更新于：2024-11-12
Fosinopril Sodium
福辛普利钠
更新于：2024-11-12
概要
基本信息
在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C30H46NNaO7P |
InChIKeyNIDZYXQFQSHBTG-WATAJHSMSA-N |
CAS号88889-14-9 |
关联
11
项与 福辛普利钠 相关的临床试验一项在健康中国参加者中评估中国产与意大利产福辛普利钠片生物等效性的单剂量、开放性、随机、双向交叉研究
一项在健康中国参加者中评估中国产与意大利产 Monopril (10 mg) 片剂生物等效性的单剂量、开放性、随机、双向交叉研究
Comparison of Efficacy and Safety Between Benidipine and Hydrochlorothiazide in Fosinopril Treated Chronic Kidney Disease Patients With Hypertension: a Randomized Controlled Trial
100 项与 福辛普利钠 相关的临床结果
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100 项与 福辛普利钠 相关的转化医学
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100 项与 福辛普利钠 相关的专利（医药）
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582
项与 福辛普利钠 相关的文献（医药）2024-06-01Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica
[Modified Fangji Huangqi Decoction alleviates renal interstitial fibrosis by inhibiting TGF-β1/Smad/Snail signaling pathway during epithelial-mesenchymal transition].
Article
作者: Jin, Li ; Deng, Ya-Wen ; Chen, Dong-Ping
This study investigated the effects of modified Fangji Huangqi Decoction on the expression of proteins related to epithelial-mesenchymal transition(EMT) in a mouse model of unilateral ureteral obstruction( UUO) and in a rat renal tubular epithelial cell(NRK-52E) model of fibrosis induced by transforming growth factor β1(TGF-β1). It aims to decipher the molecular mechanism by which modified Fangji Huangqi Decoction alleviates renal interstitial fibrosis. C57/BL mice were subjected to UUO.After the surgery, the mice were treated with 0. 5-fold and 2-fold concentrations of modified Fangji Huangqi Decoction and fosinopril sodium(positive control) for 7 days. The interstitial collagen deposition in the kidney was assessed by Masson staining. Western blot and RT-qPCR were employed to determine the expression levels of TGF-β1, phosphorylated Smad2/3(p-Smad2/3), Smad2/3, Snail,epithelial cadherin(E-cadherin), alpha smooth muscle actin(α-SMA), and vimentin. The NRK-52E cell model induced by TGF-β1was treated with the serum samples collected from SD rats treated with different concentrations of modified Fangji Huangqi Decoction.The CCK-8 assay was employed to examine the effects of the serum samples on NRK-52E cell proliferation. The cell morphology in different groups was observed under a microscope. Furthermore, the modeled cells were treated with the serum containing 1-fold decoction. Western blot and RT-qPCR were then employed to measure the expression levels of p-Smad2/3, Smad2/3, Snail,E-cadherin, α-SMA, and vimentin in the cells. Under the same conditions, sh RNA was used to silence the Snail gene, and measurements were repeated before and after treatment with the serum containing 1-fold decoction. The results indicated that modified Fangji Huangqi Decoction alleviated the fibrotic injury in the mouse model of UUO and the fibrosis in the NRK-52E cell model. The treatment with the decoction down-regulated the protein and m RNA levels of EMT-related indicators including p-Smad2/3, α-SMA,Snail, and vimentin, while it up-regulated the expression of E-cadherin. After sh RNA silencing of the Snail gene, the protein and m RNA levels of E-cadherin, α-SMA, and vimentin showed no significant differences before and after treatment with the serum containing the decoction. The results suggest that modified Fangji Huangqi Decoction may alleviate renal interstitial fibrosis by inhibiting the TGF-β1/Smad/Snail signaling pathway and regulating the EMT process.
2024-01-01Journal of ethnopharmacology
Equivalent evaluation and biological ingredients of Syringa pinnatifolia against acute myocardial ischemia in mice
Article
作者: Chai, Xingyun ; Chen, Suyile ; Wuken, Shana ; Liu, Changxin ; Ma, Xiaojing ; Xu, Jixuan ; Gao, Xiaoli ; Liang, Yana ; Chen, Hongying ; Jiao, Shungang
ETHNOPHARMACOLOGICAL RELEVANCE:
The peeled roots, stems, and twigs of Syringa pinnatifolia Hemsl., known as Shan-Chen-Xiang (SCX) in Chinese, has the traditional effects such as anti-Khii, clearing heat and relieving pain. It has been clinically applied for the treatment of heart failure and mental abnormalities, and gradually replaced agarwood in Mongolian medicine.
AIM OF STUDY:
The present study aims to evaluate whether the key subfraction C (C), a half composition in mass of total ethanol extract (T) of SCX, exerts an equivalent effect against acute myocardial ischemia (AMI) compared to fraction I (I), and what was the potential pharmacologically active constituents of SCX.
MATERIALS AND METHODS:
Cardiac function, serum marker enzymes, and myocardial tissue pathology of infarcted mice with ligation of the anterior descending (LAD) branch of the left coronary artery were used to evaluate the anti-AMI effect of C and its equivalent potency to that of I. LCMS-IT-TOF was used to identify the main constituents in C and C-. The new and known compounds were isolated from C by a combination of mass spectrometry and bioactivity-guided fractionation methods, and structures were elucidated by extensive spectroscopic and chemical methods, including calculated 13C NMR data, calculated electronic circular dichroism, and single-crystal X-ray crystallography. The protective effect of isolates against oxidative injury induced by H2O2 in H9c2 cells was evaluated according to a previously reported protocol.
RESULTS:
The results of cardiac function, serum marker enzymes and myocardial tissue pathology observations (fosinopril as a positive drug) suggested that C (40 mg/kg, orally administered once a day for 7 days) possessed the anti-AMI effect and was equivalent to that of I, while C- did not show the positive effect. Then, 32 lignans were isolated from C, including the majors (8R,8'R,9S)-4,4'-dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan (24) and (8R,8'R,9R)-4,4'-dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan (25), which were confirmed by HPLC and LC-MS characterization. Among them, 15 ones were previously undescribed, including a pair of enantiomers (6a/6b), and 11 ones (1, 2, 6a/6b, 8, 10, 12, 16, 17, 24, and 25) exhibited protective effect against oxidative injury to H9c2 cells at different concentrations (ranged from 0.156 to 80 μM).
CONCLUSION:
C (40 mg/kg) exerts cardioprotective effect in mice, which was equivalent to that of I and T. Lignans, including both representative compounds (24, 25) and other undescribed molecules with low content, significantly contribute to the anti-AMI effect of SCX. However, the anti-AMI property assessment of SCX should not exclude the contribution from the representative sesquiterpenoid ZER. Hence, the exploration of the final potential substances in SCX requires further investigation.
2023-11-01The Journal of biological chemistry
Babesia BdFE1 esterase is required for the anti-parasitic activity of the ACE inhibitor fosinopril
Article
作者: Thekkiniath, Jose ; Gewirtz, Meital ; Lonardi, Stefano ; Vydyam, Pratap ; Choi, Jae-Yeon ; Gihaz, Shalev ; Chand, Meenal ; Gennaro, Joseph C ; Ben Mamoun, Choukri
Effective and safe therapies for the treatment of diseases caused by intraerythrocytic parasites are impeded by the rapid emergence of drug resistance and the lack of novel drug targets. One such disease is human babesiosis, which is a rapidly emerging tick-borne illness caused by Babesia parasites. In this study, we identified fosinopril, a phosphonate-containing, FDA-approved angiotensin converting enzyme (ACE) inhibitor commonly used as a prodrug for hypertension and heart failure, as a potent inhibitor of Babesia duncani parasite development within human erythrocytes. Cell biological and mass spectrometry analyses revealed that the conversion of fosinopril to its active diacid molecule, fosinoprilat, is essential for its antiparasitic activity. We show that this conversion is mediated by a parasite-encoded esterase, BdFE1, which is highly conserved among apicomplexan parasites. Parasites carrying the L238H mutation in the active site of BdFE1 failed to convert the prodrug to its active moiety and became resistant to the drug. Our data set the stage for the development of this class of drugs for the therapy of vector-borne parasitic diseases.
100 项与 福辛普利钠 相关的药物交易
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心脏衰竭 | 美国 | 1991-05-16 | |
| 高血压 | 美国 | 1991-05-16 |
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临床4期 | 291 | 鏇築齋鹹積壓鏇遞醖遞(獵積糧壓鹹構醖糧構築) = 鹽艱襯築網獵積獵糧糧 餘構範獵憲簾繭鏇襯構 (壓鑰顧壓窪觸齋網艱鏇, 夢蓋淵鹹製衊餘鏇簾網 ~ 製齋範簾鑰醖顧選鬱齋) 更多 | - | 2017-12-11 | |||
(ACEI Continuation) | 鏇築齋鹹積壓鏇遞醖遞(獵積糧壓鹹構醖糧構築) = 鬱淵壓餘鹽糧憲鏇壓淵 餘構範獵憲簾繭鏇襯構 (壓鑰顧壓窪觸齋網艱鏇, 積製衊襯觸淵構遞齋簾 ~ 膚齋襯餘觸餘範構遞壓) 更多 |
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