The pharmacology, toxicology and potential applications of arecoline: a review

Liu, Yujie; Peng, Wei; Hu, Mei-Bian; Xu, Min; Wu, Chunjie

doi:10.3109/13880209.2016.1160251

Cited by 113 publications

(70 citation statements)

References 71 publications

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“…Thereafter, in vivo and in vitro bioassays are used to screen the change in bioactivity. Based on our preliminary experimental results (Supplementary files Figures S1 and S2) and related references1920, arecoline is the main alkaloid among the total alkaloids of CAN extracted by CHCl 3 . Importantly, we also found that there was no other obvious constituent that interfered in the same position as the arecoline band (Figure S2).…”

Section: Discussionmentioning

confidence: 92%

Using the “target constituent removal combined with bioactivity assay” strategy to investigate the optimum arecoline content in charred areca nut

Peng

Liu

et al. 2017

Sci Rep

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Charred areca nut (CAN) is used to treat dyspepsia and abdominal distension in children. However, reports revealed that arecoline, the most important active constituent of CAN, possesses potential toxicities. This study was designed to investigate the optimum arecoline content in CAN, using the “target constituent removal combined with bioactivity assay” strategy. Based on PTLC method, we prepared CAN lacking all arecoline (WAC-100R) and a series of different ratios of arecoline-removed CAN samples (WAC-Rx). MTT and acute toxicity assays indicated that decreasing content by 50% decreased CAN toxicity significantly. Animal results revealed arecoline contents over 50% could guarantee the beneficial effects of CAN on gastrointestinal tract. Additionally, decreasing arecoline content in CAN by 50% decreased its pro-apoptotic effects significantly. Furthermore, decreasing 50% arecoline content in CAN down-regulated the expressions of Cleaved-Caspase-3, c-jun, c-fos, COX-2, PGE2, and IL-1α. Thus, our results revealed that CAN with 50% arecoline content (WAC-50R) has similar beneficial effects on the gastrointestinal tract to CAN, whereas its toxicity was decreased significantly. Collectively, our study suggested that the strategy of “target constituent removal combined with bioactivity assay” is a promising method to identify the optimum arecoline content in CAN, which is approximately 0.12%.

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Section: Discussionmentioning

confidence: 92%

Using the “target constituent removal combined with bioactivity assay” strategy to investigate the optimum arecoline content in charred areca nut

Peng

Liu

et al. 2017

Sci Rep

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“…Interestingly, although the parasympathomimetic arecoline has been thought to be responsible for most of the effects of betel quid chewing, studies have shown that plasma concentrations of noradrenaline and adrenaline were elevated, suggesting an additional sympathetic activation [64]. In folk medicine, chewing betel nut is considered to enhance the memory [66]. However, use of betel nut is also related to palpitation, oral submucous fibrosis, oral squamous cell carcinoma, and genotoxicity.…”

Section: Arecolinementioning

confidence: 99%

“…However, use of betel nut is also related to palpitation, oral submucous fibrosis, oral squamous cell carcinoma, and genotoxicity. Arecoline is reported to be the primary toxic constituent responsible for these effects [65,66].…”

Section: Arecolinementioning

confidence: 99%

Getting More Than You Paid For: Unauthorized “Natural” Substances in Herbal Food Supplements on EU Market

Končić

2018

Planta Med

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As the population in the industrialized world develops preference for what is perceived as a natural and holistic way of disease treatment, the popularity and the number of food supplements on the market, including herbal ones, is experiencing an unprecedented rise. However, unlike herbal medicinal products, intended for treating or preventing disease, current legislation classifies food supplements as products intended for achieving nutritional or physiological effect and to supplement the normal diet. Accordingly, most food supplements are not to be associated with specific health claims. However, either due to the subtle suggestions by the producers or the wishful thinking of the consumers, certain pharmacological effects from food supplements are often expected. Medicinal plants included in food supplements usually do not produce dramatic and instant pharmacological effects. Therefore, in order to meet the expectation of their customers, some producers have turned to the illicit and dangerous practice of adulterating their products with synthetic adulterants, including naturally occurring molecules, having the desired activity. Such practice is prevalent in, although not limited to, food supplements intended for use as weight-loss aids, as well as for sport performance and libido enhancement. The review is focusing on naturally occurring alkaloids, phenylethanolamines, and their semi-synthetic derivatives in food supplements in the European Union as reported by the Rapid Alert System for Food and Feed. Their desired and undesired pharmacological effects, as well as the methods for their detection and quantification in food supplements, will be reviewed.

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“…AN extract (ANE) can induce the generation of reactive oxygen species (ROS) in both saliva and solution, as well as the modification of DNA [2,3]. The major alkaloid of AN, arecoline, is capable of causing oral submucous fibrosis (OSF), oral squamous cell carcinoma (OSCC) and genotoxicity [4]. Moreover, arecoline and another AN ingredient, oligomeric procyanidins, are known to trigger cellular apoptosis [5,6].…”

Section: Introductionmentioning

confidence: 99%

Mechanistic and compositional studies of the autophagy-inducing areca nut ingredient

Chiu

Liu

Yen

et al. 2019

Preprint

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Areca nut (AN) is a popular chewing carcinogen worldwide causing a variety of diseases such as oral and esophageal carcinomas. We previously found that the partially purified 30-100 kDa fraction of AN extract (ANE 30-100K) induces autophagy in oral carcinoma OECM-1 cells and some other different types of cells. Since autophagy is known to play important roles in tumor establishment and development, the underlying mechanisms of ANE 30-100K-induced autophagy (AIA) is worthy of further investigation. In this study, we further demonstrated that the cytotoxic concentration of ANE 30-100K induces some typical autophagy hallmarks in esophageal carcinoma (CE81T/VGH) cells in an Atg5-dependent manner. Furthermore, the endocytosis inhibitor (methyl-β-cyclodextrin) and two caveolin shRNAs, as well as two proteasome inhibitors (lactacystin and epoxomicin), were shown to attenuate ANE 30-100K-induced cytotoxicity and LC3-II accumulation significantly in OECM-1 and CE81T/VGH cells. Finally, we also analyzed the carbohydrate compositions of ANE 30-100K by phenol-sulfuric acid method and high performance anion exchange chromatography with pulse amperic detector. The results showed that ANE 30-100K contains about 67% carbohydrate and is composed of fucose (5.938%), arabinose (24.631%), glucosamine (8.066%), galactose (26.820%), glucose (21.388%), and mannose (13.157%). Collectively, these results suggest that caveolin-mediated endocytosis and proteasome are required for AIA and the major components of ANE 30-100K are carbohydrates. This study may have provided new knowledges of the action mechanisms and compositions of ANE 30-100K.

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The pharmacology, toxicology and potential applications of arecoline: a review

Cited by 113 publications

References 71 publications

Using the “target constituent removal combined with bioactivity assay” strategy to investigate the optimum arecoline content in charred areca nut

Using the “target constituent removal combined with bioactivity assay” strategy to investigate the optimum arecoline content in charred areca nut

Getting More Than You Paid For: Unauthorized “Natural” Substances in Herbal Food Supplements on EU Market

Mechanistic and compositional studies of the autophagy-inducing areca nut ingredient

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