豨莶脂溶性成分的研究

从豨莶(Siegesbeckia orientalis L.)的地上部分,分离出八个化合物,其中I和I根据理化性质和光谱数据确定其结构为ent-17-acetoxy-18-isobutyryloxy-16(α)-kauran-19-oicacid(I)和ent-17-ethoxy-16(α)-kauran-19-oicacid(II),均为新化合物,分别被命为豨莶酯酸(siegesesteric acid,I)和豨莶醚酸(siegesetheric acid,I)。其余化合物分别鉴定为腺梗豨莶萜醇酸(ent-16β,17-dihydroxy-kauran-19-oicacid,II),奇任醇(kirenol,IV,β-谷甾醇葡萄糖甙(β-sitosterolglucoside,V),二十一醇(heneicosanol,VI),花生酸甲酯(methyl arachidate,VII)和β-谷甾醇(β-sitosterol,VII)。除奇任醇和β-谷甾醇外,均为首次从该植物中分得。     

毛梗稀莶抗生育活性成分的研究

自菊科植物毛梗豨莶Siegesbeckia glabrescens Mak的全草中分得一个新的二萜甙,命名为豨莶新甙(neodarutoside),经光谱(IR,¹ HNMR,¹³ CNMR和MS)分析,确定结构为(I);同时分得的二萜有豨莶精醇(darutigenol,Ⅳ)和豨莶甙(d&rutoside,Ⅴ)。豨莶甙(Ⅴ)在20～40 mg/kg剂量时,对大鼠有明显抗早孕作用。     

HPLC-RID法测定腺梗豨莶药材中豨莶精醇等4种化合物的含量

目的建立测定腺梗豨莶中豨莶精醇、16β,17-二羟基-贝壳杉烷-19-羧酸、16α氢-贝壳杉烷-17,19-二羧酸和3',4'-二甲氧基槲皮素含量的高效液相色谱示差折光检测方法(HPLC-RID)。方法以十八烷基硅烷键合相为固定相,流动相为体积分数0.3%甲酸溶液-乙腈(体积比42∶55),流速为1.0 mL·min-1,示差检测器光学元件温度为40℃,柱温30℃。结果豨莶精醇的线性范围为0.202².02 g·L-1,16β,17-二羟基-贝壳杉烷-19-羧酸的线性范围为0.5102.02 g·L-1,16β,17-二羟基-贝壳杉烷-19-羧酸的线性范围为0.510⁵.10 g·L-1,16α氢-贝壳杉烷-17,19-二羧酸的线性范围为0.2985.10 g·L-1,16α氢-贝壳杉烷-17,19-二羧酸的线性范围为0.298².98 g·L-1,3',4'-二甲氧基槲皮素的线性范围为0.1002.98 g·L-1,3',4'-二甲氧基槲皮素的线性范围为0.100¹.00 g·L-1,4种化合物线性关系良好(r>0.999);平均加样回收率在99.2%1.00 g·L-1,4种化合物线性关系良好(r>0.999);平均加样回收率在99.2%¹04.9%内;RSD小于3.4%。结论该方法简便、准确、重复性良好,适用于腺梗豨莶中4种成分的同时测定。     

豨莶液的定性定量测定方法

目的：建立控制豨莶液质量的方法。方法：采用HPLC法定量测定豨莶液中的奇任醇含量。色谱条件：色谱柱为Allsphere ODS（4.6mm×250mm,5μm）,流动相为乙腈-水-醋酸-三乙胺（25∶75∶0.1∶0.2）,流速为1.0mL/min,检测波长为215nm,进样量为10μL,柱温为20℃。定性鉴别采用薄层色谱法。结果：在本色谱条件下,奇任醇在0.4168-1.6672μg范围内呈良好的线性关系。平均回收率为99.78%（RSD=1.51%,n=6）。薄层色谱中豨莶草的色谱斑点清晰、无干扰。结论：本法定性定量结合,准确可靠,重现性好,快速简便,可用于豨莶液的质量控制。     

高效液相色谱梯度洗脱法同时测定关节痛丸中β-蜕皮甾酮、豨莶苷、奇壬醇和豨莶精醇的含量

目的建立HPLC梯度洗脱法同时测定关节痛丸中β-蜕皮甾酮、豨莶苷、奇壬醇和豨莶精醇的含量。方法采用Diamonsil C18(4.6 mm×200 mm,5μm),以乙腈-0.1%甲酸溶液为流动相,进行梯度洗脱,流速1.0 m L·min~(-1),柱温30℃,波长切换法检测(0~17 min,250 nm,β-蜕皮甾酮;17~60min,215 nm,豨莶苷、奇壬醇和豨莶精醇),进样量为10μL。结果β-蜕皮甾酮、豨莶苷、奇壬醇和豨莶精醇4个成分的线性范围分别为4.35~87.00μg·m L~(-1)(r=0.9993)、3.78~75.60μg·m L~(-1)(r=0.9999)、8.51~170.20μg·m L~(-1)(r=0.9994)、5.35~107.00μg·m L~(-1)(r=0.9997);平均加样回收率及相应的RSD分别为98.8%(1.4%)、99.3%(1.3%)、97.4%(1.0%)、99.0%(1.2%)。结论本文建立的方法,方法专属性强,测定结果准确,可有效保障关节痛丸临床用药安全。     

3种正品豨莶草的鉴别

目的建立药典版中豨莶、腺柄豨莶、毛梗豨莶鉴别提供实验依据。方法采用显微特征,理化和薄层色谱的鉴别方法。结果3种正品豨莶具不同鉴别特征。结论能更准确地把3种正品豨莶草区别。     

豨莶通栓胶囊治疗急性期动脉粥样硬化性血栓性脑梗死的疗效观察

目的探究豨莶通栓胶囊治疗急性期动脉粥样硬化性血栓性脑梗死的临床疗效。方法 87例急性期动脉粥样硬化性血栓性脑梗死患者,按随机数字表法分为试验组(46例)和对照组(41例)。对照组给予常规治疗,试验组在对照组基础上给予豨莶通栓胶囊治疗。比较两组患者的临床疗效、美国国立卫生研究院卒中量表(NIHSS)评分及日常生活活动能力量表(BI)评分。结果试验组治疗总有效率89.13%高于对照组的70.73%,差异有统计学意义(P<0.05)。治疗后,两组NIHSS评分低于治疗前, BI评分高于治疗前,且试验组NIHSS评分(3.59±0.32)分低于对照组的(5.25±0.56)分, BI评分(76.62±5.86)分高于对照组的(61.82±6.70)分,差异有统计学意义(P<0.05)。结论豨莶通栓胶囊治疗急性期动脉粥样硬化性血栓性脑梗死临床疗效显著,可有效改善患者脑神经功能,提升其生活质量,值得临床推广。     

HPLC-RID法测定腺梗豨莶药材中奇壬醇等5种化合物的含量

目的建立测定腺梗豨莶中ent-16β,17,18-三羟基贝壳杉烷-19-羧酸、奇壬醇、ent-17,18-二羟基贝壳杉烷-19-羧酸、豨莶苷、ent-16β,17-二羟基贝壳杉烷-19-羧酸含量的高效液相色谱示差折光检测方法(HPLC-RID)。方法以十八烷基硅烷键合相为固定相,流动相为体积分数0.5%甲酸溶液-乙腈(体积比72∶28),示差检测器光学元件温度为40℃,流速为1.0 mL·min-1。结果 5种化合物线性关系良好(r>0.999),ent-16β,17,18-三羟基贝壳杉烷-19-羧酸和ent-17,18-二羟基贝壳杉烷-19-羧酸的线性范围为0.10⁰.50 g·L-1,奇壬醇的线性范围为0.500.50 g·L-1,奇壬醇的线性范围为0.50².5 g·L-1,豨莶苷的线性范围为0.202.5 g·L-1,豨莶苷的线性范围为0.20¹.0 g·L-1,ent-16β,17-二羟基贝壳杉烷-19-羧酸的线性范围为0.421.0 g·L-1,ent-16β,17-二羟基贝壳杉烷-19-羧酸的线性范围为0.42².1 g·L-1;平均加样回收率在98.3%2.1 g·L-1;平均加样回收率在98.3%¹01.1%内,RSD小于3.5%。结论该方法简便、准确、重复性良好,适用于腺梗豨莶中5种成分的同时测定。     

不同物种稀莶草急性毒性的比较

豨莶草为菊科植物,2005年版<药典>收载3个物种,分别为稀莶Siegesbeckia orientalis L.、腺梗豨莶Siegesbeckia pubescens Makino或毛梗豨莶Siegesbeckiaglabrescens Makino[1].<唐本草>、<本经逢原>和<本草纲目>等历代医书对其毒性考证认为"有小毒".     

腺梗豨莶化学成分的分离与鉴定

目的对中药腺梗豨莶(Siegesbeckia pubescensMakino.)进行化学成分的研究。方法通过硅胶柱色谱、ODS、Sephadex LH-20和制备HPLC等手段分离,利用理化性质和光谱方法鉴定结构。结果分离得到8个化合物,分别鉴定为过氧化麦角固醇(ergosterol peroxide,1)、尿嘧啶(uracil,2)、豆甾-4-烯-3-酮(stigmast-4-en-3-one,3)、豆甾醇(stigmasterol,4)、奇任醇(kirenol,5)、琥珀酸(succinicacid,6)、β-谷甾醇(β-sitosterol,7)、胡萝卜苷(daucosterol,8)。结论化合物1~3首次从该属植物中得到。     

Phage types and drug susceptibility patterns of Staphylococcus aureus from two hospitals in northwest Ethiopia.

Fifty-eight Staphylococcus aureus strains from Gonder College of Medical Sciences Hospital, (43 isolates from patients and 15 from carriers) and 28 from Debre Tabor Hospital (14 each from patients and carriers), both in northwest Ethiopia, were phage typed in 1988. Eighty-one of the 86 strains were recognized by their phage types. A multiresistant strain of type 29 was frequent among Gonder patients'. This strain was also recovered from the hospital personnel. Other well known multiresistant strains of phage type NT/A994 and 85/A994 were identified among patients from Gonder and phage type 85/A994 was recovered from 5 patients and 4 carriers from Debre Tabor. These findings suggest cross-infection with virulent strains of Staphylococcus aureus in both hospitals. All 86 phage-typed strains were tested for susceptibility to 7 antibiotics. A high frequency of multiple resistance was observed. Double resistance to penicillin and tetracycline was frequent among patients strains from Gonder. Among strains of phage type 85/A994 multiresistance to penicillin, chloramphenicol, tetracycline, streptomycin, erythromycin and oxacillin was found. Strains of phage type 85/A994 and NT/A994 were resistant to mercury. No plasmid DNA was detected in one strain of 85/A994 investigated.     

Bacteria isolated from surgical infections and their susceptibilities to antimicrobial agents --special references to bacteria isolated between April 2008 and March 2009

Bacteria isolated from infections in abdominal surgery during the period from April 2008 to March 2009 were investigated in a multicenter study in Japan, and the following results were obtained. In this series, 712 strains including 18 strains of Candida spp. were isolated from 173 (80.5%) of 215 patients with surgical infections. Three hundred and sixty-six strains were isolated from primary infections, and 346 strains were isolated from postoperative infections. From primary infections, anaerobic Gram-negative bacteria were predominant, followed by aerobic Gram-negative bacteria, while from postoperative infections aerobic Gram-positive bacteria were predominant, followed by anaerobic Gram-negative bacteria. Among aerobic Gram-positive bacteria, the isolation rate of Enterococcus spp. was highest, followed by Streptococcus spp., and Staphylococcus spp. in this order, from primary infections, while Enterococcus spp. was highest, followed by Staphylococcus spp. from postoperative infections. Among aerobic Gram-negative bacteria, Escherichia coli was the most predominantly isolated from primary infections, followed by Klebsiella pneumoniae and Pseudomonas aeruginosa, in this order, and from postoperative infections, P aeruginosa was most predominantly isolated, followed by E. coli, Enterobacter cloacae, and K. pneumoniae. Among anaerobic Gram-positive bacteria, the isolation rate of Eggerthella lenta was the highest from primary infections, followed by Parvimonas micra, Streptococcus constellatus and Gemella morbillorum, and from postoperative infections, E. lenta was most predominantly isolated. Among anaerobic Gram-negative bacteria, the isolation rate of Bacteroides fragilis was the highest from primary infections, followed by Bacteroides thetaiotaomicron, Bacteroides ovatus and Bilophila wadsworthia, and from postoperative infections, B. fragilis was most predominantly isolated, followed by B. thetaiotaomicron, B. wadsworthia and B. ovatus, in this order. In this series, we noticed no vancomycin-resistant methicillin-resistant S. aureus, and Enterococcus spp., nor multidrug-resistant P aeruginosa. We should carefully follow up B. wadsworthia which was resistant to various antibiotics, and also Bacteroides spp. which was resistant to many beta-lactam antibiotics.     

Bacteria isolated from surgical infections and its susceptibilities to antimicrobial agents--special references to bacteria isolated between April 2009 and March 2010

Bacteria isolated from surgical infections during the period from April 2009 to March 2010 were investigated in a multicenter study in Japan, and the following results were obtained. In this series, 671 strains including 16 strains of Candida spp. were isolated from 174 (79.1%) of 220 patients with surgical infections. Four hundred and eleven strains were isolated from primary infections, and 244 strains were isolated from surgical site infection. From primary infections, anaerobic Gram-negative bacteria were predominant, followed by aerobic Gram-negative bacteria, while from surgical site infection aerobic Gram-positive bacteria were predominant, followed by anaerobic Gram-negative bacteria. Among aerobic Gram-positive bacteria, the isolation rate of Enterococcus spp. was highest, followed by Streptococcus spp., and Staphylococcus spp. in this order, from primary infections, while Enterococcus spp. was highest, followed by Staphylococcus spp. from surgical site infection. Among aerobic Gram-negative bacteria, Escherichia coli was the most predominantly isolated from primary infections, followed by Klebsiella pneumoniae, Enterobacter cloacae and Pseudomonas aeruginosa, in this order, and from surgical site infection, E. coli was most predominantly isolated, followed by P. aeruginosa and E. cloacae. Among anaerobic Gram-positive bacteria, the isolation rate of Eggerthella lenta was the highest from primary infections, followed by Parvimonas micra, Streptococcus constellatus and Finegoldia magna, and from surgical site infection, E. lenta was most predominantly isolated. Among anaerobic Gram-negative bacteria, the isolation rate of Bilophila wadsworthia was the highest from primary infections, followed by Bacteroides fragilis, Bacteroides ovatus and Bacteroides thetaiotaomicron, and from surgical site infection, B. fragilis was most predominantly isolated, followed by B. ovatus, B. wadsworthia and B. thetaiotaomicron, in this order. In this series, we noticed no vancomycin-resistant Gram-positive cocci, nor multidrug-resistant P. aeruginosa. We should carefully follow up B. wadsworthia which was resistant to various antibiotics, and also Bacteroides spp. which was resistant to many beta-lactam antibiotics.     

Bacteria isolated from surgical infections and their susceptibilities to antimicrobial agents--special references to bacteria isolated between April 2000 and March 2001

Tendency of isolated bacteria from infections in general surgery and their antimicrobial susceptibilities during the period from April 2000 to March 2001 were investigated in a multicenter study in Japan, and the following results were obtained. The number of cases investigated as objectives was 234 for one year. A total of 388 strains (136 strains from primary infections and 252 strains from postoperative infections) were isolated from 165 cases (70.5% of total cases). In primary infections, anaerobic Gram-positive bacteria were predominant, while from postoperative infections, aerobic Gram-positive bacteria were predominant. Among aerobic Gram-positive bacteria, the isolation rate of Enterococcus faecalis was the highest, followed by that of Staphylococcus aureus from postoperative infections. Among anaerobic Gram-positive bacteria, the isolation rate of Peptostreptococcus spp. was the highest from both types of infections. Among aerobic Gram-negative bacteria, Escherichia coli was the most predominantly isolated from primary infections, followed by Klebsiella pneumoniae and Pseudomonas aeruginosa in this order, and from postoperative infections, P. aeruginosa was the most predominantly isolated, followed by Enterobacter spp. and Klebsiella spp. Among anaerobic Gram-negative bacteria, the isolation rate of Bacteroides fragilis group was the highest from both types of infections. There was no vancomycin-resistant S. aureus nor Enterococcus spp. Among anaerobic bacteria, there were many resistant strains against penicillins and cephems with MICs higher than 100 micrograms/ml, and the same trend was observed among other Bacteroides spp. and Prevotella spp.     

Intestinal absorption of sodium cefoxitin in rats: effect of formulation

The absorption of cefoxitin from rat intestine, rectum and small intestine was greater when the powdered form was administered than when an aqueous solution was given. Cefoxitin absorption from the small intestine was significantly increased after its administration in suppository form prepared with a triglyceride base, although rectal absorption from the suppository did not differ from that of the drug in powdered form. The increase in absorption by the small intestine from the suppository form may be due to fatty acids produced from triglyceride by lipase.     

假奓包叶不同部位挥发油的分析比较

目的对假奓包叶根皮、茎皮、果壳和种子的挥发油成分进行比较。方法采用水蒸气蒸馏法提取这4个部位中的挥发油,对提取物进行GC-MS分析。结果从假奓包叶根皮中检测到9个挥发油成分,占挥发油色谱总峰面积的88.85%;从茎皮中检测到11个挥发油成分,占挥发油色谱总峰面积的87.24%;从果壳中检测到11个挥发油成分,占挥发油色谱总峰面积的71.21%;从种子中检测到11个挥发油成分,占挥发油色谱总峰面积的87.76%。分别确定它们的相对含量,并比较其一致性。结论首次对假奓包叶根皮、茎皮、果壳和种子挥发油进行了提取和分析比较。     

Objective monitoring of graft-versus-host disease: alpha 1-antichymotrypsin concentration changes after bone marrow transplantation in patients developing graft-versus-host reactions

The levels of alpha 1-antichymotrypsin (ACT) was monitored in patients who underwent bone marrow transplantation. Seven received HLA-identical sibling bone marrow grafts, two received transplants from twins and one was given HLA-nonidentical marrow from his father. A dramatic increase of ACT was observed in all patients who developed graft-versus-host disease (GvHD). ACT did not rise at all in the case of patients who received marrow from twins, even in a patient who was given three transplants from the same donor. The patient transplanted from his father died from GvHD and the increase of ACT was the greatest fluctuation measured.     

Release of leukotrienes C (LTC) and D (LTD) from inflammatory macrophages during phagocytosis of zymosan and bacteria

Release of slow-reacting substance (SRS) was obtained from resident mouse peritoneal macrophages (R-M phi) upon stimulation with phagocytic stimuli (zymosan, bacteria). The release of SRS from thioglycollate elicited M phi was impaired, whereas that from BCG-elicited M phi was quantitatively unaffected. However, using a high pressure liquid chromatography separation procedure, qualitative variations between SRS released from R-M phi and BCG-M phi were observed. In both cases, LTC was the major component released from M phi, but greater amounts of LTD were released from BCG-M phi than from R-M phi. These data indicate that local environment alters leukotriene generation by M phi.     

BP-ANN结合正交试验设计优化白及多糖提取工艺研究

目的:优化白及多糖的提取工艺.方法:加热回流法提取白及多糖,应用UV测定含量并计算白及多糖得率.以正交试验其中的7组数据作为训练数据样本,剩余2组数据作为验证数据样本,采用误差反向传播人工神经网络(BP-ANN)进行建模及分析,以白及多糖得率作为考察指标,仿真模拟预测白及多糖最佳提取工艺参数.结果:正交试验优化的提取工...     

Geographic and ontogenic variation in venom of the western diamondback rattlesnake (Crotalus atrox)

Venom samples from western diamondback rattlesnakes (Crotalus atrox) from 13 localities in the United States were tested for i.v. and s.c. lethality for mice, protease activity, hemorrhagic activity, and the presence of Mojave toxin. Electrophoresis on polyacrylamide gel was used to compare protein composition. The neutralizing effect of two commercial antivenoms was evaluated against selected samples of venom. Venom of young snakes from north Texas was compared with that of adults from the same locality. Venom samples from the southwest portion of the range showed highest lethality, those from the northeast portion lowest. This trend was reversed with respect to protease activity. Hemorrhagic activity showed little geographic variation, but northern samples tended to be slightly higher. Differences in venom protein composition were evident between snakes from the eastern and western portions of the range. Mojave toxin in small to trace amounts was detected in two Arizona venom samples and one from west Texas. Antivenoms were relatively ineffective in neutralizing lethality. Venom of young snakes from north Texas was much more lethal by s.c. injection than that of adult snakes from any part of the range, but very low in protease activity. Hemorrhagic activity was about equal to that of adult snakes from the same region. Fifteen months later, lethality had declined almost five-fold, and protease activity had approached adult levels. There was a distinct change in protein composition. Mojave toxin was not detected in venoms of the young snakes.