Rescinnamine in Treatment of Hypertension in Hospital Clinic and in General Practice

Fife, Rose S.; Maclaurin, J. C.; Wright, J. H.

doi:10.1136/bmj.2.5216.1848

Cited by 17 publications

(8 citation statements)

References 9 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Rescinnamine is a natural product from Rauwolfia serpentine and used as an antihypertensive drug that acts via inhibition of angiotensin-converting enzyme . Syrosingopine is structurally similar to rescinnamine because it is a derivative of reserpine, which, like rescinnamine, is an alkaloid derived from the roots of Rauwolfia species. , Transcriptome profile data for these two compounds were decomposed in a chemical space composed of the rest of the CMap data set (291 compounds) with OLSA, and we noticed that some of the decomposed effects of these compounds, such as P10V and P24V effects, exhibited relatively different scores from the other decomposed effects and were selected as outliers based on interquartile range (Figure a–c). The structure and the overall transcriptome profiles of the two compounds have the greatest similarity, as evaluated with Tanimoto coefficients of Morgan-fingerprint-based description of structures and Pearson correlation coefficients of transcriptome profiles with whole variables (Figure d and e).…”

Section: Resultsmentioning

confidence: 99%

Decomposition Profile Data Analysis for Deep Understanding of Multiple Effects of Natural Products

et al. 2021

View full text Add to dashboard Cite

It is difficult to understand the entire effect of a natural product because such products generally have multiple effects. We propose a strategy to understand these effects effectively by decomposing them with a profile data analysis method we developed. A transcriptome profile data set was obtained from a public database and analyzed. Considering their high similarity in structure and transcriptome profile, we focused on rescinnamine and syrosingopine. Decomposed effects predicted clear differences between the compounds. Two of the decomposed effects, SREBF1 activation and HDAC inhibition, were investigated experimentally because the relationship between these effects and the compounds had not yet been reported. Analyses in vitro validated these effects, and their strength was consistent with predicted scores. Moreover, the number of outliers in decomposed effects per compound was higher in natural products than in drugs in the data set, which is consistent with the nature of the effects of natural products.

show abstract

Section: Resultsmentioning

confidence: 99%

Decomposition Profile Data Analysis for Deep Understanding of Multiple Effects of Natural Products

et al. 2021

View full text Add to dashboard Cite

show abstract

“…These molecules have been considered for biological applications, especially rescinnamine (that targets FLAT3 and BCL-2 G101V in this study) and bisacodyl (that targets BCL-2 in this study) are known drugs in clinical applications. Rescinnamine is a vinca alkaloid that is derived from Rauvolfia serpentina and is used as an antihypertensive drug [32,33]. Bisacodyl is a stimulant laxative drug that is being used to treat constipation and found to be both safe and effective for long-term use [34,35].…”

Section: The Top-ranked Molecules From the Traditional Concoctionsmentioning

confidence: 99%

Probing New Antileukemia Agents That Target FLT3 and BCL-2 from Traditional Concoctions through a Combination of Mass Spectrometry Analysis and Consensus Docking Methods

Adeniyi

Nlooto

et al. 2022

Applied Sciences

View full text Add to dashboard Cite

The search for new chemotherapeutics against leukemia is of great interest to researchers, owing to the limitation of the current drugs. In this research, new drug candidates against leukemia were probed through liquid chromatography-mass spectrometer (LC-MS) analysis of three traditional herbal concoctions, that provide the phytochemical profile of the samples. The identified compounds from the LC-MS were modeled for the analysis of their antileukemia activities, by using five different consensus methods, to combine the seven docking scores. The consensus methods are used to combine the docking scores to avoid losing promising drug candidates, due to a poor reproducibility of the docking scores across the different packages, due to differences in the scoring functions and training sets across the docking packages. The libraries of the potential drug candidates from the concoctions were constructed by searching the NIST database for molecules with a similar MS fragmentation. Venetoclax and gilteritinib, that target FLT3 and BCL-2 were ranked among the top hits, indicating the efficiency of this protocol without missing any potential drug. The results ranked rescinnamine and bisacodyl as new potential antileukemia agents that targets FLAT3, and BCL-2, including the mutated BCL-2 G101V receptor, that is known to be resistant to treatment with venetoclax.

show abstract

“…The genus Polygala, containing spiecs P. tenuifolia, is the richest resource for TMCA esters [19]. Additionally, TMCA esters also exist in the genus Erythroxylum [20] and Rauwolfia [21].…”

Section: Biological Activities Of Natural Tmca Ester and Amide Derivamentioning

confidence: 99%

“…Rescinnamine (N8) isolated from Rauvolfia, known as moderil or anaprel, was considered as an angiotensin-converting enzyme inhibitor used as an antihypertensive drug clinically ( Fig. 4) [21]. This ester exhibited significant inhibition against SARS (severe acute respiratory syndrome) as well.…”

Section: Biological Activities Of Natural Tmca Ester and Amide Derivamentioning

confidence: 99%

Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives

Zhao

Song

Xie

et al. 2019

European Journal of Medicinal Chemistry

View full text Add to dashboard Cite

a b s t r a c t TMCA (3,4,5-trimethoxycinnamic acid) ester and amide are privileged structural scaffolds in drug discovery which are widely distributed in natural products and consequently produced diverse therapeutically relevant pharmacological functions. Owing to the potential of TMCA ester and amide analogues as therapeutic agents, researches on chemical syntheses and modifications have been carried out to druglike candidates with broad range of medicinal properties such as antitumor, antiviral, CNS (central nervous system) agents, antimicrobial, anti-inflammatory and hematologic agents for a long time. At the same time, SAR (structure-activity relationship) studies have draw greater attention among medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is an urgent need for the medicinal chemists to further exploit the precursor in developing chemical entities with promising bioactivity and druggability. This review concisely summarizes the synthesis and biological activity for TMCA ester and amide analogues. It also comprehensively reveals the relationship of significant biological activities along with SAR studies.

show abstract

Rescinnamine in Treatment of Hypertension in Hospital Clinic and in General Practice

Cited by 17 publications

References 9 publications

Decomposition Profile Data Analysis for Deep Understanding of Multiple Effects of Natural Products

Decomposition Profile Data Analysis for Deep Understanding of Multiple Effects of Natural Products

Probing New Antileukemia Agents That Target FLT3 and BCL-2 from Traditional Concoctions through a Combination of Mass Spectrometry Analysis and Consensus Docking Methods

Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives

Contact Info

Product

Resources

About