CHEMISTRY & BIODIVERSITY
·
2023
·Vol. 20
·期 6
·e202201145
·
IF 2.9
Huiying Bai,Zhen Cao,Sha Meng,Rui Ge,Shurong Ban,Yuanlin Zhang,Li Tang,Qing-Shan Li
Myeloid differentiation protein 2 (MD2), a key TLR4 adaptor protein for sensing LPS, plays an important role in inflammatory process and has been identified as a promising target for the treatment of a variety of inflammatory diseases. In our study, a series of benzoxazolone derivatives were synthesized, characterized and tested for anti-inflammatory activity in vitro . The compounds 3c , 3d and 3g demonstrated the greatest anti-inflammatory activity against IL-6 with IC 50 values of 10.14±0.08, 5.43±0.51 and 5.09±0.88 μM, respectively. Furthermore, the bis-ANS displacement assay revealed that these compounds competitively inhibited the binding between the probe bis-ANS and the MD2 protein. The most active compound 3g , revealed a directly bind with MD2 protein via Arg90 binding and a dissociation constant value of 1.52×10 −6 mol L −1 as determined by the biological layer interference (BLI) assay. Our finding suggested that compounds 3g could be a promising lead compound as MD2 inhibitor for further anti-inflammatory agent development.
研究领域:
药理学
·
药物化学
·
炎症研究
✓ 已验证
DOI
PubMed
高影响因子
Food Chemistry: Molecular Sciences
·
2023
·
IF 3.3
Nan Xiang,Xiaoxiao Chang,Liuwei Qin,Kun Li,Siyun Wang,Xinbo Guo
In the present study, three matured Japanese plum cultivars with different colored peel and flesh were selected to mine the key transcription factors regulating anthocyanin formation in tissues. Results showed that PsMYB10 was correlated with structural genes C4H , F3H , and ANS . PsMYB6 could positively regulate C4H (r = 0.732) and accumulated anthocyanin in Sanhua plum’s flesh. Sanhua plum has the highest phenolic and anthocyanin contents (10.24 gallic acid equivalent mg·g −1 dry weight (DW) and 68.95 μg·g −1 DW), resulting itself superior biological activity as 367.1±42.9 Trolox equivalent mg·g −1 DW in oxygen radical absorbance capacity value and 72.79±4.34 quercetin equivalent mg·g -1 DW in cellular antioxidant activity value. The present work provides new insights into the regulatory mechanism of tissue-specific anthocyanin biosynthesis, confirming the pivotal role of anthocyanins in the biological activity of plums, providing essential support for the development of horticultural products enriched with anthocyanins.
研究领域:
植物科学
·
分子生物学
·
园艺学
·
食品科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ENZYME AND MICROBIAL TECHNOLOGY
·
2021
·
IF 3.493
Xinqi Xu,Xiangzhen Deng,Juan Lin,Jie Yang
Arylsulfatase is useful in industrial agar processing by removing sulfate groups. A full-length arylsulfatase gene, designated ArySMA1, was obtained from marine bacteria Serratia sp. SM1. The ArySMA1 gene encoded a novel serine-type arylsulfatase and the enzymatic properties were characterized. The enzyme presented notable capacity of removing sulfate groups from natural algae substrates. Kinetic study suggested that the microscopic thermal inactivation rate of ArySMA1 in free form was smaller than that of the enzyme-substrate complex. The presence of substrate could unexpectedly accelerate ArySMA1 to deactivate at high temperature. Such phenomenon was opposite to many findings that substrate could stabilize enzymes against heat. Molecular dynamics simulation and ANS fluorescent assay indicated the substrate led the hydrophobic regions of the active site more flexible and the sulfate group of the substrate could retard the processivity of ArySMA1 catalysis. This study provides guidance for agar desulfation and down-stream processing industry.
研究领域:
酶学
·
海洋生物技术
·
工业生物技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
·
2022
·
IF 11.504
Kefan Ouyang,Hexiang Xie,Yufeng Wang,Meng Wai Woo,Qian Chen,Sixing Lai,Hua Xiong,Qiang Zhao
In this study, phosphoric acid was used to replace hydrochloric acid which is widely reported in the production of whey protein isolate fibrils (WPF). The pH, temperature, and protein concentration for the phosphoric acid-induced fibrillation were optimized (4% w/v, pH 2.5, 90 °C). Under this condition, the mean particle size and molecular weight decreased significantly while the ζ-potential increased slightly, it suggested that the fibrillation was accompanied by hydrolysis . WPF was already formed via intermolecular interactions at 6 h, which exhibited a semiflexible and unbranched filament of about 10 nm in diameter. A few single-filament flexible fibrils (about 5 nm in diameter) formed at 24 h. Thioflavin T analysis supported by Intrinsic fluorescence showed that the use of phosphoric acid accelerated the fibrillation. The ANS fluorescence and Second-derivative UV–vis spectra indicated the increase in surface hydrophobicity, peaking after 12 h of heating. Compared with the hydrochloric acid induced, WPF induced by phosphoric acid exhibited a shorter lag phase and maintained a more stable dispersion state with a nanoscale particle size. The great interfacial properties and proper aspect ratio (length/diameter) provided the contribution that WPF effectively absorbed at the oil-water interface. Moreover, the emulsion stability of the WPF improved with increasing salt concentration. The phosphoric acid-induced WPF had the best emulsion stability at pH 5.5 which was further enhanced by proper heating.
研究领域:
食品科学
·
蛋白质化学
·
胶体科学
·
乳液技术
✓ 已验证
DOI
高影响因子
JOURNAL OF BIOSCIENCE AND BIOENGINEERING
·
2020
·
IF 2.366
Wei-Ming Chai,Zi-Yi Yu,Mei-Zhen Lin,Qi-Ming Wei,Shuang Song
In this study, 5-methoxy-2-mercaptobenzimidazole (5-M-2-MB) was confirmed as an efficient tyrosinase inhibitor by methods of enzyme kinetic, fluorescence quenching , ANS-binding, thermodynamics, energy transfer, and molecular docking in combination. The results proved that 5-M-2-MB significantly inhibited the tyrosinase (IC 50 = 60 ± 2 nM) in a reversible and competitive way with the K i value of 80 ± 1 nM. It quenched the intrinsic fluorescence of tyrosinase through a static mechanism, and caused conformational change of the enzyme by increasing the hydrophobic region. Moreover, this compound could bind to tyrosinase and form 5-M-2-MB-tyrosinase complex by hydrogen bond and hydrophobic interaction. The interactions were generated between 5-M-2-MB and specific amino acid residues (Trp-358, Thr-308, Glu-356, and Asp-357) located on the A chain of tyrosinase. Therefore, this study would offer a theoretical foundation for developing the new tyrosinase inhibitor.
研究领域:
生物化学
·
药理学
·
酶学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2021
·
IF 3.512
Xuanyu Chen,Xiaomin Deng,Xingxing Han,Yinmei Liang,Zhiping Meng,Rui Liu,Wenqiang Su,Huaxu Zhu,Tingming Fu
Silybin is a flavonoid lignin compound consisting of two diastereomers with nearly equal molar ratios. It has been reported that silybin can effectively inhibit the aggregation of amyloid protein, but the difference between the two silybin diastereomers has been rarely studied. In this work, the inhibitory ability of silybin to hen egg-white lysozyme (HEWL) was demonstrated, and the difference of kinetic parameters of two diastereomers was analyzed. Fluorescence quenching titration was utilized to analyze the binding differences to native HEWL between the diastereomers, and transmission electron microscopy (TEM) was utilized to analyze the characteristics of the surface of various samples. The differences between hydrophobicity and the secondary structure among several HEWL samples were measured by the 8-anilino-1-naphthalene sulfonic (ANS) acid fluorescence probe, Raman spectra, and far-UV circular dichroism. Moreover, the differences in the binding energy of these two diastereomers with HEWL were analyzed by molecular docking. Also, we have investigated the effect of silybin diastereomers on HEWL fibril-induced cytotoxicity in SH-SY5Y cells. Results show that silybin has a certain inhibitory effect on the HEWL fibrillogenesis process, while silybin B (SB) has a more significant inhibitory effect than silybin A (SA), especially at high concentrations. This work provides some insights into the screening of amyloid inhibitors from complicated natural products and indicates that SB has the prospect of further development as an amyloid inhibitor.
研究领域:
生物化学
·
药理学
·
分子生物学
·
生物物理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2024
·
IF 4.8
Xinyu Yao,Jinying Gao,Lanqiao Wang,Xiaoning Hou,Litao Ge,Xinxin Qin,Jiazhang Qiu,Xuming Deng,Wei Li,Jianfeng Wang
Ethnopharmacology relevance Cananga oil (CO) is derived from the flowers of the traditional medicinal plant, the ylang-ylang tree. As a traditional antidepressant, CO is commonly utilized in the treatment of various mental disorders including depression, anxiety, and autism. It is also recognized as an efficient antibacterial insecticide, and has been traditionally utilized to combat malaria and acute inflammatory responses resulting from bacterial infections both in vitro and in vivo . Aim of the study The objective of this study is to comprehensively investigate the anti- Salmonella activity and mechanism of CO both in vitro and in vivo , with the expectation of providing feasible strategies for exploring new antimicrobial strategies and developing novel drugs. Methods The in vitro antibacterial activity of CO was comprehensively analyzed by measuring MIC, MBC, growth curve, time-killing curve, surface motility, biofilm, and Live/dead bacterial staining. The analysis of the chemistry and active ingredients of CO was conducted using GC-MS. To examine the influence of CO on the membrane homeostasis of Salmonella , we conducted utilizing diverse techniques, including ANS, PI, NPN, ONPG, BCECF-AM, DiSC3(5), and scanning electron microscopy (SEM) analysis. In addition, the antibacterial mechanism of CO was analyzed and validated through metabolomics analysis. Finally, a mouse infection model of Salmonella typhimurium was established to evaluate the toxic side effects and therapeutic effects of CO. Results The antibacterial effect of CO is the result of the combined action of the main chemical components within its six (palmitic acid, α-linolenic acid, stearic acid, benzyl benzoate, benzyl acetate, and myristic acid). Furthermore, CO disrupts the balance of purine metabolism and the tricarboxylic acid cycle (TCA cycle) in Salmonella , interfering with redox processes. This leads to energy metabolic disorders and oxidative stress damage within the bacteria, resulting in bacterial shock, enhanced membrane damage, and ultimately bacterial death. It is worth emphasizing that CO exerts an effective protective influence on Salmonella infection in vivo within a non-toxic concentration range. Conclusion The outcomes indicate that CO displays remarkable anti- Salmonella activity both in vitro and in vivo . It triggers bacterial death by disrupting the balance of purine metabolism and the TCA cycle, interfering with the redox process, making it a promising anti- Salmonella medication.
研究领域:
药理学
·
微生物学
·
代谢组学
·
传染病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）