酚酸B在大鼠体内的HPLC测定

目的:探讨复方丹参注射液Ⅱ的制备及其指标成分丹酚酸B在大鼠体内的含量测定方法。方法:通过羟丙基-β-环糊精包合增加降香挥发油溶解性;用HPLC法测定主成分丹酚酸B在大鼠体内的含量。结果:成功制备复方丹参注射液Ⅱ,建立注射液中指标成分丹酚酸B在大鼠体内的HPLC测定方法。结论:复方丹参注射液Ⅱ的制备工艺可行,指标成分丹酚酸B在大鼠体内的含量测定方法准确可靠。