克拉霉素漂浮-生物粘附微囊的制备及性能研究

选用乳化-溶剂挥发法制备乙基纤维素载药微球(EMs), 并通过内部凝胶化法进行包衣制得海藻酸钠-乙基纤维素载药微囊(AEMs), 最后通过离子交联法进一步包衣制得壳聚糖-海藻酸钠-乙基纤维素载药微囊(CAEMs). 研究克拉霉素漂浮\|生物粘附微囊的制备工艺, 并考察微囊的体外漂浮性能、 粘附性能及体内滞留性能. 结果表明, CAEMs球形度较好, 药物包封率为72.3%~78.2%, 载药量为7.1%~12.7%. 在pH=5的醋酸缓冲液中, 6 h时的累积释放率为56.6%~70.6%, 漂浮率大于70%, 4 h时的体内滞留率为60.5%. CAEMs有望通过延长药物胃内滞留时间, 在临床用于根除幽门螺旋杆菌, 从而降低消化道溃疡的复发率.     

Glucuronide conjugates of Soraprazan (BY359), a new potassium-competitive acid blocker (P-CAB) for the treatment of acid-related diseases

Glucuronide conjugates of Soraprazan (BY359), a potent novel anti-secretory drug (currently in Phase II clinical trials), were not directly accessible synthetically. This was due to the relative instability of Soraprazan under the harsh Lewis acid conditions employed in popular glucuronidation methodologies and a lack of reactivity under alternative, Koenigs-Knorr, coupling conditions. We have now devised a successful synthesis using the novel N-acetylated Soraprazan to access the required glucuronide metabolites on gram scale. Coupling of this novel aglycone with methyl 1-O-trichloroacetimidoyl-2,3,5-tri-O-isobutyryl-α-d-glucopyran-uronate in the presence of trimethylsilyl trifluoromethanesulfonate (TMSOTf) gave the protected glucuronide intermediates. A one-pot two-step deprotection involving hydrolysis of the ester functionalities and removal of the N-acetyl group with alkaline hydrazine delivered the title compounds in satisfactory yield.     

Novel CD-MOF NIR-II fluorophores for gastric ulcer imaging

Gastric ulcers are one of the most common stomach diseases that often accompanied by inflammation, congestion, edema, scar tissue formation, and pyloric obstruction. Fiberoptic endoscopy and X-ray analysis of the upper GI tract have become the diagnostic procedure of choice for patients. However, conventional diagnosis technology is either invasive or radioactive. Herein, a novel CD-MOF NIR-II fluorophore (GPs-CH1055) was developed. The relative fluorophore intensity was largely consistent at various media and pH buffers, and it can swell into gel particles in solvents and be completely expelled from the gastrointestinal tract without being assimilated. GPs-CH1055 has been further evaluated in vivo, and exhibited strong retention effect on the gastric ulcer sites, bright NIR-II signals with high spatial and temporal resolution. Therefore, GPs-CH1055 shows great promise for realizing real-time gastric ulcer imaging and diagnosis.     

Decorated CuO nanoparticles over chitosan-functionalized magnetic nanoparticles: Investigation of its anti-colon carcinoma and anti-gastric cancer effects

In this study, a green protocol for supporting CuO nanoparticles over chitosan-modified amino-magnetic nanoparticles is described. The physicochemical and morphological properties of the desired nanocomposite assessed by various techniques like ICP, FT-IR, FE-SEM, EDX, TEM, XRD and VSM. In the oncological part of the recent study, the Cu(NO₃)₂, Fe₃O₄, and Fe₃O₄-NH₂@CS/CuO nanocomposite cell viability was very low against human gastric cancer cell lines i.e. MKN45, AGS, and KATO III and human colorectal carcinoma cell lines i.e. HT-29, HCT 116, HCT-8 [HRT-18], and Ramos.2G6.4C10. The IC50 of Fe₃O₄-NH₂@CS/CuO nanocomposite against MKN45, AGS, KATO III, HT-29, HCT 116, HCT-8 [HRT-18], and Ramos.2G6.4C10 cell lines were 517, 525, 544, 282, 214, 420, and 477 µg/mL, respectively. Thereby, the best anti-gastro-duodenal cancers findings of our Fe₃O₄-NH₂@CS/CuO nanocomposite was seen in the HCT 116 cell line case.     

酪酸梭菌抗阿司匹林致小鼠胃溃 疡作用的初步研究

目的 观测酪酸梭菌是否对阿司匹林导致的胃溃疡具有预防效应,并对其机制进行初步探讨。方法 取30只健康 雄性ICR 小鼠,随机分成3 组,每组各10 只,即模型组、酪酸梭菌组、奥美拉唑组。酪酸梭菌组以6×108cfu/ 只的菌量,模型组和奥美拉唑组均予以相同体积的无菌培养基,灌胃4d 后再饥饿处理48h,然后以250mg/kg 剂量的阿司匹林灌胃造模,奥美拉唑组小鼠于造模前30min,腹腔注射奥美拉唑（13mg/kg）。造模4h 后,取胃组织分别测定SOD、CAT 活力、MDA 含量;进行常规HE 染色观察胃黏膜组织结构变化,PAS染色判断黏液量的变化,免疫组化法测定Bcl-2、Bax 表达水平。结果 模型组的SOD、CAT 活性明显降低,MDA 含量显著增加,而酪酸梭菌预处理后逆转了该趋势（P＜0.01）,与奥美拉唑组比较无统计学差异。HE染色观察,酪酸梭菌能减轻胃黏膜的病理损伤,与奥美拉唑组无统计学差异。PAS 结果提示酪酸梭菌能够增加黏液量。酪酸梭菌组的Bcl-2 表达较模型组显著增多,同时Bax 表达显著减少。结论 酪酸梭菌预处理通过抗氧化应激、增加胃黏液量、上调Bcl-2/Bax 表达比例,减轻阿司匹 林造成的胃溃疡损伤。     

胃粘膜组织共焦显微拉曼光谱分类研究

采用基于小波变换的光谱去噪和背景扣除预处理技术,对32例(其中:13例正常,19例癌变)胃粘膜组织拉曼光谱进行分析,克服了手动背景扣除的一些缺点,并观察到一些新的光谱特征。基于此,给出能对所有正常组织和癌变组织进行有效分类的特征量和判据。通过研究这些特征量与胃粘膜组织癌变发展阶段之间的定量关系,可望实现胃癌的早期诊断。     

胃癌危险因素病例对照研究

报告了在南昌市进行的一项胃癌危险因素的病例对照研究，共调查胃癌病人39例和对照134例，经单因素分析，发现主要危险因素为吸烟，饮烈性酒，进食快，食辛辣食物，腌菜，精神受刺激，好生闷气，胃溃疡史等，而进食规律。多吃水果则具保护作用，同时对病例和对照做了血清微量元素测定，表明胃癌患者血清中Mo、Se和Zn缺乏与胃癌的发生有关。     

Determination of bile acids and lysolecithin in artificial and natural gastric juice by HPLC for characterization of antacida

Work-up procedures and HPLC separation systems for determination of taurocholic, glycocholic, chenodeoxycholic, and cholic acids and lysolecithin in artificial and natural gastric juice are described. These compounds are used for testing the binding capacity of antacida to the individual analytes. Work-up is simple, no extraction or filtration being required. The optimized combinations of stationary and mobile phases allow selective and sensitive determination of the respective bile acids in gastric juice. For optimization, the capacity factors of two related bile acids were evaluated for numerous commercial stationary phases. The mechanism of retention is different for free and conjugated bile acids. Special aspects of routine analysis are discussed.     

Treatment activity of a mixed-ligand coordination polymer on gastric carcinoma

Reaction of 4,4′,4″-nitrilotribenzoic acid (H₃L), a C₃-symmetric ligand, with the divalent Co(II) salt Co(NO₃)₂·6H₂O in the present of the N-donor ligand 1,2-di(4-pyridyl)ethylene (DPE) affords a new mixed-ligand coordination polymer with the chemical formula of [Co₃(TNB)(DPE)₂]·2H₂O·DMF (1). In this study, CCK-8 assay was used to determine the effect of novel compound on proliferation of gastric cancer cells. The VEGF signaling pathway in gastric cancer cells was determined through employing real-time PCR after treatment of the above complex. Further, molecular docking simulation confirmed that the biological activity was coming from the carboxyl groups through the hydrogen bonding interactions with the receptor protein, the pyridine group only bonded with the Co ion for the formation of the Co complex.     

胃癌患者血清铜、锌水平与组织学分化程度及分期的关系探讨

为研究胃癌患者血清铜、锌水平与组织学分化程度及分期的关系,对经病理确诊的１１０例胃癌患者血清铜、锌水平进行了测定。结果表明,Ⅳ期患者血清铜高于不足Ⅳ期患者,Ｐ〈０．０５;分化不良型胃癌中Ⅳ期者血清铜高于不足Ⅳ期者,Ｐ〈０．０５;分化型胃癌中Ⅳ期者血清铜与不足Ⅳ期者无显著性差异,Ｐ〉０．０５;Ⅳ期患者中分化不良型胃癌血清铜高于分化型胃癌,Ｐ〈０．０５;血清锌水平在不同分化程度及不同病期间未见明显差异