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Higenamine Effects on Weight Reduction, Cravings and Diabetes in GLOBESITY Bootcamp for the Obese

Effects of Higenamine on Weight Reduction

Authors: Marcus Free MD, Rouzbeh Motiei-Langroudi MD, Waqar Ahmad PhD, Kelly Daly RDN, and Don Juravin (Don Karl Juravin).

Abstract (Research Summary)

  • Higenamine Hydrochloric Acid (or Higenamine, aka norcoclaurine) is extracted from a variety of herbs and plants, including aconite root, Nandina domestica, Nelumbo nucifera, and Tinospora crispa (Liu 2000). It was traditionally used to treat heart failure, asthma, and gastrointestinal problems.
  • Higenamine reduces gastric motility and energy absorption leading to weight loss and satiety (Verma 2014).
  • Higenamine stimulates beta-adrenergic receptors (both beta1 and beta2) and possesses lipolytic activity (Tsukiyama 2009, Kimura 1994), resulting in burning of body fats, especially triglycerides, rather than restoring them.
  • Higenamine stimulates lipolysis and energy expenditure in both healthy men and women (Lee 2013).
  • Higenamine decreases cellular dopamine content by 55.2% (Shin 1999). Dopamine activates the brain reward system; therefore, decreased dopamine content results in decreased reward response and cravings.
  • Higenamine improves glucose levels, enhances insulin secretion, and reduces hunger hormones, such as ghrelin and neuropeptide Y, leading to a decrease in cravings (Kato 2015, Kang 1999).

Higenamine Effects on Weight Loss

Higenamine stimulates fat burning and energy expenditure and reduces energy absorption by slowing gastric motility, resulting in weight loss and a healthier body fat ratio.

  • Higenamine stimulates lipolysis and energy expenditure by significantly increasing circulating free fatty acids and energy expenditure (Lee 2013).
  • Higenamine has the potential to reduce body weight by decreasing gastric motility, reducing energy absorption, and improving satiety (Verma 2014).
  • Higenamine is a beta-adrenergic receptor agonist (similar to ephedrine and synephrine) capable of reducing fat mass (Tsukiyama 2009, de Souza 2001, Kimura 1994).

Higenamine Effects on Cravings

Higenamine decreases hormones involved with hunger and cravings such as dopamine, ghrelin, and neuropeptide.

  • Higenamine improves blood glucose levels by promoting the synthesis of glucose in the liver and decreasing cravings associated with low blood glucose (Tsukiyama 2009, Kang 1999).
  • Higenamine enhances the secretion of insulin from the pancreas, resulting in controlled glucose levels, and also suppresses hunger hormones such as ghrelin and neuropeptide Y, resulting in decreased cravings (Kang 1999).
  • Higenamine decreases cellular dopamine content by 55.2% (Shin 1999). Dopamine activates the brain reward system, and therefore, decreased dopamine content results in lower reward response and decreased cravings.

Higenamine Effects on Diabetes

Higenamine improves insulin secretion and sensitivity and blood glucose levels and benefits diabetics by increasing the glucose uptake into cells by up to 200%. 

  • Higenamine enhances glucose uptake into cells by 50%. In the presence of insulin, it enhances glucose uptake by 200%, resulting in increased insulin sensitivity (Kato 2015). This effect is beneficial in diabetic and overweight individuals, as increasing insulin sensitivity enhances blood glucose control, decreases cravings, and increases fat burning.
  • Higenamine enhances the secretion of insulin from the pancreas resulting in better glycemic control (Gregory 2015, Kato 2015, Kang 1999).

Benefits, Side Effects, Drug Interactions

Benefits

  • Higenamine (50mg to 100mg per kg) has anti-thrombotic effects which help to prevent blood clots (Yun-Choi 2001).
  • Higenamine can be effective for erectile dysfunction (Kam 2012).

Side effects

  • Nausea: Higenamine is a stimulant and beta agonist which may disturb bowel movement and peristaltic rhythms, resulting in nausea.
  • Sweating: Higenamine increases heat production by enhancing metabolism which may cause excessive sweating.
  • Insomnia: Higenamine increases sympathetic signaling to the brain and may cause insomnia.
  • Anxiety: Higenamine increases the sympathetic effect which may produce anxiety.
  • Tachycardia: Higenamine may increase the heart rate.
  • Fatigue and lethargy

Drug interactions

  • Sympatholytic drugs: Higenamine may reverse the actions of sympatholytic drugs.
  • Sympathomimetic drugs: Higenamine may increase the effects of sympathomimetic drugs.
  • Antidiabetic drugs: As both Higenamine and antidiabetic drugs decrease blood glucose levels, it is important to monitor glucose levels and speak to a physician about decreasing the antidiabetic drugs if required.
  • Anticonvulsants: Higenamine may decrease the the effectiveness of anticonvulsants.
  • Antihypertensives: Higenamine may increase blood pressure and decrease the effects of antihypertensives.
  • Antidepressants: Higenamine may increase anxiety and decrease the effects of antidepressants.

Caution

  • Surgery: Higenamine should be avoided 2 to 3 weeks prior to any surgery.
  • Hypertension and cardiovascular disease: Higenamine should be used with caution if an individual is suffering from cardiovascular disease and hypertension.
  • Pregnancy and breastfeeding: There is limited research and therefore best to avoid during pregnancy or breastfeeding.

References

  1. Bai, G., Yang, Y., Shi, Q., et al. (2008). Identification of higenamine in Radix Aconiti Lateralis Preparata as a beta2-adrenergic receptor agonist. Acta Pharmacologica Sinica, [online], 29 (10), pp. 1187-94. Available from: http://www.nature.com/aps/journal/v29/n10/pdf/aps2008144a.pdf [Accessed 16.05.2016]. 
  2. de Souza, C., Burkey, B. (2001). Beta 3-adrenoceptor agonists as anti-diabetic and anti-obesity drugs in humans. Current Pharmaceutical Design [online], 7 (14), pp. 1433-49. Available from: http://www.ncbi.nlm.nih.gov/pubmed/11472270 [Accessed 06.06.2016]. 
  3. Gregory, P., Abe, A., Hein, D. (2015). Herbal Medications and Vitamin Supplements. In Essentials of Pharmacology for Anesthesia, Pain Medicine, and Critical Care. Springer New York [online], pp. 549-62. Available from http://link.springer.com/chapter/10.1007/978-1-4614-8948-1_33 [Accessed 13.06.2016].
  4. Kam, S., Do, J., Choi, J., et al. (2012). The relaxation effect and mechanism of action of higenamine in the rat corpus cavernosum. International Journal of Impotence Research [online], 24 (2), pp. 77-83. Available from: http://www.ncbi.nlm.nih.gov/pubmed/21956762 [Accessed 13.06.2016]. 
  5. Kang, Y., Lee, Y., Lee, G., et al. (1999). Inhibition of activation of nuclear factor kappaB is responsible for inhibition of inducible nitric oxide synthase expression by higenamine, an active component of aconite root. The Journal of Pharmacology and Experimental Therapeutics [online], 291 (1), pp. 314-20. Available from: https://www.ncbi.nlm.nih.gov/pubmed/10490919 [Accessed 06.06.2016].
  6. Kato, E., Inagaki, Y., Kawabata, J. (2015). Higenamine 4′-O-β-d-glucoside in the lotus plumule induces glucose uptake of L6 cells through β2-adrenergic receptor. Bioorganic and Medicinal Chemistry [online], 23 (13), pp. 3317-21. Available from: http://www.sciencedirect.com/science/article/pii/S0968089615003624 [Accessed 16.05.2016]. 
  7. Kimura, I., Makino, M., Takamura, Y., et al. (1994). Positive chronotropic and inotropic effects of higenamine and its enhancing action on the aconitine-induced tachyarrhythmia in isolated murine atria. Japanese Journal of Pharmacology [online], 66 (1), pp. 75-80. Available from: https://www.jstage.jst.go.jp/article/jphs1951/66/1/66_1_75/_pdf [Accessed 16.05.2016].
  8. Lee, S., Schriefer, J., Gunnels, T., et al. (2013). Acute oral intake of a higenamine-based dietary supplement increases circulating free fatty acids and energy expenditure in human subjects. Lipids in Health and Disease [online], 12:148. Available from: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4016229/pdf/1476-511X-12-148.pdf [Accessed 16.05.2016]. 
  9. Liu, W., Sato, Y., Hosoda, Y., et al. (2000). Effects of higenamine on regulation of ion transport in guinea pig distal colon. Japanese Journal of Pharmacology [online], 84 (3), pp. 244-51. Available from: https://www.jstage.jst.go.jp/article/jjp/84/3/84_3_244/_pdf [Accessed 16.05.2016]. 
  10. Shin, J., Yun-Choi, H., Kim, E., et al. (1999). Inhibitory effects of higenamine on dopamine content in PC12 cells. Planta Medica [online], 65 (5), pp. 452-5. Available from: http://europepmc.org/abstract/med/10418335 [Accessed 03.06.2016]. 
  11. Tsukiyama, M., Ueki, T., Yasuda, Y., et al. (2009). Beta2-adrenoceptor-mediated tracheal relaxation induced by higenamine from Nandina domestica Thunberg. Planta Medica [online], 75 (13), pp. 1393-9. Available from: https://www.thieme-connect.com/DOI/DOI?10.1055/s-0029-1185743 [Accessed 16.05.2016]. 
  12. Verma, K., Paraidathathu, T. (2014). Herbal medicine used in the traditional Indian medicinal system as a therapeutic treatment option for overweight and obesity management: A review. International Journal of Pharmacy and Pharmaceutical Sciences [online], 6 (2), pp. 40-7. Available from: https://www.researchgate.net/profile/Rohit_Verma8/publication/260677281_HERBAL_MEDICINES_USED_IN_THE_TRADITIONAL_INDIAN_MEDICINAL_SYSTEM_AS_A_THERAPEUTIC_TREATMENT_OPTION_FOR_OVERWEIGHT_AND_OBESITY_MANAGEMENT_A_REVIEW/links/0c960531fd82d557ac000000.pdf [Accessed 06.06.2016]. 
  13. Yun-Choi, H., Pyo, M., Park, K., et al. (2001). Anti-thrombotic effects of Higenamine. Planta Medica [online] 67 (7), pp. 619-22. Available from: http://europepmc.org/abstract/med/11582538 [Accessed 03.06.2016]. 

Footnote

This research was sponsored by GLOBESITY FOUNDATION (nonprofit organization) and managed by Don Juravin. GLOBESITY Bootcamp for the obese is part of GLOBESITY FOUNDATION which helps obese with 70 to 400 lbs excess fat to adopt a healthy lifestyle and thereby achieve a healthy weight.

Tags: higenamine, weight reduction, GLOBESITY FOUNDATION, weight loss, cravings, diabetes, healthy weight