Roemerine

An OMIC approach to elaborate the antibacterial mechanisms of different alkaloids.[Pubmed:29494814]

Phytochemistry. 2018 May;149:123-131.

Plant-derived substances have regained interest in the fight against antibiotic resistance owing to their distinct antimicrobial mechanisms and multi-target properties. With the recent advances in instrumentation and analysis techniques, OMIC approaches are extensively used for target identification and elucidation of the mechanism of phytochemicals in drug discovery. In the current study, RNA sequencing based transcriptional profiling together with global differential protein expression analysis was used to comparatively elaborate the activities and the effects of the plant alkaloids boldine, bulbocapnine, and Roemerine along with the well-known antimicrobial alkaloid berberine in Bacillus subtilis cells. The transcriptomic findings were validated by qPCR. Images from scanning electron microscope were obtained to visualize the effects on the whole-cells. The results showed that among the three selected alkaloids, only Roemerine possessed antibacterial activity. Unlike berberine, which is susceptible to efflux through multidrug resistance pumps, Roemerine accumulated in the cells. This in turn resulted in oxidative stress and building up of reactive oxygen species, which eventually deregulated various pathways such as iron uptake. Treatment with boldine or bulbocapnine slightly affected various metabolic pathways but has not changed the growth patterns at all.

Roemerine Improves the Survival Rate of Septicemic BALB/c Mice by Increasing the Cell Membrane Permeability of Staphylococcus aureus.[Pubmed:26606133]

PLoS One. 2015 Nov 25;10(11):e0143863.

Staphylococcus aureus is one of the most frequently occurring hospital- and community-associated pathogenic bacteria featuring high morbidity and mortality. The occurrence of methicillin-resistant S. aureus (MRSA) has increased persistently over the years. Therefore, developing novel anti-MRSA drugs to circumvent drug resistance of S. aureus is highly important. Roemerine, an aporphine alkaloid, has previously been reported to exhibit antibacterial activity. The present study aimed to investigate whether Roemerine can maintain these activities against S.aureus in vivo and further explore the underlying mechanism. We found that Roemerine is effective in vitro against four S. aureus strains as well as in vivo against MRSA insepticemic BALB/c mice. Furthermore, Roemerine was found to increase cell membrane permeability in a concentration-dependent manner. These findings suggest that Roemerine may be developed as a promising compound for treating S. aureus, especially methicillin-resistant strains of these bacteria.

[Anti-prostate cancer effect of roemerine: An experimental study].[Pubmed:29658233]

Zhonghua Nan Ke Xue. 2017 Jan;23(1):27-33.

Objective: To investigate the anti-prostate cancer (PCa) effect of Roemerine in vitro and in vivo in the mouse model of PCa. METHODS: We detected the effects of Roemerine on the proliferation, apoptosis and migration of PCa cells DU145, LNCaP, PC-3 and 22RV1, screened out the sensitive cell line and constructed a tumor-bearing model in mice for verification of the antitumor efficacy of Roemerine in vivo. RESULTS: Roemerine inhibited the proliferation and migration of the DU145, LNCaP, PC-3 and 22RV1 cells and induced their apoptosis in different degrees, particularly those of the LNCaP cells. The average tumor weight was less in the Roemerine intervention group (1.99+/-0.95 g) than in the control (2.95+/-1.04 g), the least in the high-dose Roemerine (30 mg/kg) plus paclitaxel intervention group (0.90+/-0.16 g). The mean heart, liver, and kidney indexes were markedly lower in the Roemerine (0.58+/-0.06, 6.20+/-0.42 and 1.49+/-0.33) than in the paclitaxel group (0.66+/-0.04, 6.99+/-0.72 and 1.95+/-0.34), while the mean spleen and thymus indexes were remarkably higher in the former (0.54+/-0.11 and 0.06+/-0.01) than in the latter (0.41+/-0.09 and 0.05+/-0.01). Pathological staining showed a lower degree of malignancy and metastasis in both the Roemerine and the Roemerine + paclitaxel intervention group than in the control, as well as a lower degree of visceral injury in the Roemerine and Roemerine + paclitaxel groups than in the paclitaxel group. CONCLUSIONS: Roemerine has some anti-PCa effect and alleviates adverse reactions in paclitaxel combination administration.

New antiplasmodial alkaloids from Stephania rotunda.[Pubmed:23127648]

J Ethnopharmacol. 2013 Jan 9;145(1):381-5.

ETHNOPHARMACOLOGICAL RELEVANCE: Stephania rotunda Lour. (Menispermaceae) is a creeper growing in many countries of Asia and commonly found in the mountainous areas of Cambodia. As a folk medicine, it has been mainly used for the treatment of fever and malaria. The pharmacological activity is mostly due to alkaloids. Thus the aim of this study is to isolate new bioactive alkaloids from Stephania rotunda and to evaluate their in vitro antiplasmodial activity. MATERIALS AND METHODS: Alkaloids were isolated and identified from dichloromethane and aqueous extracts using a combination of flash chromatography, high performance liquid chromatography, mass spectrometry and nuclear magnetic resonance. The purified compounds were tested for in vitro antiplasmodial activity on chloroquine-resistant W2 strain of Plasmodium falciparum. RESULTS: A new aporphine alkaloid named vireakine (2) along with two known alkaloids stephanine (1) and pseudopalmatine (8), described for the first time in Stephania rotunda, and together five known alkaloids tetrahydropalmatine (3), xylopinine (4), Roemerine (5), cepharanthine (6) and palmatine (7) were isolated and identified. The structure of the new alkaloid was established on the basis of 1D and 2D NMR experiments and mass spectrometry. The compounds were evaluated for their in vitro antiplasmodial and cytotoxic activities. All tested compounds showed significant antiplasmodial activities with IC(50) ranged from 1.2 muM to 52.3 muM with a good selectivity index for pseudopalmatine with IC(50) of 2.8 muM against W2 strain of Plasmodium falciparum and IC(50)>25 muM on K562S cells. CONCLUSIONS: This study provides evidence to support the use of Stephania rotunda for the treatment of malaria and/or fever by the healers. Alkaloids of the tuber exhibited antiplasmodial activity and particularly cepharanthine and pseudopalmatine.

Modeling and optimizing inhibitory activities of Nelumbinis folium extract on xanthine oxidase using response surface methodology.[Pubmed:28273649]

J Pharm Biomed Anal. 2017 May 30;139:37-43.

Xanthine oxidase (XOD), which could oxidize hypoxanthine to xanthine and then to uric acid, is a key enzyme in the pathogenesis of hyperuricemia and also a well-known target for the drug development to treat gout. In our study, the total alkaloids of Nelumbinis folium markedly inhibited XOD activity, with IC50 value being 3.313mug/mL. UHPLC-Q-TOF-MS and 3D docking analysis indicated that Roemerine was a potential active ingredient. A response surface methodology combined with central composite design experiment was further developed and validated for the optimization of the reaction conditions between the total alkaloids of Nelumbinis folium and XOD, which could be considered as a meaningful research for the development of XOD inhibitor rapidly and sensitively.