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Rauwolfia extract is obtained from the bark of the Rauwolfia Serpentina plant and has been used for centuries as herbal medicine in Ayurveda therapy. The plant originates from India and Sri Lanka and is widely used for the treatment of hypertension and insomnia. It contains a variety of active alkaloids that have psychoactive properties. Today, there are several types of rauwolfia extract available on the market. They include the following:
Standardized Extracts
These extracts are specifically standardized to contain a fixed and specific concentration of the active alkaloids such as reserpine, ajmaline, and yohimbine. This was mainly done for the consumers' convenience and to ensure consistent dosage for certain therapeutic effects such as hypertension and insomnia. Thus, available products often be labeled with the percentage of these alkaloids present in them.
Whole Plant Extracts
Some products use the whole Rauwolfia Serpentina plant rather than just the bark. These extracts contain all the plant's alkaloids and can be compounds, unlike the others, which are derived solely from the reserpine. Whole plant extracts are often marketed as more natural or holistic because they are not concentrated or isolated.
Bark Powder
This is the most basic form of extracted Rauwolfia Serpentina. It involves drying and grinding the bark into powder. Though not highly concentrated, this raw powder contains all the alkaloids and other beneficial compounds within the bark. Some users prefer bark powder because it is minimally processed and the way they feel is more natural.
Water-Soluble Extracts
These are specially formulated Rauwolfia extracts meant for easy use in water-based solutions like teas or herbal syrups. These extracts are often used in traditional medicine due to their ease of preparation and consumption. However, water-soluble extraction may not totally capture all the alkaloids in the extraction process, thus possibly reducing the extract's potency.
Capsules and Tablets
To make consumption easy and more accessible, extract of Rauwolfia is often available in capsule or tablet form. These formats provide an easy way to incorporate the extract into a daily routine; they are often mixed with other herbs for synergistic effects or other health benefits related to hypertension and insomnia.
Tinctures and Liquid Extracts
Liquids or tinctures are extracts that are prepared by soaking the bark in alcohol or glycerin solution to extract the active compounds. These tinctures are potent and easy to take and absorb faster than capsules or powder for quick treatment of health issues like high blood pressure and psychological disorders.
Rauwolfia extracts are derived solely from the Rauwlfia Serpentina plant. The extracts are taken from the bark of the Rauwolfia Serpentina tree. It's important to note that the alkaloids found in the extracts are not derived from other plants. However, in some cases, when the extracted alkaloids are isolated and standardized for higher concentration, artificial reserpine is synthesized in the laboratory using the following:
Plant-Based Precursors
Once the extraction and isolation of alkaloids are done, the reserpine can be artificially synthesized with chemicals like succinic anhydride, α-methyltyramine, and 3,4-dimethoxytam. Once these ingredients are put together through a series of chemical reactions, they result in a compound with a similar molecular structure to reserpine found in the tree's bark. Since reserpine contains several methoxy groups that are critical in the process of synthesizing reserpine, succinic anhydride and catechol are used to shield them during the reaction in order to make a precursor compound known as 3,4-Dimethoxy-N-(beta-hydroxyethyl) benzene propenyl amine.
Simultaneous Ring Closing and Opening
Once the methoxy groups have been protected, the reaction mixture is treated with lithium diisopropyl amide (LDA) and other electrophiles in order to create a new carbon-carbon bond. At this stage, an indole ring may potentially form. However, because the preceding step involved other electrophiles with a high potential to react, there is a possibility that one of the reaction products will eliminate the methoxy groups that had just been added.
N-Boc Protection of the Amino Group
In a situation where LDA also has the potential to react with the amine group and eliminate it, a protecting group is introduced into the reaction. During this stage, N-Boc will be introduced into the reaction so as to ensure that the amino group does not participate in any reaction processes that may lead to its elimination. It is important to note that the N-Boc protection is temporary and will eventually undergo hydrolysis in the last steps of the synthesis of the product in order to free the amine functional group.
Synthesis of Spirocyclic Intermediates
Spiro ring systems play a fundamental role in the process of drug design and identification, especially for a certain class of alkaloids. Therefore, during the course of synthesizing reserpine, a few reaction conditions will be done to form these spirocycles, which will then drive the product structure closer to the desired compound.
Rauwolfia extracts have notable commercial value and applications in various sectors. The following are the commercial value and uses of Rauwolfia extracts:
Pharmaceutical Industry
The purest extracts are important for the pharmaceutical industry due to their Rauwolfia Serpentina high-value application in the formulation of antihypertensive drugs and psychotropic medications for treating mental disorders such as schizophrenia. Due to its high medicinal application, reserpine was widely used as the principal component of antihypertensive drugs until the 1970s.
Today, due to the advancement of technology, the market for reserpine is spending less on hypertension management, but there are still people who depend on it to control their blood pressure. Aside from its application in blood pressure control and mental illness treatment, it also has analgesic and sedative properties, increasing its market potential.
Report from Statista indicates that prescription drugs generated revenue of approximately 440 billion U.S. dollars in 2021 and that forecasted market size is expected to reach 236 billion U.S. dollars by 2026.
Health and Wellness Products
Modern consumers increasingly prefer natural and botanical ingredients to conventional pharmaceuticals. Therefore, extracts of Rauwolfia Serpentina are usually used in dietary supplements intended to support cardiovascular health, manage stress, and enhance sleep quality. Because of this, the global dietary supplements market is anticipated to grow at a compound annual growth rate (CAGR) of 8% between 2023 and 2028 and a value of 69 billion U.S. dollars by 2028.
Traditional and Alternative Medicine
Market for Rauwolfia extracts in traditional and alternative medicine, particularly in Ayurveda and herbal medicine, is expanding. In India and Southeast Asian countries, the extracts are commonly used to treat hypertension, insomnia, and mental disorders. Due to the increasing acceptance of traditional medicine over synthetic medicine, the extract market is likely to grow significantly, especially in countries that highly consider herbal remedies.
Cosmetics and Personal Care Products
Ajmaline and other alkaloids found in Rauwolfia extracts are sometimes used in hair care products due to their purported ability to stimulate hair growth and reduce dandruff. This made the extract provide a niche market within the cosmetic industry, particularly in natural and organic hair care formulations.
Export and Economic Impact
The extract market can significantly benefit countries where Rauwolfia Serpentina grows abundantly as a cash crop. Thus, this plant will contribute to the economy through export revenues and provide livelihoods to smallholder farmers engaged in the cultivation and harvesting of the raw materials for the extract.
Research and Development
The demand for Rauwolfia Serpentina extracts increases interest in its pharmacological properties. This also offers opportunities for research and development in the field of medicinal chemistry and drug discovery. For instance, isolating and characterizing new alkaloids can contribute to the development of innovative treatments for hypertension and mental health diseases.
The price of rauwolfia extract varies depending on several factors. Below are some of the factors that influence the pricing of rauwolfia extracts:
Purity and Concentration
This is because the extraction method used during the extraction process determines the alkaloid concentration. Extracts with higher concentrations of active alkaloids, such as reserpine, usually cost more due to their potency and energy-seeking ability. The reason why researchers prefer High-performance liquid chromatography (HPLC) as an extraction method is that it creates highly concentrated extracts of Rauwolfia Serpentina that are pure and potent. It also costs more to obtain raw materials without contamination.
Quality of Raw Material
Rauwolfia extract prices may differ depending on the quality of the raw materials. Extracts sourced from mature Namon plants with optimal alkaloid concentrations will have higher medicinal value and potency than those harvested early or improperly. The practices of the farmers who cultivated their Rauwolfia Serpentina plants also have a substantial impact on the quality of the extracts. Extract prices obtained from plants grown under organic farming conditions also stand at a higher price than those using chemical fertilizers and pesticides. Reason being that organic extracts are more hygienic and have few or no chemical traces that would otherwise spoil their quality.
Extraction and Processing Methods
The extraction method will strongly influence the price since some methods are more sophisticated than others. Tinctures prepared using HPLC and other advanced technologies seem to be more expensive than those prepared using traditional methods like boiling and soaking in alcohol. Also, the purification and standardization processes are cost-intensive, affecting the final product price. Buyers should consider the method used when buying the extract so they can get effective extraction.
Market Demand and Supply
The demand for extracts of Rauwolfia Serpentina significantly impacts its price. Higher demand for extracts in pharmaceutical applications means higher prices, particularly in markets where natural remedies outcompete modern medicine, such as Southeast Asia. Likewise, limited supply resulting from poor harvest, climatic conditions, or decreased availability of raw materials causes fluctuations in extract prices.
Formulation and Packaging
The type of product buyers choose affects the price. For instance, rauwolfia extracts in tinctures, syrups, and capsules are usually more expensive than simple powdered bark due to sophisticated extraction and processing methods. Also, the packaging used in the extract affects the price. Packaging like amber glass bottles for liquid extracts offers a higher financial safety margin for the extracts from light atrophying and tampering than plastic. All these formulations and packaging increase the extract prices.
Rauwolfia extracts have several health benefits, making them highly sought after in the health and wellness industry. Below are some of the benefits of Rauwolfia extracts:
Hypertension Management
Rauwolfia was largely used as a traditional medicine before the advent of contemporary medicine. It is widely regarded as one of the first antihypertensive agents in modern medicine. The reason it works the way it does is because it contains reserpine, an alkaloid that acts primarily on adrenergic receptors in a highly specific manner. by displacing norepinephrine from vesicles, which is then released into the synaptic cleft where it interacts with adrenergic receptors.
This ultimately results in generalized vasodilation and decreased peripheral vascular resistance, which translates to low blood pressure. Additionally, reserpine has the ability to inhibit the uptake of serotonin into vesicles, leading to its accumulation in the synaptic cleft, where it interacts with receptors to promote its inherent effects such as decreasing heart rate and lowering blood pressure.The mechanism of action has been proven effective through several clinical trials that support its use in hypertension.
Insomnia and Sleep Disorders
Rauwolfia extracts have a long-standing application in promoting good sleep and treating insomnia. For instance, an alkaloid called reserpine possesses sedative properties, helping calm the nervous system and facilitating better sleep.
It does this by increasing the availability of neurotransmitters such as serotonin. Serotonin is primarily released into the synaptic cleft, where it interacts with specific receptors to promote its functions, such as vasodilation and decreased neuronal excitability. That way, users derive better sleep quality as well as reduced insomnia symptoms who use the extract.
Mental Health Support
The extract is used to treat various mental health conditions and illnesses, such as schizophrenia. Ajmaline and other alkaloids have psychoactive properties, thus accounting for their use in the therapy of psychiatric disorders.
For example, reserpine was used in the treatment of schizophrenia and other psychotic disorders in the past. But today, other more effective drugs have been discovered, although it is still used to treat these conditions.
Cardiovascular Benefits
Rauwolfia extract can help improve heart health due to its vasodilatory properties that promote blood circulation. Also, the decrease in blood pressure enables better blood flow to vital organs, enhancing heart efficiency and health.
Traditional Uses
In Ayurvedic and traditional medicine, after considering its modern uses, they also used Rauwolfia extracts for other purposes. For instance, they treat headaches, insomnia, and fever and use them as a purgative. Due to the presence of yohimbine, the extracts were also purported to enhance libido and treat erectile dysfunction.
A1. Rauwolfia Retragenois is known as a source of psychoactive alkaloids, especially reserpine. It has been a long-standing application in hypertension management and mental health treatment, such as schizophrenia. People also use it as a traditional remedy for various ailments, including headaches and insomnia.
A2. Both yes and no. While Rauwolfia is traditionally considered a herbal remedy, modern pharmacology has identified and isolated its components to develop conventional drugs, particularly antihypertensive and antipsychotic drugs. For this reason, it is classified as a medicinal herb and a pharmaceutical drug.
A3. Rauwolfia is a small shrub that can grow 1–3 meters tall. It has slender branches and elongated, oval-shaped leaves. The leaves can grow 15–30 cm in length and 5–10 cm in width. The flowers are small and inconspicuous, typically pale green or white. The plant's most notable feature is its mandala-shaped fruit, which looks like a small berry. The fruit usually ripens red or purplish-black.
A4. Since Rauwolfia extract is standardly harnessed from the Rauwolfia Serpentina plant, the extract is generally safe for users. But only when used moderately. Excessive use can lead to adverse effects like bradycardia, hypotension, sedation, or depression.
