Ephedrine

Posted on September 16, 2024 by Robert Barrington

Ephedrine is an alkaloid that is found in the Ephedra sinica plant. Ephedrine is a stimulant of the central nervous system and can activate the sympathetic nervous system. Ephedrine is of interest nutritionally because it also has thermogenic effects in humans, and this means it has fat loss properties. The thermogenic effects of ephedrine have shown that it can increase energy expenditure in humans because it stimulates the release of adrenaline and noradrenaline which can then activate adrenergic receptors. Ephedrine and the concomitantly released adrenaline can stimulate the cardiovascular system through the α-1, α-2, and β-1 adrenergic receptors. However, thermogenic effects from ephedrine likely stem from its ability to stimulate the β-3, β-1and β-2 adrenergic receptors in brown and white adipose tissue, and the downstream effect of this is to cause an increase in cellular liposisis. Ephedrine may also decrease the activity of the monoamine oxidase enzyme system that can potentiate the effects of adrenaline and noradrenaline in the brain providing a more prolonged rise in brain levels of catecholamines.   

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Stohs, S. J. and Badmaev, V. 2016. A review of natural stimulant and non‐stimulant thermogenic agents. Phytotherapy Research. 30(5): 732-740
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Synephrine Versus Ephedrine

Posted on September 13, 2024 by Robert Barrington

Synephrine is the name of a chemical compound found in the peel of the unripe Citrus aurantium fruit. The form of synephrine in Citrus aurantium is p-synephrine. Synephrine is sold as a weight loss supplement on account of its ability to activate adrenergic receptors, some of which might be involved in accelerating fat oxidation rates in cells. Synephrine is often compared to ephedrine (an alkaloid from the Ephedra sinica plant), a known central nervous system stimulant that has been shown to have significant benefits at causing weight loss in humans and animals. Pharmacologically, p-Synephrine, does not have a high affinity for the α-1 and α-2 adrenergic receptors, and nor does it have a high affinity for the β-1 and β-2 adrenergic receptors. This explains the lack of cardiovascular effects in p-synephrine. However, p-synephrine may activate the β-3 adrenergic receptors, which are involved in the upregulation of lipolysis in brown and white adipose tissue. The pharmacology of p-synephrine appears to be related to its hydroxyl group that is present on the para-position of the phenol ring. Further studies suggest that noradrenaline and adrenaline levels are not increased through normal use of p-synephrine. In contrast to p-synephrine, m-synephrine (phenylephrine) possesses a hydroxyl group in the meta-position of the phenol ring. Commercially available m-synephrine is synthesised artificially and is not present in citrus fruit. Ephedrine acts on α-1, β-1, and β-2 adrenergic receptors to produce cardiovascular effects, while interacting with β-3 adrenergic receptors to promote thermogenesis. Phenylephrine (m-synephrine) exerts cardiovascular effects similar to ephedrine as well as bronchodilation suggesting its receptor binding is more similar to ephedrine than to  p-synephrine. 

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Stohs, S. J., Shara, M. and Ray, S. D. 2020. p‐Synephrine, ephedrine, p‐octopamine and m‐synephrine: Comparative mechanistic, physiological and pharmacological properties. Phytotherapy Research. 34(8): 1838-1846
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Synephrine and Raspberry Ketone: Why No Central Effects?

Posted on September 12, 2024 by Robert Barrington

Synephrine and raspberry ketone are structurally similar compounds found in Citrus Aurantium peel and Rubus Idaeus, respectively. Both compounds have a pharmacological profile that suggests that they cause lipolysis through activation of β3 adrenergic receptors. There is also likely some general adrenergic stimulation caused by affinity for other adrenergic receptors, and the exact pharmacology will depend on the compound of interest, with synephrine being composed of a number of structural isomers that differ slightly in their affinities for receptors. Further, capsaicin from the Capsiucum chili pepper also may have similar activity as it is structurally related to both synephrine and raspberry ketone. The basic structure of synephrine and raspberry ketones is that of a phenol ring with a side chain containing nitrogen. In this regard the structures are similar to central nervous stimulants including amphetamine and ephedrine. However, synephrine and raspberry ketones do not stimulate the central nervous system and this likely relates to their inability to cross the blood brain barrier. This may be because the hydroxyl group on the phenol ring in position 3 and 4 inhibits this activity. As amphetamine and ephedrine are not hydroxylated in either position 3 or 4 of the phenol ring, they can cross the blood brain barrier and provide significant stimulatory effects on the consumer. 

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Rossato, L. G., Costa, V. M., Limberger, R. P., de Lourdes Bastos, M. and Remião, F. 2011. Synephrine: from trace concentrations to massive consumption in weight-loss. Food and Chemical Toxicology. 49(1): 8-16
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Synephrine

Posted on September 11, 2024 by Robert Barrington

Synephrine is the active component in citrus aurantium, a tree that belongs to the Rutacaea family of plants. Common names for Citrus aurantium include bitter orange, seville orange, sour orange, green orange, zhi shi and kijitsu. Other species of citrus also contain synephrine. The unripe fruits contain high amounts of synephrine in their peels. Synephrine is present as a number of similar chemicals m-synephrine and p-synephrine. Chemically, synephrine has an aromatic ring with an ethylamine substituted side chain. These chemicals have their biological effects because they activate noradrenaline receptors. This explains the ability of synephrine to cause weight loss through its ability to activate noradrenaline receptors which in turn increase lipolysis. This ability to stimulate noradrenaline receptors is quite broad and there is no specific receptor subtype that is targeted. In animal models, synephrine shows anti-depressant effects which is consistent with noradrenaline stimulation. Animal studies also show that synephrine can activate serotonergic receptors, which may also confer anti-depressant effects. 

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Rossato, L. G., Costa, V. M., Limberger, R. P., de Lourdes Bastos, M. and Remião, F. 2011. Synephrine: from trace concentrations to massive consumption in weight-loss. Food and chemical toxicology. 49(1): 8-16
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Raspberry Ketone: Effects

Posted on September 10, 2024 by Robert Barrington

Raspberry ketone is an aromatic phenolic group of compounds that is chemically called  4-(4-hydroxyphenyl) butan-2-one). Although named because it occurs in the raspberry plants (Rubus idaeus), raspberry ketone is also found in other plants including kiwifruit, peaches, and apples. A number of health effects for raspberry ketones have been described including hepatic protection, cardiovascular benefits, gastric protection, anti-hyperlipidemic effects, anti-obesity activity, anti-inflammatory effect and depigmentation effects, and it may also play a role in sexual maturation. Studies show that raspberry ketones are absorbed in animals and excretion from the blood takes around 24 hours. Excretion of raspberry ketones include methylation and conversion to raspberry alcohol. Raspberry ketone may stimulate the metabolism of white and brown adipose tissues because it is able to activate norepinephrine-induced lipolysis. Raspberry ketone may also inhibit the absorption of lipids in the small intestine, and this may reduce energy intake. The antioxidant and anti-inflammatory effects of raspberry ketone may explain many of the general health effects of the compound. Specific effects, including the stimulation of lipolysis may require receptor activation. 

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Rao, S., Kurakula, M., Mamidipalli, N., Tiyyagura, P., Patel, B. and Manne, R. 2021. Pharmacological Exploration of Phenolic Compound: Raspberry Ketone—Update 2020. Plants. 10(7)
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Testosterone: Production and Release

Posted on September 9, 2024 by Robert Barrington

Maintaining optimal testosterone (17b-hydroxy-4-androstene-3-one) levels is not only important as a means of maintaining adequate muscle mass, but is also related to health and well being. This is true for both men and women, although the levels of testosterone in women are much lower (testosterone levels are about 10 times higher in men compared to women). Testosterone is synthesised in the leydig cells of the testes from cholesterol and the pathway passes through a number of intermediate stages that includes progesterone, dehydroepiandrosterone (DHEA) and androstenedione. In women testosterone is produced in the ovaries and the zona reticularis of the adrenal glands and this occurs because testosterone is involved in the synthesis of other chemicals such as estradiol, cortisol and aldosterone, and the excess then spills over into the blood for metabolic purposes. Because women and young boys do not have functioning leydig cells capable of synthesising testosterone, there is no significant increase in testosterone in response to exercise as is seen in men. In men, intense exercise, particularly resistance training, significantly increases circulating levels of testosterone. 

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Vingren, J. L., Kraemer, W. J., Ratamess, N. A., Anderson, J. M., Volek, J. S. and Maresh, C. M. 2010. Testosterone physiology in resistance exercise and training. Sports Medicine. 40(12): 1037-1053
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Clove (Syzygium aromaticum)

Posted on September 6, 2024 by Robert Barrington

Clove (Syzygium aromaticum) is a spice that has traditionally been used as a food preservative and flavouring agent. Cloves grow as a tree, and the flow buds are collected and dried, and it is this part of the tree that is used as a spice. Clove originated in Indonesia, but commercial demand for clove has resulted in a much wider distribution of the plant. The plant has medicinal properties on account of its very high polyphenol content, something that confers significant antioxidant potential to the consumer. Polyphenols contained within cloves include eugenol, eugenol acetate and gallic acid, with eugenol being the main bioactive compound. Clove is rich in phytochemicals groups including flavonoids, hydroxybenzoic acids, hydroxycinnamic acids and hydroxyphenyl propens. As with many spices, the antioxidant content of clove is higher than most fruits and vegetables yet at the same time it is low in energy. The flavour of clove in combination with its antioxidant capacity and low energy content makes it ideal to add to other foods in order to increase the nutritional value.  

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Cortés-Rojas, D. F., de Souza, C. R. F. and Oliveira, W. P. 2014. Clove (Syzygium aromaticum): a precious spice. Asian Pacific Journal of Tropical Biomedicine. 4(2): 90
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Bergamot Polyphenols for Metabolic Syndrome

Posted on September 5, 2024 by Robert Barrington

Bergamot (Citrus bergamia) is a plant that produces the bergamot orange. From bergamot oranges bergamot is produced from the rind of the oranges and is used in food manufacture as a spice, such as in the case of Earl Grey tea. The bergamot tree grows naturally in Calabria in Southern Italy. The Essence from bergamot has been used as a pain relieving substance and as a fragrance. In the local economy where it is grown, bergamot plays an important role and it is processed to extract its essential oil. Like all plants bergamot contains a high number of phytochemicals and in particular is rich in polyphenols including flavonoids and their glycosides. The flavonoids in bergamot include neoeriocitrin, neohesperidin, naringin, rutin and poncirin. 

Flavonoids are antioxidants and in this role they may benefit human health because they are bioavailable and accumulate in tissues including the blood, albeit in a metabolised form. One role that bergamot may play is in normalising levels of blood lipids, which can become elevated during development of the metabolic syndrome. The reason that bergamot polyphenols may be beneficial to metabolic syndrome is because metabolic syndrome is caused by inflammation in the liver that is a direct result of poor quality food. The damage from metabolic syndrome, which includes modifications of metabolic pathways, is caused by oxidative stress. The polyphenols in bergamot may prevent this oxidative stress and therefore may delay or prevent the development of the damaging metabolic changes.  

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Carresi, C., Gliozzi, M., Musolino, V., Scicchitano, M., Scarano, F., Bosco, F., Nucera, S., Maiuolo, J., Macrì, R., Ruga, S., Oppedisano, F., Zito, M. C., Guarnieri, L., Mollace, R., Tavernese, A., Palma, E., Bombardelli, E., Fini, M., Mollace, V. 2020. The Effect of Natural Antioxidants in the Development of Metabolic Syndrome: Focus on Bergamot Polyphenolic Fraction. Nutrients. 12: 1504
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Bergamot and Earl Grey Tea

Posted on September 4, 2024 by Robert Barrington

The bergamot orange (Citrus bergamia) is a citrus fruit that is used in aromatherapy as an anxiolytic and calmative agent. The rind of the orange is used to produce bergamot tea, which is black tea with added bergamot. Bergamot has a number of pharmacological effects and in this regard, bergamot is useful in the treatment of anxiety disorders. Bergamot has central nervous system effects that allow it to interact with neurones in the brain and this may be how it exerts its effects on mood. Bergamot may influence neurotransmitter function in the hippocampus and may alter synaptic plasticity. These effects may cause neural protection although the mechanisms are not fully clear. It is thought that the pharmacological effects of bergamot come from the essential oil of the plant. The essential oil is rich in a number of phytochemicals including the monoterpene hydrocarbons limonene gamma-terpinene beta-pinene, the monoterpene alcohol linalool, as well as the monoterpene ester linalyl acetate. The non-volatile part of the oil contains waxes and flavones as well as the potentially toxic bergapten. 

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Bagetta, G., Morrone, L. A., Rombolà, L., & Amantea, D. 2010. Neuropharmacology of the essential oil of bergamot. Fitoterapia. 81: 453-461
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Peppermint Tea (Mentha piperita)

Posted on September 3, 2024 by Robert Barrington

Peppermint tea (Mentha piperita) is the most commonly drunk herbal tea, if you exclude true tea which comes from the Camellia sinensis plant. Peppermint tea is rich in phytochemical nutrients that have been shown to be bioavailable in humans. For example, the leaves of peppermint contain rosmarinic acid, a polyphenol that may have antioxidant effects in humans and animals. The leaves also contain flavonoids, which include particularly eriocitrin, luteolin and hesperidin, all of which have been researched in humans and animals for their health effects, something that likely stems from their antioxidant and anti-inflammatory potential. Peppermint is perhaps best known for its calming effect on digestion, something that results from its ability to cause the relaxation of smooth muscle. This relaxing effect may come from the essential oils that are contained within peppermint. In the gastrointestinal tract, peppermint tea may also have antibacterial activity and may reduce food intolerances, perhaps because of its ability to improve digestion. Because peppermint does not contain caffeine, it is also suitable as a tea for hydrating, and in this regard can be drunk into the evening and prior to bed, as it may aid sleep due to its relaxing properties on smooth muscle. 

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McKay, D. L., & Blumberg, J. B. 2006. A review of the bioactivity and potential health benefits of peppermint tea (Mentha piperita L.). Phytotherapy Research: An International Journal Devoted to Pharmacological and Toxicological Evaluation of Natural Product Derivatives. 20(8): 619-63
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