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Natural Product Compounds from Plants in Neurodegenerative Diseases
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Priya Darshani, Md TanjimAlam, Prem P. Tripathi, V.S. Pragadheesh
Vinpocetine, a semi-synthetic chemical derived from the vincamine, present in the leaves of Vinca minor L., is used for the treatment of dementia and mental impairment. Vinpocetine is sold as a drug in Europe named Cavinton, whereas, in the United States, it is sold as a dietary supplement to treat memory loss. Vinpocetine has been reported to enhance neurotransmitter production in the brain and improve cerebral metabolism by enhancing the glucose and oxygen consumption in the brain and elevating cerebral cAMP and ATP levels. It has been shown to ameliorate microcirculation and cerebral blood flow by inhibiting platelet aggregation. Vinpocetine has been evaluated in several double-blind clinical trials that demonstrated its significant benefits in patients of AD (Szatmari and Whitehouse, 2003; Balestreri et al., 1987).
Vinca rosea (Madagascar Periwinkle) and Adhatoda vesica (Malabar Nut)
Published in Azamal Husen, Herbs, Shrubs, and Trees of Potential Medicinal Benefits, 2022
Rajib Hossain, Md Shahazul Islam, Dipta Dey, Muhammad Torequl Islam
The V. rosea plant is good for the brain. It contains substances that enhance blood flow to the brain and boost the amount of oxygen available to the brain. It also inhibits irregular blood-clotting and increases levels of serotonin. Vincamine is an alkaloid that helps to maintain blood thinness and improves cognitive function. As a result, it is beneficial in the prevention of dementia, particularly vascular dementia. If taken orally, periwinkle can be harmful. Pregnant women should stay away from the plant (Singh et al., 1991, 2017). In folk and traditional medicine, the alkaloids from V. rosea are used to treat a range of non-malignant illnesses; while in Africa, herbal medicine is used to treat menorrhagia and rheumatism (Waltz, 2004). V. rosea has been employed to treat diabetes for many decades, and its hypoglycemic effect has been demonstrated via inducing diabetes in mice (Cuellar and Lorincz, 1975). Because of the rise in hyperglycemia as well as the stimulation of insulin synthesis, it has hypoglycemic properties. (Singh et al., 2001; Kumari and Gupta, 2013).
Catalog of Herbs
Published in James A. Duke, Handbook of Medicinal Herbs, 2018
In old herbáis, periwinkle was used for tumors of the uvula. Reserpine shows anticancer activity in the CA, SA, and WA tumor systems; beta-sitosterol in the CA, LL, and WA systems; ursolic acid in the PS system.10 Acid, astringent, bactericide, carminative, colly-rium, depurative, diuretic, emetic, hemostat, lactagogue, sedative, spasmolytic, and tonic, the periwinkle is used for bleeding, catarrh, diarrhea, dysentery, eczema, fits, hypertension, hysteria, menorrhagia, nervous disorders, phthisis, piles, tumors, and nightmares.32,33 Periwinkle used to be tied around cramped limbs as a remedy. Bruised leaves with lard used for piles. Used homeopathically for hemorrhagia. Flowers said to be purgative when fresh. Bruised leaves are stuffed into the nostrils to stop nose bleed.2 Leaves are a bitter astringent used against dysentery and hemorrhoids.11 Aqueous extracts injected in cats are hypotensive. Given orally, the plant lowers arterial hypertension. Vincamine has a weak antagonistic action on the pressor activity of adrenaline. Infusion of the herb used as a gargle and mouthwash and the extract as a vermifuge.1 The plant is applied to scalp ailments. While the literature available to me suggests that this plant is lactagogue, Parvati suggests its usage to control overabundant milk and to dry up milk when weaning. She recommends it for vaginal hemorrhage, with motherwort for bloated congestion with a late period, and as a douche with chaparral, oatstraw, and slippery elm for trichomoniasis.48
Surface-tailoring of emulsomes for boosting brain delivery of vinpocetine via intranasal route: in vitro optimization and in vivo pharmacokinetic assessment
Published in Drug Delivery, 2022
Hibah M. Aldawsari, Shaimaa M. Badr-Eldin, Nourah Y. Assiri, Nabil A. Alhakamy, Anna Privitera, Filippo Caraci, Giuseppe Caruso
Vinpocetine (VNP; 14-ethoxycarbonyl-(3a,16a-ethyl)-14,15-eburnamine) is a synthetic derivative of vincamine alkaloid used for the management of several CNS disorders including cerebrovascular ischemia, Alzheimer’s disease, and other different types of dementia (Zhang et al., 2018). Unfortunately, VNP is a poorly aqueous soluble active agent that is exposed to dramatic presystemic metabolism, therefore, it possesses an extremely short half-life. These faults could result in reduced bioavailability and diminished brain concentrations restricting its clinical applications (Vyas et al., 2010; Ucisik et al., 2015). It is then highly recommended to develop a drug delivery system able to effectively enhance VNP solubility and promote its brain delivery. Based on the above, this work aimed at developing and optimizing intranasal surface-tailored VNP nanoemulsomes for boosting drug brain levels.
Effect of different doses of borneol on the pharmacokinetics of vinpocetine in rat plasma and brain after intraocular administration
Published in Xenobiotica, 2020
Qun Ma, Manman Dai, Huimin Zhang, Luyu Bai, Ning He
Vinpocetine (VIN), a vincamine derivative, is an extract from the Vinca minor plant and was the first identified nootropic. Vinpocetine exerts several pharmacological and biochemical effects, including neuroprotection effects, the promotion of brain metabolism, and the improvement of brain microcirculation. VIN was first marketed in Hungary, and is mainly administered orally and intravenously for the treatment of ischemic stroke and other cerebrovascular diseases, such as residual cerebral hemorrhage, residual cerebral infarction, and cerebral artery cirrhosis (Bereczki & Fekete, 1999; Lin et al.,2014). However, a previous study clearly showed that its low water solubility (∼5 µg/mL), poor absorption, and first-pass effects resulted in very low oral bioavailability (∼7%) of VIN in humans, which may limit its clinical application (Grandt et al., 1989). Furthermore, VIN has a short elimination half-life (1–2 h) following intravenous administration, resulting in the need to administer frequent doses (three times daily), extensive distribution in the body, and higher drug concentrations in the lung, spleen, liver, and kidney than in the brain (Zhuang et al., 2010). An alternative route of administration may help to overcome these problems.
Optimized preparation of vinpocetine micelles and in vivo evaluation of its pharmacokinetics in rats
Published in Pharmaceutical Development and Technology, 2020
Jiaxin Zhou, Wenfang Zhang, Jiali Pang, Xiaoting Wang, Zijie Zheng, Yuanxin Li, Fan Yang, Wei Yang
Vinpocetine (VP) is a vincamine derivative used for the treatment of disorders arising from cerebrovascular and cerebral degenerative diseases. (Subhan and Hindmarch 1985; Chiu et al. 1988). VP is claimed to increase cerebral metabolism and circulation that the mechanism is mainly associated with the inhibition of phosphodiesterase 1 and vasodilation (Feigin et al. 2001; Patyar et al. 2011). However, VP is a poorly water-soluble base-type drug (pKa = 7.1) its water solubility value is about 5 μg/mL and is characterized by a short half-life time of about 2 h (Polgar et al. 1985; Miskolczi et al. 1990). Due to the poor solubility in aqueous solutions and significant first-pass effect, the oral bioavailability of VP in humans is only 7% that greatly restricted its clinical use (Grandt et al. 1989; Szakacs et al. 2001). Therefore, a kind of controlled release dosage form for parenteral administration is preferred because it may possibly promote the bioavailability of VP.