Friday, 14 February 2020

Antioxidants Triterpenoids, a Natural Antihistamines

By Kyle J. Norton

Histamine, found within granules of basophils and mast cells (>90% of body stores) is a biogenic amine and an organic nitrogen compound that occurs to various degrees in many foods such as cherries to about 0.17-13.46 ng/g, bananas, and grapes, rice, and cereals, herbs, olive oil, wine, beer, etc.

In healthy persons, dietary histamine can be rapidly detoxified by amine oxidases, whereas persons with low amine oxidase activity are at risk of histamine toxicity(a). The hormone, as a neurotransmitter is involved in regulating physiological function in the gut and immune response to foreign pathogens.

Antihistamines are medicines that treat allergic rhinitis and other allergies associated with relief from nasal congestion, sneezing, or hives caused by pollen.

Health benefits of hormone histamine may include
* Histamine and motivation
Brain histamine may affect a variety of different behavioral and physiological functions; however, its role in promoting wakefulness has overshadowed its other important functions.

*  Role of histamine in motion sickness
The Faculty of Pharmaceutical Sciences, University of Tokyo, found that shaking the animals for 2 min increased HA contents in telencephalon and diencephalon without significantly changing the t-MH levels. alpha-Fluoromethylhistidine (alpha-FMH), which is presumed to deplete the neuronal HA, tended to raise the HA levels. alpha-FMH slightly alleviated the vomiting response to motion stimulus and suppressed the HA increase in diencephalon caused by shaking.

* Histamine and IgE-mediated diseases
The release of preformed histamine from mast cells causes increased vascular permeability via smooth muscle contraction and development of a wheal; inflammatory mediators initiate a neural reflex causing vasodilatation, leading to erythema (the flare)(19).

* Histamine in addiction and addiction-related behaviors
Research conducted during the past decade demonstrated that the ability of many antihistaminic drugs to potentiate addiction-related behaviors essentially results from non-specific effects and does not constitute a valid argument in support of an inhibitory function of histamine on reward processes.

* Histamine and stimulate gastric acid secretion
Ghrelin, a novel growth hormone-releasing peptide, is present in the rat and human stomach and is known to stimulate the acid secretion and stomach motility. In the study to elucidate the role of histamine in ghrelin-induced acid secretion in the rat stomach. Intravenous administration of ghrelin at 0.8 to 20 microg/kg dose-dependently increased gastric acid secretion, as measured by the gastric lumen perfusion method.

* Histamine and neurotransmitter release
In the study to investigate the effect of histamine-3 (H(3)) receptors, expressed in the tuberomammillary nucleus (TMN) of the hypothalamus and in the prefrontal cortex (PFC), on histamine neurotransmission in the rat brain, showed that systemic administration of the selective H(3)-agonist, immepip, decreases, and the reverse H(3) /H(4)-agonist, thioperamide, increases the firing activity of histamine neurons in the TMN and the release of histamine in TMN and PFC.


Beta-Sitosterol is a phytochemical in the class of Phytosterols, belongings to the group of Lipids, found abundantly in avocados, rice bran, wheat germ, corn oils, fennel, peanuts, soybeans, hawthorn, basil, buckwheat. etc.

On finding a potential phytochemical for the prevention and treatment of inflammatory diseases, researchers examined the antihistaminic activity of triterpenoids isolated from Bursera cuneata.

The study included phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) induced edema in mice treated by 3 extracts of different polarities.
According to the chemical analysis,
* The dichloromethane extract had the highest anti-inflammatory effect (89.1 ± 2.2% inhibition) over that of the hexane (53.3 ± 1.2%) and methanolic (77.4 ± 1.8%) extracts at a dose of 0.1 mg/ear.

* The FS-3 fraction, obtained from the dichloromethane extract, comprised triterpenes β-sitosterol (1), α-amyrin (2), moronic acid (3), and ursolic acid (4), and all the compounds showed significant activity in comparison with that of indomethacin (41.5 ± 0.6%) at 0.1 mg/mouse ear.

* Moronic acid displayed the highest inhibitory effect (68.1 ± 1.3%).

* Moronic acid was the most active (73.3 ± 1.1%, indomethacin 33.8 ± 0.8%) on histaminic activity.

Finally, moronic acid was found to be a principal anti-inflammatory and antihistaminic compound present in B. cuneata. 

Furthermore, in RAW 264.7 cell stimulated with LPS, moronic acid at 30 and 15 mg/mL a significant reduction of ON was observed (36% and 28% respectively) but had no significant effect on TNFα production.

Based on the findings, researchers said, "the organic extracts and isolated compounds from the aerial parts of B. cuneata had topical anti-inflammatory and antihistaminic activities in vivo, but in vitro only modified the production of ON in RAW cells. The results of this study validated the use of B. cuneata in folk medicine for the treatment of inflammatory diseases".

Taken altogether, beta-Sitosterol may be considered a supplement for the prevention and treatment of bacterial infectious diseases, pending to the confirmation of the larger sample size and multicenter human study.

Intake of beta-Sitosterol in the form of supplements should be taken with extreme care to prevent overdose acute liver toxicity.


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Author Biography
Kyle J. Norton (Scholar, Master of Nutrition, All right reserved)
Health article writer and researcher; Over 10.000 articles and research papers have been written and published online, including worldwide health, ezine articles, article base, health blogs, self-growth, best before it's news, the karate GB daily, etc.,.
Named TOP 50 MEDICAL ESSAYS FOR ARTISTS & AUTHORS TO READ by Disilgold.com Named 50 of the best health Tweeters Canada - Huffington Post
Nominated for shorty award over last 4 years
Some articles have been used as references in medical research, such as international journal Pharma and Bioscience, ISSN 0975-6299.

Sources
(1) Anti-inflammatory and antihistaminic activity of triterpenoids isolated from Bursera cuneata (Schldl.) Engl by Figueroa-Suárez MZ1, González Christen J2, Cardoso-Taketa AT3, Gutiérrez Villafuerte MDC4, Rodríguez-López V. (PubMed)
(2) Antihistaminic and antiallergic actions of extracts of Solanum nigrum berries: possible role in the treatment of asthma by Nirmal SA1, Patel AP, Bhawar SB, Pattan SR. (PubMed)
(3) The Effects of Hormone Histamine (3) by Kyle J. Norton

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