Due to its numerous health advantages, bitter orange, also known as Citrus aurantium in science, has long been utilized as a dietary supplement. Bitter orange, which has its roots in Southeast Asia, has been grown around the world, notably in the Americas and the Mediterranean region. This fruit is frequently used as a substitute for ephedra, which is outlawed in the US due to its connection to a number of health hazards.
Numerous bioactive substances, most notably synephrine in bitter orange and in charge of many of its physiological effects, are present in bitter orange. The nature of bitter orange, its health advantages, the best dosage, its adverse effects, potential drug interactions, and safe use will all be covered in this article.
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Bitter Orange: Benefits, Dosage, Side Effects, Drug Interactions, and Other Important Information is an original (NootropicsPlanet) article.
Nature of Bitter Orange
Bitter orange is a little, evergreen tree with fragrant white blossoms and dark green leaves. The fruit is tiny, rounded, and has a thick, abrasive peel. Alkaloids, volatile oils, flavonoids, and other bioactive substances can all be found in bitter orange. Synephrine, an alkaloid with a structure resembling ephedrine, is the main active ingredient contributing to bitter orange’s health advantages.
Health Benefits of Bitter Orange
Weight Control
The main active ingredient in bitter oranges, synephrine, stimulates adrenergic receptors, especially the 3-adrenergic receptor, by acting as a sympathomimetic agent. The process of breaking down fat cells, known as lipolysis, depends heavily on this receptor. Synephrine enhances the rate of lipolysis by activating these receptors, which might increase energy expenditure and weight reduction.
Numerous clinical studies have shown that supplementing with bitter orange extract or synephrine may help with weight loss and enhance body composition. Bitter orange extract increased weight reduction statistically significantly compared to placebo, according to a meta-analysis by Stohs et al. (2012), whether alone or in combination with other components.
Improved Sports Performance
Due to its stimulating qualities, bitter orange extract has been utilized by athletes to improve their performance. Norepinephrine is a neurotransmitter that raises alertness, attention, and energy, and it has been discovered that synephrine boosts its secretion. Improvements in exercise performance, particularly in terms of power output and endurance, may result from this enhanced norepinephrine release.
Bitter orange extract supplementation was found to increase anaerobic power production in resistance-trained male athletes in research by Ratamess et al. (2016). The study authors hypothesized that athletes engaged in high-intensity, brief-duration sports could benefit from acute administration of bitter orange extract.
Properties that Reduce Inflammation and Free Radicals
Flavonoids, which have strong antioxidant and anti-inflammatory properties, are abundant in bitter orange. By scavenging free radicals, certain flavonoids, like hesperidin and naringin, might lessen oxidative stress and inflammation. As a result, bitter orange extract may aid in preventing chronic diseases like cancer and cardiovascular disease linked to oxidative stress and inflammation.
Chemistry of Bitter Orange
Alkaloids, flavonoids, volatile oils, and other bioactive substances can all be found in bitter orange. Synephrine, which comes in three stereoisomers (p-, m-, and o-synephrine), is the most significant alkaloid in bitter orange. The bitter orange primarily contains the biologically active isomer of synephrine, which has strong sympathomimetic properties. Octopamine, tyramine, and N-methyltyramine are other alkaloids found in bitter orange.
Hesperidin and naringin are flavonoids in bitter oranges with potent anti-inflammatory and antioxidant activities. The peel and the pulp contain these substances, giving the fruit its distinctive bitter flavor. In addition to others, limonene, myrcene, and linalool are among the volatile oils principally found in the peel. These oils perhaps possess antibacterial qualities in addition to adding to the fruit’s aromatic scent.
Physiological Mechanisms of Action
Bitter orange extract, especially synephrine, works by stimulating adrenergic receptors. These receptors are located in the sympathetic nervous system, which controls the “fight or flight” reaction. Synephrine stimulates these receptors and causes various physiological changes, such as elevated heart rate, blood pressure, and energy expenditure.
Activation of the 3-adrenergic Receptor
The primary target of synephrine is the 3-adrenergic receptor, found in adipose tissue and essential for the breakdown of fat cells (lipolysis). Synephrine stimulates a signaling cascade that synthesizes cyclic AMP (cAMP) and activates protein kinase A (PKA) when it binds to the 3-adrenergic receptor. Hormone-sensitive lipase (HSL), which converts triglycerides stored in fat cells into free fatty acids and glycerol, is then activated as a result. The body can then utilize these compounds to produce energy, leading to an increase in energy use and weight loss.
Synephrine Also Increases Norepinephrine Release
Norepinephrine is a neurotransmitter that controls alertness, focus, and energy levels. Bitter orange extract can enhance exercise performance by raising norepinephrine levels, especially in terms of power production and endurance.
Mechanisms Controlling Inflammation and Antioxidants
Hesperidin and naringin, two flavonoids found in bitter orange, work to reduce pro-inflammatory signaling pathways and scavenge reactive oxygen species (ROS) to provide their antioxidant and anti-inflammatory properties. This can aid in preventing cellular damage and inflammation, which are linked to the emergence of a number of chronic illnesses, including cancer and cardiovascular disease.
By knowing the chemistry and physiological mechanisms of action of bitter orange, researchers and healthcare practitioners can more accurately evaluate its possible advantages and hazards and create valuable suggestions for its usage as a nutritional supplement.
Optimal Dosage of Bitter Orange
The ideal synephrine or bitter orange extract dosage varies according to the person’s age, weight, and intended health advantages. Synephrine has been demonstrated to be beneficial for weight management at 10-53 mg daily doses. Acute intake of 100–200 mg of bitter orange extract before exercise may enhance athletic performance. However, seeking medical advice before beginning any supplementation regimen is crucial to determine the correct dosage for each person’s needs and prevent potential side effects.
Side Effects of Bitter Orange
While moderate bitter orange consumption is generally considered safe, excessive consumption can have adverse effects. Among the side effects that have been mentioned are:
Cardiovascular Result
As a stimulant, synephrine can raise blood pressure and heart rate. Particularly in people with pre-existing cardiovascular diseases or those who are sensitive to stimulants, this might occasionally result in major cardiovascular events like myocardial infarction, stroke, or even sudden death.
Effects on the Digestive System
High doses of synephrine or bitter orange extract may cause nausea, vomiting, and abdominal pain in addition to other gastrointestinal symptoms. When bitter orange is ingested on an empty stomach, these negative effects are more likely to manifest.
Neurological Effects
Bitter orange’s stimulant qualities can result in nervous system adverse effects such as anxiety, jitteriness, and insomnia, particularly when taken in high quantities or in combination with other stimulants.
Potential Substance Interactions with Bitter Orange
Bitter oranges can have negative interactions with several drugs and other substances. These interactions include, among others:
MAOIs are monoamine oxidase inhibitors.
Antidepressant drugs in the MAOI class may interact with synephrine, raising blood pressure to potentially hazardous levels. A hypertensive crisis, a potentially fatal illness, can result from this combination and must be treated right away.
Drugs that are stimulating
As both bitter orange and other stimulant drugs like amphetamines or methylphenidate can raise blood pressure and heart rate, taking them together increases the risk of cardiovascular side effects.
Caffeine.
Bitter oranges can interact with caffeine, a popular element in many supplements for weight reduction and athletic performance, resulting in additive stimulant effects and a higher risk of negative effects.
Responsible Use of Bitter Orange
Take into account the following recommendations to ensure the best and safest usage of bitter oranges as a nutritional supplement:
Speak with a healthcare provider.
Before beginning any supplement routine, speak with a healthcare expert to ascertain whether bitter orange suits your particular needs and to find the best dosage.
Select a Reputable Brand
Choose a bitter orange supplement from a reputed manufacturer to ensure the product has the correct quantity of active ingredients and is free of contaminants.
Observe any side effects
Be aware of any potential side effects when using bitter orange, and stop using it immediately if it materializes.
Keeping Other Stimulants Separate
Avoid combining bitter oranges with other stimulants, like caffeine or stimulant drugs, to reduce the chance of unwanted effects.
Bitter Orange:
Conclusion
Bitter orange has traditionally been used in various cultures for culinary and medicinal purposes. It’s important to note that while bitter orange has potential health benefits, it also contains synephrine, which is structurally similar to ephedrine. Ephedrine, a compound found in some weight loss supplements, has been associated with cardiovascular and other adverse effects.
As a result, the use of bitter orange, particularly in supplement form, should be approached with caution, and individuals with pre-existing health conditions should consult with a healthcare professional before using it. Always keep in mind that individual responses to supplements can vary, and it’s crucial to prioritize a balanced diet, regular exercise, and overall healthy lifestyle practices for well-being. If you are considering using bitter orange supplements, consult a healthcare professional to ensure they are safe and suitable for your specific health circumstances.
References:
- Bitter Orange: An Overview of its Potential Health Benefits and Side Effects. Retrieved from: https://www.webmd.com/vitamins/ai/ingredientmono-976/bitter-orange
- Bitter Orange Extract and Synephrine Effects on Metabolic Rate and Body Composition. Retrieved from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3444973/
- The Effects of Bitter Orange Extract on Exercise Performance. Retrieved from: https://journals.lww.com/nsca-jscr/Fulltext/2016/03000/Acute_Effects_of_a_Multi_Ingredient.9.aspx
Important Note: The information contained in this article is for general informational purposes only, and should not be construed as health or medical advice, nor is it intended to diagnose, prevent, treat, or cure any disease or health condition. Before embarking on any diet, fitness regimen, or program of nutritional supplementation, it is advisable to consult your healthcare professional in order to determine its safety and probable efficacy in terms of your individual state of health.
Regarding Nutritional Supplements Or Other Non-Prescription Health Products: If any nutritional supplements or other non-prescription health products are mentioned in the foregoing article, any claims or statements made about them have not been evaluated by the U.S. Food and Drug Administration, and such nutritional supplements or other health products are not intended to diagnose, treat, cure, or prevent any disease.
