Frontiers in Pharmacology
·
2022
·
IF 5.988
Rakotondrabe Tojofaniry Fabien,Fan Minxia,Guo Mingquan
E. humifusa Willd, a monoecious annual plant, native to Eastern Asia, has been traditionally attributed to the treatment and prevention of miscellaneous diseases, including diabetes mellitus and its associated complications. Earlier studies have supported this species’ pharmacological efficacies including its antibacterial, antidiabetic, and anti-inflammatory properties. Even so, the underlying bioactive components with their mechanisms of action associated with its antidiabetic and anti-inflammatory effects remain elusive. The preamble in vitro assessments of the crude extract and its different fractions revealed that the n-butanol fraction (EHNB) exhibited the best activity, which was subsequently subjected to a rapid screening of candidate ligands through bio-affinity ultrafiltration with the two enzyme targets: α-glucosidase (α-Glu) and cycloxygenase-2 (COX-2) combined with UPLC/QTOF-MS. As a result, 7 compounds were identified from EHNB, among them, vitexin and astragalin were screened out as the most active ligand compounds. Vitexin showed great specific binding (SB) affinity values of 1.26 toward α-Glu and 1.32 toward COX-2, while astragalin showed 1.32 and 1.36, respectively. The docking simulation results exhibited strong interactions of vitexin and astragalin with the key residues of the enzyme targets, suggesting their possible mechanisms of action. The in vitro antidiabetic validation revealed noticeable half-maximal inhibitory effects (IC50) of 36.38 ± 3.06 µM for vitexin and 42.47 ± 4.13 µM for astragalin, much better than that of the positive drug acarbose (109.54 ± 14.23 µM). Similarly, these two compounds showed the inhibitory activity against COX-2 with the half-maximal inhibitory effects (IC50) at 27.91 ± 1.74 µM and 49.05 ± 1.49 µM, respectively. Therefore, these two flavonoid compounds (vitexin and astragalin) were speculated as potential antidiabetic and anti-inflammatory compounds from E. humifusa. Taken together, the integrated strategy applied to E. humifusa led to the fast identification of two potential double-acting flavonoids and enlightened its antidiabetic and anti-inflammatory uses. Besides these findings, the integrated strategy in this study could also be used to facilitate the rapid discovery and development of active candidates from other traditional herbal medicines against multi-drug targets and to aid in revealing their mechanisms of action for their traditional uses.
研究领域:
药理学
·
植物化学
✓ 已验证
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2023
·
IF 8.8
Caixia Li,Wenyue Li,Xia Zhang,Guidan Wang,Xuebo Liu,Yutang Wang,Lijun Sun
Three physical treatments, including ball-milling (BM), high pressure homogenization (HPH) and cold plasma (CP) were applied to modify structural and functional properties of Cyperus esculentus protein (CEP). The results showed that three treatments significantly altered morphology and reduced particle size of CEP. Both primary and secondary structures of CEP were hardly changed, while disulfide bonds and hydrophobic forces between amino acid residues of CEP were interrupted by three treatments, releasing free sulfhydryls and hydrophobic groups. With the free moiety accumulation, the reformed interactions between them enhanced the crystallinity and thermostability of CEP. Besides, solubility and emulsifying properties of CEP were significantly improved within a certain range of treatment duration and intensity, and three treatments decreased water but increased oil holding capacity of CEP. Conclusively, the modified physicochemical properties of CEP were decided by the changed molecular structures of CEP, and different treatments may satisfy different processing requirements for the protein.
研究领域:
食品科学
·
蛋白质化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Toxicology Research
·
2024
·Vol. 13
·期 2
·
IF 2.2
Niu Junjie,Hu Jinyang,Wang Zhu
BackgroundTriple-negative breast cancer (TNBC) lacks effective therapeutic targets. Scutellaria barbata D.Don (SB) has been revealed to have anti-breast cancer (BC) effect, but the effect of SB extract in TNBC is still unclear. Herein, this research delves into the underlying mechanism.MethodsSB was extracted by solvent extraction, and the main components were identified using an Agilent 6,520 HPLC-Chip/Q-TOF (Chip/Q-TOF) MS system. In vitro cell experiments were conducted. The effects of SB extract alone, SB extract plus EGF, GSK alone, GSK plus Ezrin overexpression, or SB extract plus Ezrin overexpression on cell viability, invasion, migration, and apoptosis were examined by cell function experiments. The apoptosis- and RhoA/ROCK1 pathway-related protein levels were analyzed by western blot assay.ResultsMass spectrometry analysis exhibited that SB extract mainly contains long-chain fatty acids and ursolic acid. SB extract mitigated TNBC cell biological phenotypes, apoptosis- and RhoA/ROCK1 pathway-related marker expressions, which were reversed by EGF. The further results found that GSK obviously weakens TNBC cell biological behaviors, apoptosis- and RhoA/ROCK1 signaling-related protein levels, while oe-Ezrin treatment reverses the effect of GSK on TNBC cells. Moreover, SB extract regulated Ezrin-mediated function of TNBC cells by impeding the RhoA/ROCK1 pathway.ConclusionOur findings demonstrated that SB extract regulated Ezrin-mediated proliferation, migration, invasion, and apoptosis of TNBC cells via suppressing the RhoA /ROCK1 signaling. Our results offer the experimental foundation for further investigation of the anti-cancer role of SB in TNBC cells.HighlightsSB extract inhibits the biological phenotypes of TNBC cells.SB extract inhibits the biological behaviors of TNBC cells through the RhoA/ROCK1 pathway.SB extract modulates Ezrin-mediated TNBC cell proliferation, migration, invasion, and apoptosis via restraining the RhoA/ROCK1 signaling.
研究领域:
肿瘤学
·
药理学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
·
2019
·
IF 3.375
Phongphat Prawang,Yongqiang Zhang,Ying Zhang,Hui Wang
Poly(ethylene glycol) (PEG), a kind of “green” medium, was used to extract artemisinin from the Chinese herb Artemisia annua L. to replace the traditional volatile and explosive solvents like petroleum ether, diethyl ether, etc. PEGs, with different molecular weights, show excellent ability for artemisinin extraction, and the extraction efficiency decreased with the increase of molecular weight. It was also demonstrated that ultrasonic irradiation could further enhance extraction efficiency compared with conventional water bath heating. Results indicate that the extraction amount of artemisinin from one gram of the leaves could reach 15.8 mg/g under the optimal conditions with ultrasonic power of 100 W, the temperature of 50 °C, time of 1 h in PEG-200, which were optimized by response surface method. Compared with Soxhlet extraction using petroleum ether (PE), the method developed here shows higher extraction efficiency (15.8 mg/g for PEG vs. 14.9 mg/g for PE process) and shorter extraction time (1 h vs. ca. 12 h). Additionally, artemisinin in the PEG solution can be recovered using resin adsorber. The results show that the recovery of artemisinin could reach almost 100% by D101 or H103 porous resin, and then the drug could be desorbed from the resin by ethanol or ethyl acetate. Moreover, the kinetic and mechanism studies of the extraction process revealed that ultrasonic irradiation could enhance mass transfer and the hydrogen bonding interactions between artemisinin and PEG further facilitate the separation of artemisinin from the leaves. This work provides an alternative process for efficient artemisinin extraction by using an environmentally benign medium with outfield intensification, which could be potentially extended to the production of other natural drugs.
研究领域:
药学
·
环境化学
·
生物技术
·
化工
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）