1.Hypoglycemic activities of flowers of Xanthoceras sorbifolia and identification of anti-oxidant components by off-line UPLC-QTOF-MS/MS-free radical scavenging detection.
Xiajing XU ; Yongli GUO ; Menglin CHEN ; Ning LI ; Yi SUN ; Shumeng REN ; Jiao XIAO ; Dongmei WANG ; Xiaoqiu LIU ; Yingni PAN
Chinese Herbal Medicines 2024;16(1):151-161
OBJECTIVE:
To identify phytochemical constituents present in the extract of flowers of Xanthoceras sorbifolia and evaluate their anti-oxidant and anti-hyperglycemic capacities.
METHODS:
The AlCl3 colorimetric method and Prussian Blue assay were used to determine the contents of total flavonoids and total phenolic acids in extraction layers, and the bioactive layers was screened through anti - oxidative activity in vitro. The Waters ACQUITY UPLC system and a Waters ACQUITY UPLC BEH C18 column (2.0 mm × 150 mm, 5 μm) were used to identify the ingredients. And anti-oxidative ingredients were screened by off-line UPLC-QTOF-MS/MS-free radical scavenging. The ameliorative role of it was further evaluated in a high-fat, streptozotocin-induced type 2 diabetic rat model and the study was carried out on NADPH oxidase (PDB ID: 2CDU) by molecular docking.
RESULTS:
Combined with the results of activity screening in vitro, the anti - oxidative part was identified as the ethyl acetate layer. A total of 24 chemical constituents were identified by liquid chromatography-mass spectrometry in the ethyl acetate layer and 13 main anti-oxidative active constituents were preliminarily screened out through off-line UPLC-QTOF-MS/MS-free radical scavenging. In vivo experiments showed that flowers of X. sorbifolia could significantly reduce the blood glucose level of diabetic mice and alleviate liver cell damage. Based on the results of docking analysis related to the identified phytocompounds and oxidase which involved in type 2 diabetes, quercetin 3-O-rutinoside, kaempferol-3-O-rhamnoside, isorhamnetin-3-O-glucoside, and isoquercitrin showed a better inhibitory profile.
CONCLUSION
The ethyl acetate layer was rich in flavonoids and phenolic acids and had significant anti-oxidant activity, which could prevent hyperglycemia. This observed activity profile suggested X. sorbifolia flowers as a promising new source of tea to develop alternative natural anti-diabetic products with a high safety margin.
2.Novel benzothiazole derivatives target the Gac/Rsm two-component system as antibacterial synergists against Pseudomonas aeruginosa infections.
Jun LIU ; Wenfu WU ; Jiayi HU ; Siyu ZHAO ; Yiqun CHANG ; Qiuxian CHEN ; Yujie LI ; Jie TANG ; Zhenmeng ZHANG ; Xiao WU ; Shumeng JIAO ; Haichuan XIAO ; Qiang ZHANG ; Jiarui DU ; Jianfu ZHAO ; Kaihe YE ; Meiyan HUANG ; Jun XU ; Haibo ZHOU ; Junxia ZHENG ; Pinghua SUN
Acta Pharmaceutica Sinica B 2024;14(11):4934-4961
The management of antibiotic-resistant, bacterial biofilm infections in skin wounds poses an increasingly challenging clinical scenario. Pseudomonas aeruginosa infection is difficult to eradicate because of biofilm formation and antibiotic resistance. In this study, we identified a new benzothiazole derivative compound, SN12 (IC50 = 43.3 nmol/L), demonstrating remarkable biofilm inhibition at nanomolar concentrations in vitro. In further activity assays and mechanistic studies, we formulated an unconventional strategy for combating P. aeruginosa-derived infections by targeting the two-component (Gac/Rsm) system. Furthermore, SN12 slowed the development of ciprofloxacin and tobramycin resistance. By using murine skin wound infection models, we observed that SN12 significantly augmented the antibacterial effects of three widely used antibiotics-tobramycin (100-fold), vancomycin (200-fold), and ciprofloxacin (1000-fold)-compared with single-dose antibiotic treatments for P. aeruginosa infection in vivo. The findings of this study suggest the potential of SN12 as a promising antibacterial synergist, highlighting the effectiveness of targeting the two-component system in treating challenging bacterial biofilm infections in humans.
3.Application of LBW index combined with energy spectrum CT in reducing the contrast agent dose of liver enhanced CT
Xiaoqian JIA ; Yiming WANG ; Wei TONG ; Yuan QU ; Jiao CHEN ; Chunying HAN ; Qian TIAN ; Shumeng ZHU ; Jianxin GUO ; Miao LI
Journal of Xi'an Jiaotong University(Medical Sciences) 2021;42(6):880-884
【Objective】 To compare the enhancement effects of lean body weight (LBW) and total body weight (TBW) as indexes to calculate the contrast agent dosage under the condition of energy spectrum CT scanning. 【Methods】 A total of 218 patients who received liver enhancement CT from November 2018 to January 2019 were enrolled in this study. There were 101 patients in LBW group and 117 patients in TBW group. Both groups were scanned by energy spectrum CT, and the parameters of scanning and reconstruction were identical. The contrast agent dose was 500 mgI/kg (LBW) in LBW group and 450 mgI/kg (TBW) in TBW group, and the injection rate was 2.8 mL/s. Images were transferred to a GE AW4.7 workstation and the 50 keV monochromatic images were analyzed. We compared the dosage of contrast medium, CT value of aorta in arterial phase (HU-aorta), hepatic enhancement CT value in venous phase (-liver), the rate of reaching the enhancement standard and variability in the two groups. 【Results】 Compared with TBW group, LBW group had lower contrast agent dosage, HU-aorta and ∆-liver (P<0.05), LBW and TBW group had no statistically different enhanced rate of HU-aorta as (91.09% vs. 90.60%) or ∆-liver (92.08% vs. 88.89%) (P>0.05). The variation rate of HU-aorta and ∆-liver in LBW group was lower than that in TBW group. Using LBW as an index to calculate the dosage of liver enhanced CT also made the enhancement of liver parenchyma more consistent in different patients. 【Conclusion】 Even on the premise of energy spectrum CT scanning, using LBW-based contrast injection in liver enhanced CT can not only reduce contrast dose, but also make the enhancement in liver parenchyma more consistent among different patients.
4.The effects of 80 kVp combined with ASiR-V on image quality of iliac artery in preoperative evaluation of kidney transplantation
Xiaoqian JIA ; Wenting XU ; Wei TONG ; Jiao CHEN ; Shumeng ZHU ; Qian TIAN ; Xinyi NIU ; Xiangli ZHANG ; Jianxin GUO
Journal of Xi'an Jiaotong University(Medical Sciences) 2021;42(5):763-768
【Objective】 To investigate the effects of 80 kVp combined with multi-model adaptive statistical iterative reconstruction algorithm (ASiR-V) on the image quality of CT angiography (CTA) of iliac artery in kidney transplantation candidates before operation. 【Methods】 Totally 50 kidney transplantation candidates underwent “one-stop” scanning combined CTA for coronary and iliac arteries were recruited consecutively. After the scanning, images were reconstructed with different ASiR-V levels on the iliac artery from 50% to 100% at a 10% interval, and 6 groups of images were obtained. We evaluated and compared all image qualities, DLP and CTDI in the patients’ examination were recorded, and the effective dose (ED) was calculated. 【Results】 All of the image quality objective scores of different ASiR-V levels on the iliac artery were above 3 points (3.32±0.24), and the average CT value was (344.30±74.53)HU. The ED received by the patient throughout the examination was (2.71±0.42)mSv. The image noise decreased while SNR and CNR increased monotonically as the ASiR-V levels increased, among which 80% ASiR-V image quality score was the highest with 3.41±0.26. 【Conclusion】 For patients who need to have both coronary and iliac arteries evaluated before kidney transplantation operation, low tube voltage (80 kVp) combined with 80% ASiR-V can obtain high-quality iliac artery images under the premise of reducing the ED dose, which can provide practical basis for further reducing the dose in personalized scanning scheme for such patients. It has good feasibility and clinical application value.

Result Analysis
Print
Save
E-mail