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Markers of Cholinergic Dysfunction in Alzheimer Disease
Published in Robert E. Becker, Ezio Giacobini, Alzheimer Disease, 2020
Ezio Giacobini, Kiminobu Sugaya, Rodger J. Elble
In a recent series of pharmacological challenges in 83 neuropsychiatric patients and controls, Sunderland et al. (1988) contrasted the effect of scopolamine (0.1-0.5 mg i.v.) with infusion of two cholinergic agonists [arecoline (1-4 mg/hr) and nicotine (0.125-0.50 μg/kg/min)]. Alzheimer patients exhibited greater sensitivity to central cholinergic blockade than age-matched controls or elderly depressives. A differential sensitivity to arecoline and nicotine was also observed. Newhouse et al. (1988) also compared patients with AD to elderly depressed patients and found a greater sensitivity to scopolamine in AD. However, the sensitivity and selectivity of these pharmacologic probes are still unestablished, and the effect of these probes on specific neuropsychological measures may be expected to vary among patients with the same disease (e.g. AD) and particularly among patients with different diseases.
Treatment Of Alzheimer’s Disease
Published in Zaven S. Khachaturian, Teresa S. Radebaugh, Alzheimer’s Disease, 2019
Lina Shihabuddin, Kenneth L. Davis
Arecoline is a natural alkaloid with both muscarinic and nicotinic agonist properties. Arecoline administration to normal volunteers improves learning (Sitaram et al., 1978). Modest improvement in verbal and spatial memory has been observed after continuous intravenous infusion of arecoline for 5 days in patients with Alzheimer’s disease (Raffaele et al., 1991).
Parasympathomimetic Amines
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Arecoline is a tertiary amine obtained from the betel or areca nut (Areca catechu) (Table 8.2). It has muscarinic activity that is dependent upon the pH of the medium; at the pH of plasma and most physiological salt solutions (7.4) it is 60% protonated and has ~80% of the muscarinic activity of Ach. The non-protonated form is virtually inactive. Betel nuts have been chewed in many parts of Asia to produce salivation and for its mild central stimulant action. They are not used therapeutically in human medicine but arecoline has been employed in veterinary medicine as a purgative and vermifuge for Taenia, although it is not taenicidal. It probably expels the worm by intense intestinal contractions.
Metabolism of the areca alkaloids – toxic and psychoactive constituents of the areca (betel) nut
Published in Drug Metabolism Reviews, 2022
The work of Meghji et al. (1987) showed that arecoline is metabolized to arecaidine in normal and diseased (OSF) human fibroblasts, although the metabolism rates did not differ between fibroblast types. Jeng et al. (1999) found that arecoline-induced cytotoxicity to human oral mucosal fibroblasts can be abolished by the addition of pig liver esterase, suggesting a detoxification role of carboxylesterase. Similarly, Chang et al. (2013) found that addition of pig liver carboxylesterase prevents arecoline-induced stimulated buccal mucosa fibroblast (OMF)-populated collagen gel contraction; however, pig liver esterase was unable to reverse AN extract mediated contraction, suggesting the involvement of other AN compounds in AN-induced oral carcinogenesis. Interestingly, in the presence of rat S9, a significant reduction in arecoline-induced mutagenicity in cellular models was observed (Wang and Peng 1996), which speculatively could be due to detoxification by esterase enzymes.
Arecoline plays dual role on adrenal function and glucose-glycogen homeostasis under thermal stress in mice
Published in Archives of Physiology and Biochemistry, 2020
Romi Dasgupta, Indraneel Saha, Prajna Paramita Ray, Aniruddha Maity, Debajoyti Pradhan, Hari Prasad Sarkar, B. R. Maiti
Arecoline is a plant alkaloid, present abundantly in the betel nut of Areca catechu (Rooban et al. 2005) which is chewed raw or with betel quid by millions of people for stress reduction and heightened alertness. Arecoline is used for the treatment of presenile dementia with Alzheimer’s disease (Soncrant et al. 1993) and schizophrenia (Sullivan et al. 2000). It has a wide spectrum of untoward effects, such as oral carcinoma, immunosuppression, antioxidant depression and hepatotoxicity (Dasgupta et al. 2006) in mice. Arecoline has multiple actions on endocrine functions, while it stimulates adrenal and testicular functions, suppresses pineal and thyroid activities in rats and mice (Saha et al. 2007, Dasgupta et al. 2010a, 2010b). There are also reports that arecoline aggravates hypothyroidism in metabolic stress (Dasgupta et al. 2017) and ameliorates hypothyroid condition in cold stress. Recently Saha et al. (2017) have reported that, arecoline cannot exert its action on pineal-testicular function in noise in rats. Thus, it is pertinent to examine the role of arecoline on adrenocortical and adrenomedullary functions including their target on glucose-glycogen homeostasis in cold and heat stress in mice.
Arecoline suppresses epithelial cell viability by upregulating tropomyosin-1 through the transforming growth factor-β/Smad pathway
Published in Pharmaceutical Biology, 2020
Long Li, Liqun Gu, Zhigang Yao, Yuehong Wang, Zhangui Tang, Xiaoying Wu
Arecoline is considered a paramount factor in the development of OSF. In several studies, arecoline suppressed cell growth and induced an increase in the percentage of HaCaT cells remaining in the G1 phase (Gu et al. 2019; Zhou et al. 2013). Arecoline significantly suppressed HaCaT cell viability and induced cell apoptosis in another study (Li et al. 2014). Our findings are consistent with these previous reports. However, contrary to a previous study on cell migration, we observed no obvious differences between HaCaT cell lines treated with arecoline and the controls. Previous studies have shown that human oral epithelial cells treated with a low dose of arecoline for a prolonged time (90 days) displayed increased migration compared with untreated controls (Wang et al. 2016). This discrepancy may be due to the different treatment concentrations and treatment times of arecoline used in the studies.