PHARMACOLOGY
·
2016
·
IF 1.533
Wang Zhe,Gong Yun,Zeng Da-li,Chen Lian-guo,Lin Gao-tong,Huang Cheng-ke,Sun Wei,Chen Meng-Chun,Hu Guo-xin,Chen Rui-jie
Background: CYP2C9 is one of the most important phase I drug-metabolizing enzymes in liver. The objective of this work was to investigate the effects of apigenin on the metabolism of losartan and human CYP2C9 and rat CYP2C11 activity in vitro. Methods: Different concentrations of apigenin were added to a 100 mmol/l Tris-HCl reaction mixture containing 2 pmol/ml recombinant human CYP2C9.1, 0.25 mg/ml human liver microsomes or 0.5 mg/ml rat liver microsomes to determine the half maximal inhibition or a half-maximal inhibitory concentration (IC50) on the metabolism of losartan. In addition, diclofenac used as CYP2C9 substrate was performed to determine the effects of apigenin on CYP2C9. Results: The results showed that apigenin has the inhibitory effect on the metabolism of losartan in vitro, the IC50 was 7.61, 4.10 and 11.07 μmol/l on recombinant CYP2C9 microsomes, human liver microsomes and rat liver microsomes, respectively. Meanwhile, apigenin's mode of action on human CYP2C9 activity was competitive for the substrate diclofenac. In contrast to its potent inhibition of CYP2C9 in humans (9.51 μmol/l), apigenin had lesser effects on CYP2C11 in rat (IC50 = 15.51 μmol/l). Conclusion: The observations imply that apigenin has the inhibitory effect on the metabolism of losartan and CYP2C9 activity in vitro. More attention should be paid as to when losartan should be administrated combined with apigenin
研究领域:
药理学
·
生物化学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Irfan Ijaz,Aysha Bukhari,Ammara Nazir,Ezaz Gilani,Hina Zain,Attia Shaheen,Mohammed Rafi Shaik,Mujeeb Khan
Lowering the threat of antibiotics is a hot issue in environmental chemistry. To overcome this problem, a novel MBene-based adsorbent, DTT@BC@MoBT x , was designed by modification of bacterial cellulose (BC) using MoBT x MBene and 1,4-dithiothreitol (DTT). Several characterization methods, including Fourier transforms infrared (FTIR), X-ray photoelectron spectroscopy (XPS), and X-ray Diffraction (XRD), confirmed the successful synthesis of DTT@BC@MoBT x composite. It was discovered that the abundance of functional groups, higher specific surface area, and porosity were facilitative for DTT@BC@MoBT x adsorbents to indomethacin (IDM) and losartan (LP). The adsorption of IDM and LP well fitted to the pseudo-second-order kinetic model and Langmuir isotherm model, suggesting the single-layer chemisorption occurred on the adsorbent. The maximum sorption capabilities of the DTT@BC@MoBT x adsorbent were 1041.26 mg/g for IDM and 887.31 mg/g for LP, indicating excellent adsorption performance. The adsorption capacities of IDM and LP showed a slight decline after four consecutive adsorption-desorption tests, indicating excellent regeneration ability and stability. Interfering monoanionic (Na + and K + ) and monoanionic (Cl − and NO 3 − ) exhibited negligible impacts on IDM and LP elimination rates at all three concentrations. Additionally, it was discovered that metal ions had a greater ability for interference in a higher valency state (Mg 2+ , Ca 2+ , SO 4 2− , and CO 3 2− ) than in a lower valency state (Na + , K + , Cl − , and NO 3 − ). The adsorption processes of IDM and LP by the DTT@BC@MoBT x adsorbent involved hydrogen bonding and electrostatic attraction, as shown by FTIR and XPS analyses. This work offered a novel MBene-based adsorbent for the quick and effective adsorption of IDM and LP from water.
研究领域:
环境化学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Biomaterials Science
·
2022
·Vol. 11
·期 2
·583-595
·
IF 7.59
Yihui Huang,Jingwen Li,Yan Wang,Danyang Chen,Jianglong Huang,Wubin Dai,Pan Peng,Liang Guo,Yifeng Lei
High-quality postoperative rehabilitation is the focus of most patients currently, and hypertrophic scar (HS) greatly reduces the patient's quality of life due to the symptom of severe itching. Traditional HS therapies are associated with limitations, such as poor drug delivery efficiency for topical administration and severe pain for intralesional injection. In this study, we developed a personalized microneedle patch system for minimally invasive and effective treatment of HSs. The microneedle patches were personalized designed and fabricated with 3D printing in order to adapt to individual HS. The optimized microneedle patches were composed of dissolving gelatin and starch and loaded with losartan. Losartan, as a drug class of angiotensin II receptor blockers (ARBs), can effectively inhibit the proliferation and migration of hypertrophic scar fibroblasts (HSFs) and downregulate the gene expression related to scar formation in HSFs. The dissolving microneedle patches exhibited strong mechanical strength, effectively penetrated the stratum corneum of HSs and increased the losartan delivery into HSs upon dissolution of gelatin and starch. Together, the losartan-loaded microneedle patches effectively inhibited the formation of HSs in rabbit ears with reduced scar elevation index (SEI), and decreased fibrosis and collagen deposition in HSs. This personalized microneedle patch system increases the drug delivery efficiency into HSs with minimal invasion, and opens a new window for personalized management and treatment of skin diseases.
研究领域:
药学
·
生物医学工程
·
皮肤科
✓ 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）