1.The basic and applied basic researches are the foundation of research and development of new drugs
Journal of Peking University(Health Sciences) 2001;33(3):193-198
From the soon-to-be-completed Human Genome Project to Combinatorial Chemistry and High-Throughput Screening combined with bioinformatic tools, scie n tific advances are poised to revolutionize drug discovery and even health care. The research directions in the State Key Laboratory of Natural and Biomimetic Dr ugs of Peking University mainly focus on the study of interaction between biolog ical targets and active compounds with structural diversity including endogeno us and exogenous substances, especially the natural products that come from anim als, plants and inorganic medicines. The new lead compounds have been designed and s ynthesized based on the structure-activity relationship and computer modeling. T he research activities are involved in 76 national research projects. From 1996 -20 00, 310 papers have been published, 8 patents obtained an d 14 prizes of scientific achievements awarded by the Chinese government and min istries.
2.CHEMICAL CONSTITUENTS FROM CHINESE ANTHO-PLEURA XANTHOGRAMMICA BERKLY(II)
Hongzheng FU ; Lihe ZHANG ; Wenhan LIN
Chinese Journal of Marine Drugs 1994;0(03):-
From ethyl acetate fraction of Chinese Anthopleura xanthogrammica B, collected from Qingdao beach, three new glycerolipids named 1-O-hexadecanoyl-2-O (9-oc-tadecenoyl )-3-O-( 9, 12-octadecadienoyl ) glycerol (3)'1-O-hexadecahoyl-3-O-(14-eiosyle-cenoyl)glycerol (4)and l-O-(9,12-octadecadienoyl)-2-O-(9,12-octadecadienoyl)glycerol (5) as well as two lipidic acids named 9,12-octadecadienoic acidd) and 9,14-docosandienoic acid (2) were isolated. Their structures were identified by various spectrial(IR,PNMR ,CNMR, MS,et al)analysis and chemical conversion.
3.Nucleosides from Anthopleura stell
Rupeng ZHUO ; Hongzheng FU ; Lihe ZHANG ; Wenhan LIN
Chinese Traditional and Herbal Drugs 2001;32(4):289-291
To study the chemical constituents of sea anemone, Anthopleura stell Verrill.Methods The chemical constituents were isolated and purified by chromatographic methods and their structures elucidated by chemical evidences and spectra data.Results 5 nucleosides were obtained and identified from the ethanolic extract as 2-hydroxy purine (Ⅰ); deoxyinosine (Ⅱ); 1-methylxanthosine (Ⅲ); deoxyguanosine (Ⅳ), and deoxyribo-thymidine (Ⅴ).Conclusion Compound Ⅲ was a new natural product, while the others were found from sea anemone for the first time.
4.Study on the relationship between body mass index and dose area product as well as fluoroscopy time in Han nationality during coronary angiography
Hailing DING ; Kai ZHANG ; Lihe DAI ; Minjie WANG
Journal of Interventional Radiology 2015;(9):763-766
Objective To investigate the relationship between body mass index (BMI) and dose area product (DAP) as well as fluoroscopy time during coronary angiography (CAG) in Han nationality subjects in order to improve early judging and reducing high radiation risk. Methods CAG materials of 451 Han nationality subjects were retrospectively analyzed. The patients included 276 males (age 32-87 years) and 175 females (age 42-84 years), and the BMI values ranged from 17.30 to 35.42 kg/m2. According to BMI values, the patients were divided into group A(BMI<20 kg/m2,n=25), group B (BMI 20-24.9 kg/m2,n=204), group C (BMI 25-29.9 kg/m2,n=192) and group D (BMI>30 kg/m2,n=30). The mean DAP and fluoroscopy time of each group were calculated; the DAP values were compared between each other among the four groups by using nonparametric Kruskal-Wallis test, while the fluoroscopy time was compared between each other among the four groups by using single factor analysis of variance or LSD-t test. Results The mean DAP of group A, B, C and D was(1 070.07±541.33) μGym2,(1 326.82±606.91) μGym2,(1 937.99±1 030.31) μGym2 and (2 654.53±1 296.69) μGym2 respectively. The mean fluoroscopy time of group A, B, C and D was (3.53± 2.08) min, (2.70 ±1.80) min, (2.75 ±1.88) min and (2.71 ±1.69) min respectively. Statistically significant difference in DAP values existed between each other among the four groups (P<0.05) except between group A and group B (P=0.232). Statistically significant difference in fluoroscopy time existed between group A and other three groups (P<0.05), while the difference in fluoroscopy time between each other among B, C and D groups was not significant (P>0.05). Conclusion The DAP values of adult Han subjects receiving CAG are increased with the increase of BMI values; the fluoroscopy time is significantly prolonged in patients with BMI<20 kg/m2. In performing interventional procedure, the operator should not only understand that the increase of BMI can cause the increase of DAP, but also need to pay special attention to the increase of DAP value caused by operation difficulty when the patient’s BMI is <20 kg/m2.
5.Small incision thymectomy under single lumen endotracheal intubation of thoracoscope
Peifeng LIN ; Lihe CHEN ; Jianhai ZHANG ; Xianwu WENG ; Chengzhi LIANG
China Journal of Endoscopy 2016;22(3):57-59
Objective To investigate the difference between single lumen endotracheal intubation of thoracoscope and traditional double lumen endotracheal intubation of thoracoscope in process of thymectomy. Methods From January 2010 to June 2014, clinical data of 30 cases with thymectomy under single lumen endotracheal intubation of thoracoscope (group A) and 30 cases with thymectomy under traditional double lumen endotracheal intubation thora-coscope (group B) were analyzed. Results There were no death patients in both groups. Group A:endotracheal intu-bation time (2.67 ± 0.72) min, surgery time (48.37 ± 4.64) min, the bleeding (26.17 ± 9.62) ml; Group B:endotracheal intubation time (5.55 ± 0.71) min, surgery time (52.10 ± 5.68) min, the bleeding (33.00 ± 7.94) ml. Conclusion Compared with traditional double lumen endotracheal intubation under thoracoscope, the single lumen endotracheal intubation of thoracoscope showed that intubation time was significantly shorter, and reduced the oc-currence of postoperative complications, the operative field was exposed more completely, reduced operation time and blood loss.
6.The synthesis of purine derivatives and its inhibitory activity on CD38 NADase.
Na LI ; Wenjie ZHU ; Xiwen XUE ; Yongjuan ZHAO ; Honcheung LEE ; Liangren ZHANG ; Lihe ZHANG
Acta Pharmaceutica Sinica 2015;50(8):1013-20
CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
7.Ultrasonographic and pathologic features in fetal arthrogryposis multiplex congenita
Guohong LI ; Miao HE ; Yanfang PENG ; Lihe ZHANG ; Ting LEI ; Hongning XIE
Chinese Journal of Ultrasonography 2021;30(4):331-335
Objective:To summarize the prenatal sonographic characteristics of affected joints of fetal arthrogryposis multiplex congenita (AMC) by comparing the ultrasonographic features and the postnatal pathological manifestations.Methods:The cases of AMC detected by antenatal ultrasound and confirmed by postnatal pathology were collected in the First Affiliated Hospital of Sun Yat-Sen University and Kaiping Central Hospital from January 2015 to June 2020. The differences between prenatal ultrasonic manifestations, types of affected joints and postnatal pathological features were analyzed. And the different involvements of joints in AMC cases with or without other system abnormalities were also explored separately.Results:A total of 31 cases of AMC were included, in which 11 cases were with other system abnormalities and 20 cases without. No significant difference was observed in number of affected joints between these two groups ( P>0.05). The prenatal sonogram features were completely consistent with the postnatal pathological manifestations in 21 (21/31, 67.7%) cases. Among 31 cases, the involvement rates of joints were: interphalangeal joints of fingers (23/31, 74.2%), knee joints (20/31, 64.5%) and ankle joints (19/31, 61.3%), temporomandibular joint (11/31, 35.5%), wrists (11/31, 35.5%), elbow joints (10/31, 32.3%), interphalangeal joints of toes (6/31, 19.4%), spinal joints (2/31, 6.5%), shoulder joint (1/31, 3.2%) and hip joint (1/31, 3.2%), respectively. The coincidence rates of prenatal ultrasound in involved joints were: interphalangeal joints of fingers (100%), ankles (100%), spines (100%), hips (100%), wrists (90.9%), knees (75.0%), elbows (70.0%), jaws (54.5%), interphalangeal joints of toes (50.0%), and shoulders (0), respectively. Conclusions:When postural abnormalities of fetal upper and lower extremities are detected by prenatal ultrasound screening, especially overlapping fingers, extended knee and club foot, AMC should be kept on alert. Simultaneously, other joints should be carefully scanned to improve the prenatal detection rate of AMC.
8.Design and synthesis of photoaffinity biotin labelled 2'-O-propargyl-guanosine.
Luxin NA ; Xin LIU ; Zhuoming MENG ; Zhu GUAN ; Lihe ZHANG ; Zhenjun YANG
Acta Pharmaceutica Sinica 2015;50(1):59-63
Photoaffinity labeling is widely applied to demonstrate targets of small molecule ligands. In this paper, biotin photoaffinity labeled molecule with propargyl group 1 has been designed and synthesized, followed it's labeling of N2-acetyl-2'-O-propargyl guanosine 9 by "click chemistry". This technology presents delight development potential in labeling of second messenger cyclic nucleotide, antisense oligonucleotide or siRNA.
9.Effect of heat phlegm and nourishing Yin combined with glucocorticoids in the treatment of refractory Mycoplasma pneumoniae pneumonia in children
Chinese Journal of Primary Medicine and Pharmacy 2018;25(8):1030-1033
Objective To evaluate the clinical efficacy of phlegm and nourishing Yin combined with glucocorticoids in the treatment of refractory Mycoplasma pneumoniae pneumonia in children .Methods 134 children with Mycoplasma pneumonia were divided into control group and observation group according to the random number , 67 cases in each group .The control group were given hydrocortisone ,and the observation group received phlegm and nourishing Yin combined with glucocorticoid .After intervention ,the clinical data and the improvement of the clinical symptoms of the two groups were compared .Results There was no statistically significant difference in antipyretic time between the two groups(P>0.05).The time of cough relief,the absorption time of lung rales,the disappearance time of pleural effusion of the observation group were (3.61 ±1.13) d,(6.52 ±1.90) d and (7.02 ±2.10) d, respectively,which were significantly shorter than those of the control group [(4.89 ±2.18)d,t=2.920,P=0.021;(8.24 ±2.75)d,t=3.108,P=0.000;(9.26 ±2.38)d,t=5.027,P=0.000].There were no statistically signifi-cant differences in the total white blood cell count ,C-reactive protein and erythrocyte sedimentation rate between the two groups(all P>0.05).The percentage of lymphocytes in the observation group [(55.25 ±4.91)%] was signifi-cantly higher than that in the control group [(50.16 ±4.83)%,t=2.597,P=0.037].The effective treatment rate in the observation group was 97.01%,which was significantly higher than 83.58%in the control group (χ26.849,P=0.009).Conclusion Heat phlegm and nourishing Yin combined with glucocorticoid can not only effectively improve the patients'clinical symptoms , improve the proportion of lymphocyte , but also can improve the overall efficacy of children,it is worthy of clinical promotion .
10.Evaluation on allergic rhinitis treated by sphenopalatine ganglion stimulation with acupuncture:a systematic review
Lihe CHEN ; Lu ZHANG ; Wenhong MAO ; Jianwu SHEN ; Bo LI ; Zhixian XU ; Mengmeng GUO ; Kejian WANG ; Lijuan ZHANG ; Feng XU
International Journal of Traditional Chinese Medicine 2016;38(3):254-260
Objective The advantages of the treating allergic rhinitis (AR) by sphenopalatine ganglion stimulation with acupuncture were evaluated.Methods Databases including CBMDisk, CNKI, WanFang, VIP, Cochrane Library, PubMed, ProQuest, ChiCTR, ISRCTN, ClinicalTrials.gov and CENTRAL were searched from the beginning of database established to Jan 2015. All issues from Jan 2004 to Jan 2015 published onjournals Chinese Acupuncture & Moxibustion,Shanghai Journal of Acupuncture and Moxibustion, Acupuncture Research,Journal of Clinical Acupuncture and Moxibustion,Chinese Journal of Integrated Traditional and Western Medicine and Chinese Journal of Otorhinolaryngology in Integrative Medicine were searched by hand at meantime. All data were extracted based on the inclusive and exclusive criteria which was pre-designed, the Revman5.3 was applied for meta-analysis, and the studies qualities were analyzed by grade score.Results 118 articles were collected, 7 studies that involving 1 230 patients met the inclusive criteria. The result indicated that the sphenopalatine ganglion stimulation with acupuncture as the main treatment of AR showed the better total response rate compared to conventional drugs, theOR(95%CI) was 3.22(1.81 - 5.75); however the change of total symptom score had no statistical significant difference, the MD(95%CI) was 0.69 (-0.56 - 1.93), the change of IgE had no statistical significant difference,theSMD(95%CI) was -0.07 (-0.97 - 0.83).Conclusion The main treatment on AR by sphenopalatine ganglion stimulation with acupuncture may has better efficacy than western medicine. But due to the methodological biases existed in most studies, future high-quality RCTs were needed to be included into Meta-analysis to test today’s study conclusion.