1.Extraction of total-saponins from Patrinia Villosa Juss based on uniform design method
Jiexin XU ; Fangqin ZHOU ; Fangming JIANG ; Yanzhi LIAO
Chinese Traditional Patent Medicine 1992;0(04):-
AIM: To confirm the optimum extraction of the total-saponins from Patrinia Villosa Juss. METHODS: Optimum conditions(ethanol concentration,extraction hours,ethanol solution quantity) were determined by the uniform design test,the extract was refined with macropore resin AB-8,and samples were measured colorimetrically at ?=560 nm compared with oleanolic acid as reference substance. RESULTS: The result was 95% ethanol as solvent, extraction time for 1 h adding 8 times amount of ethanol solution at 100 ℃ water bath for two times.under this condition,the total-saponins content was 0.668%,in accordance with the design forecast. CONCLUSION: The optimum extraction technique and purified methods could extract the total-saponins efficiently from Patrinia Villosa Juss.The technique is simple and adapts for production.
2.Phototaxis effect of Oncomelania hupensis hupensis and O . h . robertsoni-- a comparative study
Zhenqiang GONG ; Chuanchang LI ; Bo TAO ; Yan WANG ; Xianmin ZHOU ; Jiexin ZOU
Chinese Journal of Zoonoses 2014;(8):833-839
The aim of this study was to determine the differences in phototaxis between Oncomelania hupensis (O .h .) hupensis and O .h .robertsoni as well as four related geographic strains of male and female snails and Schistosoma japonicum-infected and-uninfected snails .Field collection of O . hupensis was performed in S . j aponicum-endemic areas of Xingzi and Yushan counties in Jiangxi Province ,China ,as well as Tianquan and Pengshan counties in Sichuan Province ,China .Infected and uninfected snails were screened using the cercariae escaping method ,with artificial separation of male and female snails . The experiment was carried out in an in-house constructed dark phototaxis experiment box using white light as the main source of light at the most suitable light intensity .Under a light intensity of 1 500 Lux for 30 minutes ,all of the snails from the experimental group showed obvious phototaxis .The statistical analysis showed no significant difference in the phototaxis index between male and female snails ,and there was also no significant difference in the phototaxis index between different geograph-ical strains of the same subspecies of snails .A significant difference in phototaxis was observed between the two subspecies during the 30-minute experimental period :O .h .hupensis displayed a higher phototaxis index than that of O .h .robertsoni , whereas S .japonicum-infected snails showed a lower phototaxis index than that of uninfected snails .A difference in phototaxis was found between different subspecies of O .hupensis and within the same subspecies .All uninfected snails displayed the same phototaxis index .When snails were infected with S .japonicum ,phototaxis reduced .
3.Quantitative computed tomography analysis for stratifying the severity of Coronavirus Disease 2019
Cong SHEN ; Nan YU ; Shubo CAI ; Jie ZHOU ; Jiexin SHENG ; Kang LIU ; Heping ZHOU ; Youmin GUO ; Gang NIU
Journal of Pharmaceutical Analysis 2020;10(2):123-129
To examine the feasibility of using a computer tool for stratifying the severity of Coronavirus Disease 2019 (COVID-19) based on computed tomography (CT) images. We retrospectively examined 44 confirmed COVID-19 cases. All cases were evaluated separately by radiologists (visually) and through an in-house computer software. The degree of lesions was visually scored by the radiologist, as follows, for each of the 5 lung lobes:0, no lesion present;1,<1/3 involvement;2,>1/3 and<2/3 involvement;and 3,>2/3 involvement. Lesion density was assessed based on the proportion of ground-glass opacity (GGO), consolidation and fibrosis of the lesions. The parameters obtained using the computer tool included lung volume (mL), lesion volume (mL), lesion percentage (%), and mean lesion density (HU) of the whole lung, right lung, left lung, and each lobe. The scores obtained by the radiologists and quantitative results generated by the computer software were tested for correlation. A Chi-square test was used to test the consistency of radiologist- and computer-derived lesion percentage in the right/left lung, upper/lower lobe, and each of the 5 lobes. The results showed a strong to moderate correlation between lesion percentage scores obtained by radiologists and the computer software (r ranged from 0.7679 to 0.8373, P < 0.05), and a moderate correlation between the proportion of GGO and mean lesion density (r=-0.5894, P<0.05), and proportion of consolidation and mean lesion density (r=0.6282, P<0.05). Computer-aided quantification showed a statistical significant higher lesion percentage for lower lobes than that assessed by the radiologists (x2 = 8.160, P = 0.004). Our experiments demonstrated that the computer tool could reliably and accurately assess the severity and distribution of pneumonia on CT scans.
4.Classification of collateral blood compensation pathways in patients with common carotid artery occlusive disease
Yang LIU ; Jianan WANG ; Jiexin ZHOU ; Tuoyi WANG
Chinese Journal of Neuromedicine 2019;18(5):470-474
Objective To explore the classification of collateral blood compensation pathways and collateral blood compensation characteristics in patients with common carotid artery occlusive disease.Methods The hemodynamie and imaging data of 20 patients with common carotid artery occlusive disease,admitted to our hospital from May 2016 to September 2018,were collected.The patients were classified according to whether they had internal carotid artery stealing and collateral circulation compensating for collateral flow.Results Internal carotid artery hematoma was found in 11 of the 20 patients;there was collateral circulation in 17 patients,including 10 branches of the anterior communicating artery,9 branches of the posterior communicating artery,11 branches of the posterior cerebral artery-middle cerebral arterial pia anastomosis,and 8 branches of the ocular artery.There were three types of collateral blood compensation pathways to be discovered in the 20 patients with common carotid artery occlusive disease;type Ⅰ (n=3) was the collateral blood compensation pathway with simple internal carotid artery stealing,type Ⅱ (n=8) was the collateral blood compensation pathway with internal carotid artery stealing and collateral circulation,and type Ⅲ (n=9) was the collateral blood compensation pathways with simple collateral circulation.Conclusion In some patients with common carotid artery occlusion,the internal carotid artery stealing route exists in the collateral flow compensation.
5.A novel inhibitor of N 6-methyladenosine demethylase FTO induces mRNA methylation and shows anti-cancer activities.
Guoyou XIE ; Xu-Nian WU ; Yuyi LING ; Yalan RUI ; Deyan WU ; Jiawang ZHOU ; Jiexin LI ; Shuibin LIN ; Qin PENG ; Zigang LI ; Hongsheng WANG ; Hai-Bin LUO
Acta Pharmaceutica Sinica B 2022;12(2):853-866
N 6-methyladenosine (m6A) modification is critical for mRNA splicing, nuclear export, stability and translation. Fat mass and obesity-associated protein (FTO), the first identified m6A demethylase, is critical for cancer progression. Herein, we developed small-molecule inhibitors of FTO by virtual screening, structural optimization, and bioassay. As a result, two FTO inhibitors namely 18077 and 18097 were identified, which can selectively inhibit demethylase activity of FTO. Specifically, 18097 bound to the active site of FTO and then inhibited cell cycle process and migration of cancer cells. In addition, 18097 reprogrammed the epi-transcriptome of breast cancer cells, particularly for genes related to P53 pathway. 18097 increased the abundance of m6A modification of suppressor of cytokine signaling 1 (SOCS1) mRNA, which recruited IGF2BP1 to increase mRNA stability of SOCS1 and subsequently activated the P53 signaling pathway. Further, 18097 suppressed cellular lipogenesis via downregulation of peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT/enhancer-binding protein alpha (C/EBPα), and C/EBPβ. Animal studies confirmed that 18097 can significantly suppress in vivo growth and lung colonization of breast cancer cells. Collectively, we identified that FTO can work as a potential drug target and the small-molecule inhibitor 18097 can serve as a potential agent against breast cancer.