1.SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-[(SUBSTITUTED PHENYL)VINYL] INDOLE DERIVATIVES
Acta Pharmaceutica Sinica 2001;36(2):100-104
AIM To synthesize derivatives of 2-[substituted phenyl)vinyl] indole and find compounds with biological activities by screening in vitro. METHODS Twenty-one compounds of 2-[(substituted phenyl)vinyl] indole were synthesized by reduction, oxidation and Witting reaction. MS, 1HNMR and elemental analysis were used to determine the structures of the new compounds. RESULTS These compounds are new ones. CONCLUSION Six compounds (3,9,11,13,18 and 20) showed effects on some different receptors, such as alpha2, D2 and H1, and is worth further studying.
2.Research progress on role of Wnt signaling pathway in regulation of tumors
Chinese Pharmacological Bulletin 2017;33(1):14-17,18
Wnt signaling pathway is a highly conservative signal pathway controlling cell growth,differentiation,apoptosis and self-renewal.This signal pathway is often abnormally activated in tumor development and progression,which can cooperate or antagonize with other signal pathways to regulate tumor prolifera-tion,migration and invasion.This paper makes a review of the recent research of Wnt signaling pathway progression and its function in tumor growth regulation.
3.SYNTHESIS OF SUBSTITUTED 4-STYRYLCOUMARIN AND THEIR ANTITUMOR ACTIVITIES
Song XU ; Shiping XU ; Lanmin LI
Acta Pharmaceutica Sinica 2001;36(4):269-273
AIM A series of 4-styrylcoumarin derivatives had been designed and synthesized in order to find compounds of antitumor activities by screening. METHODS Title compounds (1-20) were synthesized by Phase-Transfer Wittig reaction or Wittig-Horner reaction, and screened by several antitumor models in vitro. Their structures were determined by 1HNMR, MS and elemental analysis. RESULTS Twenty compounds (1-20) are new compounds. Compound 18 had effects on KB cell lines in vitro. CONCLUSION It was seen that compound 18 had certain antitumor activities, and it was worth further studying.
4.SYNTHESIS AND ANTICANCER ACTIVITY OF 3-[(3′-METHYL-4′-(SUBSTITUTED PHENYL)-1′,3′-BUTADIENYL] INDOLE DERIVATIVES
Li XU ; Jie LIU ; Shiping XU
Acta Pharmaceutica Sinica 2001;36(1):29-33
AIM To study the synthesis and anticancer activity of 3-[(3′-methyl-4′-(substituted phenyl)-1′,3′-butadienyl] indole derivatives. METHODS Electrophilic-substitution, aldol-condensation, selective-reduction, phase-transfer Wittig reaction and hydrolysis reaction were used in the synthesis of the title compounds. RESULTS Eleven compounds of 3-[(3′-methyl-4′-(substituted phenyl)-1′,3′-butadienyl] indole were synthesized. They are new compounds. Compound 8 showed different inhibitory effects on HL-60, HCT-8 and Bel7402 cell lines in vitro, and its inhibitory rate of antiinflammation was 100% at 10-5 mol*L-1 concentration. CONCLUSION Compound 8 showed high anticancer and antiinflammatory activities, and is worth further studying.
5.Coexistence of phaeochromocytoma and renal cell carcinoma
Enci XU ; Shiping CHEN ; Zipu CHEN
Chinese Journal of Urology 2000;0(12):-
Objectives To evaluate the relationship between phaeochromocytoma and renal cell carcinoma,and to present 2 cases of coexisting phaeochromocytoma and renal cell carcinoma. Methods 2 cases of coexisting phaeochromocytoma and renal cell carcinoma diagnosed and treated were reviewed and studied. A case of left adrenal phaeochromocytoma was disdiagnosed as metastatic carcinoma from the left kidney.Nephrectomy and adrenalectomy were carried out without preoperative preparation crisis occurred in the operation and was managed in time.The another is a case of coexising right adrenal phaeochromocytoma and right renal cell carcinoma.After adequate preoperative preparation,the operation was carried out safely.The postoperative course of both the patients has been uneventful. Conclusions An adrenal growth on the same side of a renal cases may not be a metestatic carcinoma.The possibility of an coexisting phaeochromocytoma shuld be kept in mind.Surgical management was the only means for cure and preoperative preparation was extremely important.
6.APE/Ref-1 expression in gastric cancer
Shiping XU ; Haili HUANG ; Benyan WU
Medical Journal of Chinese People's Liberation Army 2001;0(10):-
Objective To study the expression of APE/Ref-1 in gastric cancer. Methods Detection of APE/Ref-1 protein was performed with gastric cancer tissue microarray (TMA) by IHC in gastric cancer, non-neoplastic mucosa and lymph node with metastasis. Results The positive rates of APE/Ref-1 in cytoblast in non-neoplastic mucosa, tumor tissue, and metastatic lymph nodes were 96.6%, 97.1% and 98.9%, respectively, while the positive rates in cytoplasm were 71.8%, 21.4% and 10.0%, respectively and in both cytoblast and cytoplasm were 71.4%, 21.4% and 10.0%, respectively. Compared to non-neoplastic mucosa, tumor lesion had lower APE/Ref-1 expression in cytoblast and cytoplasm. In 35.9% of patients it was decreased slightly and in 11.2% of them it was decreased markedly in cytoblast (P
7.The TCM handbook of AIDS diagnosis and treatment based on evidence-based medicine
Shiping XIE ; Yanping HU ; Qianlei XU
China Journal of Traditional Chinese Medicine and Pharmacy 2006;0(09):-
By employing the methods of literature research and specialist consultation,comprehensively and systematically collected case history at home and abroad on Chinese and western medicine in the treatment of AIDS,by distilling the etiopathogenisis and pathogenesis,the character,the clinical stage,TCM four methods of examination,di erentiation of symptoms,the therapeutical principle and method and the e ective prescription,etc,the paper clari ed the character,pathology,etiology and pathogenesis of AIDS by the evaluation and statistic of qualitative and quantitative analysis of evidence based medicine,grasped the present situation of the treatment of AIDS with Chinese and western medicine in the treatment of AIDS,the rule of syndrome di erentiation and the facticity and application of the clinical e cacy.All these are used to the TCM handbook of AIDS diagnosis and treatment.
8.Clinical characteristics of acute pancreatitis in elderly patients
Shiping XU ; Xing MA ; Benyan WU
Chinese Journal of Geriatrics 2001;0(01):-
Objective To study the clinical features of acute pancreatitis (AP) in elderly patients. Methods The elderly AP patients from January 1993 to October 1999 in our hospital were studied retrospectively. Results There are 83 cases with a male to female ratio of 1 5∶1 and a median age of 72 7 years.AP was diagnosed in 83 cases for 107 times which included 80 times of mild AP and 27 times of severe AP 13 patien with APts were diagnosed for more than one times.Abdominal pain was the primary symptom in 94 4% patients. 6 patients had no pain 53 0%(44/83) and 84 6%(11/13) patients had cholelithiasis and recurrent AP respectively.60 5% and 72 6% patients were diagnosed by type B ultrasonic and CT respectively . Conclusions In elderly AP patients,abdominal pain was the primary symptom, but a part of patients had no typical symptoms.Cholelithiasis including biliary sludge was an inducement especially in recurrent AP patients. Type B ultrasonic and CT examination were important means in diagnosis.
9.Risk factors for early cognitive dysfunction after cardiac valve surgery
Yuanyuan FU ; Meng HU ; Jinhui XU ; Wenjie SUN ; Shiping YIN
Journal of Medical Postgraduates 2017;30(5):515-520
Objective Postoperative cognitive dysfunction (POCD) is a common complication of cardiac surgery, which seriously affects the prognosis of the patient.This study aimed to explore the risk factors for early POCD in patients undergoing cardiac valve surgery and the correlation between early POCD and the serum S100B protein level.Methods Eighty patients underwent mitral valve replacement surgery in combination with tricuspid plasty.At 1 day before and 5 days after surgery, we assessed the cognitive function of the patients and divided them into a POCD and a non-POCD group.We obtained such data as the age, sex, education, New EuroSCORE Ⅱ, and preoperative NYHA cardiac function grades and left ventricle ejection fraction (LVEF) of the patients, collected the venous blood to determine serum S100B protein concentration by ELISA, and analyzed the independent risk factors of early POCD using single-factor and binary logistic regression analyses.Results POCD was found in 20 (25%) of the patients, , Logistic regression analysis showed the independent risk factors for early POCD to be hyperglycemia (OR=6.038, 95% CI: 1.202-30.337), operation time (OR=6.423, 95% CI: 1.276-32.332), and aspartate aminotransferase (AST, 2 times higher than normal) (OR=12.878, 95% CI: 2.289-72.445).The serum S100B protein concentrations in the POCD group were (1.9±0.3) μg/L and (1.7±0.4) μg/L at 48 and 72 hours after cardiopulmonary bypass, significantly lower than (2.4±0.4) μg/L and (2.1±0.3) μg/L at 30 minutes and 24 hours (P<0.05), and so was it in the non-POCD group at 72 than at 48 hours postoperatively ([1.4±0.4]) vs [1.5±0.4] μg/L, P<0.05).Conclusion Long operation time, perioperative hyperglycemia and high AST are independent predictors and the serum S100B protein level is a significant marker of early POCD.
10.Effect of Ershen Zeshu Mixture on the peritoneal lymphatic stomata and the ascites drainage
Shiping DING ; Jicheng LI ; Liangen MAO ; Jian XU ; Jiandon LIU
Chinese Journal of Pathophysiology 2000;0(11):-
AIM: To further study the effect of Ershen Zeshu Mixture, a Chinese medicine, on the peritoneal lymphatic stomata and the ascites drainage in experimental mice model of CCl 4-induced fibrosis.By the application of NO supplier (sodium nitroprusside,SNP) and NO suppressor (N G-mononethyl-L-arginine,L-NMMA),the effect of NO on the peritoneal lymphatic stomata and the ascites drainage was studied to clarify the relationship between Ershen Zeshu Mixture and NO in the regulation of the peritoneal lymphatic stomata.METHODS: The mouse model of fibrosis was established with the application of intragastric installations of carbon tetrachloride one time every three days;Scanning electron microscope and computer image processing were used to detect the girth,area and distribution density of the peritoneal lymphatic stomata;the concentration of urinary ions was measured in the experiment.RESULTS: ①Compared to NS group and model group,Ershen Zeshu Mixture could significantly increase the girth and the area of the peritoneal lymphatic stomata,promote its distribution density ( P