蚕沙叶绿素的降解及二氢卟吩P6酰胺衍生物的合成

以蚕沙粗品叶绿素为原料,经降解、氧化反应制得紫红素－１８（３）,并以３为关键中间体合成了１０个二氢卟吩Ｐ６酰胺衍生物,其中９个为首次报道。     

叶绿素降解产物金属络合物的合成及其对~(60)Co辐射小鼠的放射保护作用

通过蚕沙叶绿素的降解反应，研究了焦脱镁叶绿酸ａ、二氢卟吩ｅ６单甲酯及紫红素１８等二氢卟吩衍生物的制备方法，首次设计合成了蚕沙叶绿素降解产物的钴、铜、锌金属络合物。在确认结构的基础上观察了它们对６０Ｃｏ辐射小鼠的放射治疗作用，结果发现二氢卟吩ｅ６单甲酯铜络合物（７）能显著延长实验小鼠的存活时间，增加２１ｄ后小鼠存活数量。     

叶绿素降解产物金属络合物的合成及其对60Co辐射小鼠的放射保护作用

通过蚕沙叶绿素的降解反应,研究了焦脱镁叶绿酸a、二氢卟吩e₆单甲酯及紫红素18等二氢卟吩衍生物的制备方法,首次设计合成了蚕沙叶绿素降解产物的钴、铜、锌金属络合物。在确认结构的基础上观察了它们对60Co辐射小鼠的放射治疗作用,结果发现二氢卟吩e₆单甲酯铜络合物(7)能显著延长实验小鼠的存活时间,增加21d后小鼠存活数量。     

二氢卟吩f的合成新法

首次报道了由蚕沙糊状叶绿素经酸、碱降解制得的紫红素—18于25％KOH—EtOH中煮沸回流后脱羧，定向合成二氢卟吩f的新方法。收率60．4％。     

叶绿素a降解产物紫红素—18的光动力效应

对叶绿素a降解产物紫红素－18（1）在非细胞体系中的光敏化力和对小鼠肉瘤－180的光动力治疗作用进行了研究。结果表明,1在D2O中对NADPH的光氧化作用的敏化效应明显高于参比药物血卟啉衍生物（HpD);其4mg/kg时肿瘤抑制率可达95．1％,疗效较HpD显著（P＜0．01）。     

松针叶绿素-胡萝卜素膏对HP定植的胃溃疡大鼠的作用

目的研究松针叶绿素-胡萝卜素膏对HP定植的乙醇烧灼型胃溃疡大鼠的作用。方法采用幽门螺杆菌多次重复感染乙醇烧灼型胃溃疡大鼠,造成HP感染相关的胃溃疡模型,然后再给药。取血清和胃组织等样本,检测不同处理组溃疡指数及血清和胃组织中的超氧化物歧化酶(SOD)、丙二醛(MDA)、前列腺素E2(PGE2)以及胃泌素(GAS)等指标的含量,观察松针叶绿素-胡萝卜素膏的抗胃溃疡作用。结果松针叶绿素-胡萝卜素膏能有效抑制此种胃溃疡模型,可能机制是增强SOD、PGE2的活性,同时抑制MDA、GAS的活性。结论松针叶绿素-胡萝卜素膏对HP定植的乙醇烧灼型胃溃疡具有治疗作用。     

消化性溃疡患者血清LPO含量及SOD活性变化的初步研究

对８４例消化性溃疡患者血清ＬＰＯ含量及Ｃｕ，Ｚｎ－ＳＯＤ活性进行了测定，发现胃溃疡及复合性溃疡患者血清ＬＰＯ含明明显高于正常对照（Ｐ〈０．００１），血清Ｃｕ，Ｚｎ－ＳＯＤ活性则显低于正常对照（Ｐ〈０．０１）；十二指肠球部溃疡患者血清ＬＰＯ含量有升高趋势，而血清Ｃｕ，Ｚｎ－ＳＯＤ活性在正常范围，结果提示，胃溃疡的发生可能与氧自由基的作用有关。     

中华胃康·对实验性胃溃疡及HP抑制作用的研究

应用大、小鼠胃溃疡实验性胃溃疡模型,研究中华胃康的抗溃疡作用。结果证明,中华胃康5～20mg·kg－1,明显抑制大鼠应激性、幽门结扎型、利血平型、消炎痛型和小鼠组织胺型胃溃疡,并伴有胃液量、胃酸、胃蛋白酶活性降低,Alcian－blue测胃粘液合成增加;并可促进乙酸型溃疡愈合;效应与剂量相关。对幽门螺旋菌（HP）具有强烈抑制作用,MIC为0．024～0．048mg·kg－1。     

二氢卟吩p6-13,15-环酰亚胺类光敏剂的设计合成

目的 设计合成比紫红素-18（2）化学性质更稳定的二氢卟吩p6-13,15-环酰亚胺类光敏剂（1）。方法 以蚕沙叶绿素a粗提物（糊状叶绿素）酸水解产物脱镁叶绿酸a（3）的五元β-酮基羧酸酯环经碱性条件下空气氧化降解制得的紫红素-18（2）为原料,用各种胺包括羧基保护的氨基酸与其酸酐环发生缩合反应制得目标化合物。结果 以32.6%~65.2%的收率成功合成了目标化合物1a~1j,其结构经电喷雾质谱（ESI-MS）、氢谱（¹H NMR）、紫外谱（UV）和元素分析确证。结论 紫红素-18（2）和胺反应可以制得目标化合物1。该合成路线具有原料廉价易得、反应条件温和、操作简便等优点。     

糖性白内障大鼠晶体中SOD与血糖相关的实验观察

本文用半乳糖诱发大鼠白内障，观察正常组、10天组、20天组血糖及晶体中铜锌超氧化物歧化酶（CuZnSOD）、锰超氧化物歧酶（Mn－SOD）的活性，以探讨SOD与糖性白内障形成的关系。材料和方法一、白内障模型建立：取同一天出生大鼠27只，雌雄不限，体重18～22g。随机分成正常组、1     

Synthesis and Biological Evaluation of 3, 8‐dimethyl‐5‐isopropylazulene Derivatives as Anti‐gastric Ulcer Agent

Recent studies showed that Guaiazulene (GA) and Sodium guaiazulene sulfonate (GAS‐Na) have good anti‐gastric ulcer effect. Here, two series of GA derivatives were synthesized and evaluated for their anti‐gastric ulcer activity. The data obtained from in vivo testing of these compounds in a rodent ethanol‐induced stomach injury model are discussed. Among the tested compounds, A1 , A4 , and A9 (ulcer index: 1.125 ± 1.246**, 1.714 ± 0.756*, 1.875 ± 1.126*) exhibited better anti‐gastric ulcer activity than the positive control Omeprazole (2.005 ± 1.011*). The information got from these studies and the results of 3D‐SAR investigation may be useful in the design of novel anti‐gastric ulcer agents.     

Evalution of anti-ulcer activity of Polyalthia longifolia (Sonn.) Thwaites in experimental animals

Objective:

To evaluate the anti-ulcer activity of ethanol extract of leaves of Polyalthia longifolia (Sonn.) Thwaites.

Materials and Methods:

The ethanol extract of Polyalthia longifolia was investigated for its anti-ulcer activity against aspirin plus pylorous ligation induced gastric ulcer in rats, HCl -Ethanol induced ulcer in mice and water immersion stress induced ulcer in rats at 300 mg/kg body weight.p.o.

Results:

A significant (P < 0.01, P < 0.001) anti ulcer activity was observed in all the models. Pylorous ligation showed significant (P< 0.01) reduction in gastric volume, free acidity and ulcer index as compared to control. It also showed 89.71% ulcer inhibition in HCl- Ethanol induced ulcer and 95.3% ulcer protection index in stress induced ulcer.

Conclusion:

This present study indicates that P. longifolia leaves extract have potential anti ulcer activity in the three models tested.     

胃散对胃溃疡模型大鼠胃黏膜保护作用的研究

目的 研究胃散对胃溃疡大鼠胃黏膜的保护作用。方法 采用乙酸烧灼型胃溃疡模型、幽门结扎型胃溃疡模型、乙醇损伤型胃溃疡模型,检测溃疡指数、胃酸总酸度、胃酸分泌速度和胃蛋白酶活性,综合考察胃散对胃溃疡模型大鼠胃黏膜的保护作用。结果 胃散在1、0.5、0.25 g/kg剂量下,对乙酸烧灼型胃溃疡有非常显著的促愈合作用;对幽门结扎型胃溃疡的形成有显著的抑制作用;对乙醇损伤的胃黏膜也有显著的保护作用;对胃液总酸度、胃酸分泌速度和胃蛋白酶活性有明显抑制作用,显著增加胃液分泌量。结论 胃散具有增加胃液分泌、抑制胃酸分泌、抑制胃蛋白酶活性、保护胃黏膜和防止胃溃疡的作用。     

锌二氢卟吩e4的合成及初步抗胃溃疡活性和对急性肝损伤的保护作用

目的　研究锌二氢卟吩e₄(1)的合成及实验性抗溃疡活性和对急性肝损伤的保护作用。方法　蚕沙叶绿素粗品经酸碱降解反应制得二氢卟吩e₆(3),3经吡啶回流降解制得二氢卟吩e₄(2),2与醋酸锌络合制得1;并测定1对消炎痛诱发的大鼠胃溃疡的保护作用及对硫代乙酰胺、四氯化碳所致小鼠急性肝损伤的防治作用。结果　1为新化合物。生物活性实验结果表明,1能显著降低消炎痛诱发的大鼠胃溃疡指数和溃疡个数;能显著降低小鼠硫代乙酰胺或四氯化碳急性肝损伤后升高的SGPT活性。结论　1对消炎痛诱发的大鼠胃溃疡和硫代乙酰胺、四氯化碳所致小鼠急性肝损伤具有显著的保护作用。     

Effect of SR 58611A,a beta-3 receptor agonist,against experimental gastro-duodenal ulcers

The present study was designed to study the effect of SR 58611A, a selective beta 3-adrenoceptor agonist against gastric ulcers: pylorus ligation, water immersion plus restraint stress (WIRS), ethanol, aspirin-induced and on cysteamine-induced duodenal ulcers, in rats. SR 58611A (10 mg/kg, p.o.) was found to be effective in attenuating gastric ulceration and the results were comparable with those from standard cimetidine-treated group. Apart from reducing ulcer index, SR 58611A significantly decreased total acidity and thereby exhibited antisecretory activity in pylorus ligation model. SR 58611A showed significant reduction in ulcer index alongwith significant rise in the gastric wall mucus content in WIRS model. Further it showed significant cytoprotective activity against ethanol insult, that was evident from significant reduction in ulcer index. It showed significant reduction in gastric ulceration in aspirin-treated rats. The drug was found to be ineffective in inhibiting the cysteamine-induced duodenal ulcers as evident from the ulcer index and total lesion area parameters. It is concluded that SR 586111A possesses significant gastroprotective activity. This activity could be attributed to the inhibition of gastric acidity, increase in gastric wall mucus content and the reversal of gastric microvascular injury resulting into protection of the vascular integrity.     

C‐phycocyanin protects against ethanol‐induced gastric ulcers in rats: Role of HMGB1/NLRP3/NF‐κB pathway

Gastric ulcer is a widespread inflammatory disease with high socio‐economic burden. C‐phycocyanin is one of the active constituents of Spirulina microalgae, and although it is well known for its antioxidant and anti‐inflammatory properties, its protective effects against gastric ulcer have not yet been identified. High‐mobility group box 1 (HMGB1) is a nuclear protein that, once secreted extracellularly, initiates several inflammatory reactions, and it is involved in the pathogenesis of gastric ulcer. The aim of the present study was to investigate the anti‐inflammatory and anti‐ulcerogenic effects of C‐phycocyanin against ethanol‐induced gastric ulcer targeting HMGB1/NLRP3/NF‐κB pathway. Ulcer induction showed increase in HMGB1 expression through activation of nucleotide‐binding domain and leucine‐rich repeat‐containing protein 3 (NLRP3) inflammasome and nuclear factor kappa p65 (NF‐κB p65). Moreover, oxidative stress and inflammatory markers were elevated in the ulcer‐treated group compared to the normal control group. However, pre‐treatment with C‐phycocyanin significantly reduced HMGB1 expression via suppression of NLRP3/NF‐κB, oxidative markers, IL‐1β, tumour necrosis factor‐α (TNF‐α) and ulcer index value. These results were consistent with histopathological and immunohistochemistry examination. Thus, C‐phycocyanin is a potential therapeutic strategy with anti‐inflammatory and anti‐ulcerogenic effects against ethanol‐induced gastric ulcer.     

三油酸甘油酯抗胃粘膜损伤及作用机制

考察了三油酸甘油酯对无水乙醇所致大鼠胃粘膜损伤的保护作用及其对抗aspirin、reser pine所致小鼠胃溃疡的作用 .并进一步探讨了三油酸甘油酯抗溃疡作用的机制 .实验结果表明 ,三油酸甘油酯可降低上述各模型中大鼠及小鼠的溃疡指数 ,其作用是以增强胃的防御因子为主 .主要机制研究表明 ,三油酸甘油酯是通过促进胃内前列腺素E2 (PGE2 )和粘液的合成及分泌而起到保护胃粘膜的作用     

Evaluation of anti-ulcer activity of Samanea saman (Jacq) merr bark on ethanol and stress induced gastric lesions in albino rats

Objective:

To evaluate the antiulcer activity of Samanea saman (Jacq) Merr bark on ethanol and stress induced gastric lesions in albino rats.

Materials and Methods:

Gastric lesions were induced in rats by oral administration of absolute ethanol (5 ml/kg) and stress induced by water immersion. The antiulcer activity of methanolic extract of Samanea saman (Jacq) Merr bark (100 mg/kg, 200 mg/kg, 400 mg/kg) was compared with standard drugs. The parameters studied were ulcer index, gastric juice volume, pH, free acidity and total acidity.

Result:

Samanea saman (Jacq) Merr showed a dose dependent curative ratio compared to ulcer control groups. The extract at 400 mg/kg showed significant anti ulcer activity which is almost equal to that of the standard drug in both models. The volume of acid secretion, total and free acidity was decreased and pH of the gastric juice was increased compared to ulcer control group.

Conclusions:

The present study indicates that Samanea saman (Jacq) Merr bark extracts have potential anti ulcer activity.     

呋喃唑酮与枳实、白芨合用对大鼠胃溃疡的影响

预先大鼠2次/日灌胃连续给药一周之后采用幽门结扎法造成大鼠胃溃疡模型,收集胃液量并测定胃酸,查找溃疡点数,结果表明:呋喃唑酮组(20mg/200g),呋喃唑酮与枳实、白芨剂组(45mg/200g)抗溃疡效果明显优于甲氰咪胍组(40mg/200g)。说明呋喃唑酮及合剂具有较强的抗溃疡作用。     

Effects of the anti-ulcer agents on the amine contents and regulating enzyme activity of gastric mucosa during the healing process of acetic acid induced gastric ulcer in rats

In order to elucidate the action of an H2 blocker (cimetidine) and gastric mucosal protection agents (sucralfate and sofalcone) on the relapse and recurrence of gastric ulcer, the effects of cimetidine, sucralfate and sofalcone on the contents of histamine and serotonin and histidine decarboxylase (HDC) activity in the gastric mucosa were examined in the ulcer region and the intact region at the 10th day after the operation to produce acetic acid-induced gastric ulcer in rats. The following results were obtained: 1) HDC activity in the gastric mucosa of rats treated with cimetidine (100 mg/kg twice daily) tended to increase in the intact region, and it was significantly increased in the ulcer region. 2) Increased HDC activity due to cimetidine treatment was observed at the 10th day after interruption of cimetidine administration. 3) The HDC activity in the gastric mucosa was not changed by the treatment with sucralfate (500 mg/kg/day) and sofalcone (200 mg/kg/day). The results suggest that the increased HDC activity in the gastric mucosa might participate in the relapse and recurrence of gastric ulcer after discontinuation of cimetidine administration.