Increasing the Sensitivity of Adipocytes and Skeletal Muscle Cells to Insulin
Christophe Wiart in Medicinal Plants in Asia for Metabolic Syndrome, 2017
Arecoline (Figure 4.23) at a concentration of 60 μM inhibited adipogenesis in 3T3-L1 cells by 82% with reduction of CCAAT/enhancer-binding protein-α, -γ and downstream targets fatty acid-binding protein, glucose transporter-4, lipoprotein lipase.341 In differentiated 3T3-L1 adipocytes, this alkaloid at 500 μM evoked lipolysis as evidenced by a burst in glycerol release (on probable account of cyclic adenosine monophosphate/adenylyl cyclase) and abrogated insulin-dependent glucose uptake by 18%.341 This alkaloid at a much lower concentration (20 μg/mL) reduced the accumulation of lipid droplet in 3T3-L1 adipocytes via downregulation of CCAAT/enhancer-binding protein-β and peroxisome proliferator-activated receptor-γ.342 In the same experiment, arecoline at 20 µg/ml downregulated insulin receptor, insulin receptor substrate-1, glucose transporter-4, fatty acid synthetase, perilipin, and adipophilin.342 Arecoline is a M3 muscarinic agonist.343 Yang et al. observed that acetylcholine at 1 μM attenuated insulin-stimulated glucose uptake and the release of glycerol from adipose tissues isolated from Wistar rats via M3 muscarinic receptor activation.344 It must be recalled that arecoline is toxic for the liver and testicles.345
Metabolic Mapping with Deoxyglucose Autoradiography as an Approach for Assessing Drug Action in the Central Nervous System
Edythe D. London in Imaging Drug Action in the Brain, 2017
Overall, drugs that affect cholinergic systems clearly have metabolic effects in brain structures and systems intimately associated with learning and memory functions. Cholinergic agonists enhance performance in experimental paradigms which involve memory tasks both in man and animals while cholinergic antagonists have the opposite effect (see Collerton, 1986). Interestingly, doses of arecoline that cause memory improvements in aged monkeys (0.05 to 0.1 ml/kg) (Bartus et al., 1985) are similar to those that cause selective enhancement of hippocampal glucose use in the rat (Soncrant et al., 1985a). In the rodent brain, senescence is associated with a reduction in the density of muscarinic receptors (Gurwitz et al., 1981; Pedigo et al., 1984). Despite this finding, however, the regional cerebral metabolic responsivity to arecoline is no different in aged compared to young rats (Soncrant et al., 1989).
Markers of Cholinergic Dysfunction in Alzheimer Disease
Robert E. Becker, Ezio Giacobini in Alzheimer Disease, 2020
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.
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.
Text, picture or video: effects of different consumption guidance methods on betel nut sensory evaluation and risk perception
Published in Journal of Substance Use, 2022
Hong Wen, Hong Zheng, Lifang Li, Fengshan Li
Betel nut (BN) is the fourth most popular psychoactive substance in the world (IARC, 2004). The arecoline and arecaidine in BN can increase the adrenaline, resist anxiety, and make people excited and addicted (Chu, 2001; Lim, 2003). Meanwhile, BN has been listed as a first-class carcinogen by the World Health Organization (IARC, 2004). It is confirmed that BN has certain damage on the body’s energy metabolism regulation and immune response, such as hyperglycemia, atherosclerosis, and inflammation (Wei et al., 2017). Chewing BN will also cause great damage to the oral cavity (Chang et al., 2017), including oral ulcers, oral mucosa damage, and even oral leukoplakia and oral submucous fibrosis, which are high-risk preneoplastic states (Lee et al., 2003).
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