1.Design and synthesis of novel antifungal compounds bearing quinoline and thiophene moieties
Lei PANG ; Jing ZHAO ; Tingjunhong NI ; Chengxu ZANG ; Zichao DING ; Dazhi ZHANG ; Yuanying JIANG
Journal of Pharmaceutical Practice 2017;35(1):17-21,86
Objective Based on the structure-activity relationships on the reported antifungal agents bearing quinoline or thiophene moieties ,novel compounds bearing both quinoline and thiophene were designed ,synthesized ,and evaluated for in vitro antifungal activity against Candida albicans .Methods With 5-cyanothiophene-2-carbaldehyde or 5-cyanothiophene-3-car-baldehyde as starting materials ,13 compounds were synthesized via reductive amination ,reduction of cyano group and amida-tion of quinoline-or isoquinoline-carboxylic acid .Their chemical structures were characterized by 1 H NMR and MS . In vitro antifungal screening against Candida albicans SC5314 was performed with the microbroth dilution method .Results All the compounds exhibited potent antifungal activities against Candida albicans .Among them ,compound 6k showed the highest an-tifungal activity with MIC80 value of 0 .5 μg/ml ,which is same potent as fluconazole .Conclusion The designed compounds bearing both quinoline and thiophene exhibited potent antifungal activities ,and deserve further research .
2.The predictive value of microvascular obstruction for adverse left ventricular remodeling after primary percutaneous coronary intervention in patients with acute ST-elevation myocardial infarction: a prospective study
Si CHEN ; Haixia DIAO ; Yiqing ZHAO ; Zichao JIANG ; Kang LIU ; Zeyu ZHANG ; Xin A ; Weiwei LING ; Geng QIAN
Chinese Journal of Internal Medicine 2023;62(12):1458-1464
Objectives:Microvascular obstruction (MVO) is a specific cardiac magnetic resonance (CMR) imaging feature in patients with acute myocardial infarction. The purpose of this study was to elucidate the predictive value of MVO in left ventricular adverse remodeling after primary percutaneous coronary intervention (PCI) in patients with acute ST-elevation myocardial infarction (STEMI).Methods:A total of 167 patients with STEMI undergoing primary PCI in the Chinese PLA General Hospital from 2016 to 2020 were enrolled in this prospective cohort study, the average age of study patients was 57±10 years old, with 151 males (90.4%) and 16 females (9.6%). The patients were divided into the MVO group ( n=81) and non-MVO group ( n=86) according to the presence or absence of MVO on CMR imaging, respectively. The primary endpoint of the study was the occurrence of left ventricular adverse remodeling, which was defined as an increase in left ventricular end diastolic volume (LVEDV) by >20% at 6 months after primary PCI compared with the baseline. Patients who completed follow-up were diagnosed as left ventricular adverse remodeling or no left ventricular adverse remodeling according to CMR. The baseline data, perioperative data, and related data of end points were compared between the MVO group and non-MVO group. Finally, the predictive value of MVO in left ventricular adverse remodeling was calculated by receiver operating characteristic curve analysis. Results:In the baseline data, preoperative thrombolysis in myocardial infarction (TIMI) flow ( χ2=13.74, P=0.003) and postoperative TIMI flow ( χ2=14.87, P=0.001) were both obviously decreased in the MVO group. After 6 months of follow-up, the incidence of left ventricular adverse remodeling in the MVO group was significantly higher than that in the non-MVO group [37.0%(27/73) vs. 18.9%(14/74), χ2=5.96, P=0.015]. The left ventricular end systolic volume at 6 months post infarction in the MVO group was significantly larger than that in the non-MVO group [(94±32) vs. (68±20) ml, t=-5.98, P<0.001], as well as the LVEDV [(169±38) vs. (143±29) ml, t=-4.74, P<0.001]. Receiver operating characteristic curve showed that the area under the curve of MVO size for predicting left ventricular adverse remodeling was 0.637. Conclusion:The risk of left ventricular adverse remodeling is significantly increased in patients with MVO after primary PCI for acute STEMI.
3.Circadian rhythm of cutaneous pruritus
Zichao JIANG ; Xiaoxue SANG ; Jianyun LU ; Lihua GAO
Journal of Central South University(Medical Sciences) 2024;49(2):190-196
One of the most common and significant symptoms for skin disorders is pruritus.Additionally,it serves as a significant catalyst for the exacerbation or reoccurrence of skin diseases.Pruritus seriously affects patients'physical and mental health,and even the quality of life.It brings a heavy burden to the patients,the families,even the whole society.The pathogenesis and regulation mechanisms for pruritus are complicated and have not yet been elucidated.Previous clinical studies have shown that itch worsens at night in scabies,chronic pruritus,atopic dermatitis,and psoriasis,suggesting that skin pruritus may change with circadian rhythm.Cortisol,melatonin,core temperature,cytokines,and prostaglandins are the main regulatory factors of the circadian rhythm of pruritus.Recent studies have shown that some CLOCK genes,such as BMAL1,CLOCK,PER,and CRY,play an important role in the regulation of the circadian rhythm of pruritus by regulating the Janus tyrosine kinase(JAK)-signal transducer and activator of transcription(STAT)and nuclear factor kappa-B(NF-κB)signaling pathways.However,the mechanisms for circadian clock genes in regulation of circadian rhythm of pruritus have not been fully elucidated.Further studies on the mechanism of circadian clock genes in the regulation of circadian rhythm of pruritus will lay a foundation for elucidating the regulatory mechanisms for pruritus,and also provide new ideas for the control of pruritus and the alleviation of skin diseases.
4.The Carabelli's traits on permanent maxillary molars in 803 Han Chinese college students
Zichao ZHOU ; Daorui WANG ; Qianxia ZHANG ; Yidan ZHANG ; Aiyun CHUAN ; Jianing LI ; Wenkai JIANG ; Shengchao WANG
STOMATOLOGY 2024;44(8):586-589
Objective To investigate the Carabelli's traits on permanent maxillary molars in Han Chinese college students.Methods Intraoral photos and plaster models from 803 Han Chinese college students were observed and the Carabelli's traits on permanent maxillary molars were categorized by the Arizona State University Dental Anthropology System.Chi-square tests were performed for the comparison of the differences between male and female,permanent maxillary first and second molars.Kendall's tau-b correlation analy-ses were performed for the correlation between bilateral antimeric molars.Results The frequencies of Carabelli's traits on permanent maxillary first and second molars were 37.61%and 3.99%respectively,46.73%and 6.30%in males,27.95%and 1.54%in females,which were statistically significant between permanent maxillary first and second molars(P<0.01),male and female(P<0.01).In the positive expression,the low-grade expression(ASUDAS 1-4)was predominant and accounted for 67.37%and 59.52%on the perma-nent maxillary first and second molars.The correlation between bilateral antimeric teeth were statistically significant on permanent max-illary first molars(tau-b=0.756,P<0.01)and second molars(tau-b=0.477,P<0.01).Conclusion The Carabelli's traits on perma-nent maxillary molars in Han Chinese college students mostly occur on permanent maxillary first molars with low-grade expression,and understanding this has great anthropological and clinical significance.