Betulinic acid, a natural PDE inhibitor restores hippocampal cAMP/cGMP and BDNF, improve cerebral blood flow and recover memory deficits in permanent BCCAO induced vascular dementia in rats
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Betulinic acid
Vascular dementia
Betulinic acids are a kind of natural product with anti-HIV-1 virus and anti-tumor activity extractable from a lot of plants. They include betulinic acid,23-hydroxy betulinic acid, betulin, and others. Nowaday a large quantity of betulinic acid derivatives with biological activity has been synthesized by structure modification. In this paper, the research advances in this field are reviewed.
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Betulin
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Vascular dementia
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Vascular dementia
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Betulinic acid
Betulin
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Betulinic acid is found in the several foods and plants, such as sour jujube fruits, papaya, persimmon, betulinic acid exhibits low toxicity and a wide range of anticancer activities. Ferritinophagy and ferroptosis are related to tumor formation and therapeutic effects, both of which are controlled by iron metabolism and inextricably linked. In this study, we discovered that betulinic acid could suppress proliferation and migration of hepatoma cells, raised ROS level and inhibited antioxidation level in cells. Ferrostatin-1 was used to determine the death way of hepatoma cells induced by betulinic acid. Betulinic acid could cause ferritinophagy-related phenomenon in vivo and in vitro, promote ferritinophagy-protiens expressions, induce ferritinophagy to inhibit tumours finally. In vivo studies revealed the low toxicity of betulinic acid in mice, the dose of human was about 10 times that of mice, the using dose of human could also be achievable. These findings illustrate the potential of betulinic acid for treatment of cancer.
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Betulinic acid, a pentacyclic triterpene, is widely distributed throughout the tropics. It possesses several biological properties such as anticancer, anti-inflammatory, antiviral, antiseptic, antimalarial, spermicidal, antimicrobial, antileshmanial, antihelmentic and antifeedent activities. However, betulinic acid was highly regarded for its anticancer and anti-HIV activities. Anticancer role of betulinic acid appeared by inducing apoptosis in cells irrespective of their p53 status. Due to high order safety in betulinic acid, a number of structural modifications carried out to improve its potency and efficacy. The C-1, C-2, C-3, C-4, C-20 and C-28 positions are the diversity centers in betulinic acid, and the derivatives resulted on various structural modifications at these positions screened for their anticancer activity. This review presents the structure activity relationship carried out on C-1, C-2, C-3, C-4, C-20, C-28, A-ring, D-ring and E-ring modified betulinic acid derivatives. We have compiled the most active betulinic acid derivatives along with their activity profile in each series. Structure activity relationship studies revealed that C-28 carboxylic acid was essential for the cytotoxicity. The halo substituent at C-2 position in betulinic acid enhanced the cytotoxicity. Though the relation of the cytotoxicity with the nature of substituents at C-3 position could not be generalized but the ester functionality appeared to be a better substituent for enhancing the cytotoxicity. An interesting observation is that the three rings skeleton (A, B and C rings) had played an important role in eliciting anticancer activity, which could be a new molecular skeleton to design new anticancer drugs.
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Aim:To improve the anti-tumor effects and to screen candidate for anti-tumor agent,30-hydroxy derivatives 6a-e and 7a were obtained from the modification of 23-hydroxy betulinic acid.Methods:After protection of the hydroxyl at C-3 and C-23 and carboxyl at C-28 of 23-hydroxy betulinic acid,the oxidation of compounds 5a-e was processed with m-chloroperoxybenzoic acid in chloroform by refluxing for 6 h.Meanwhile,the anti-tumor activity of the target compounds was tested by MTT.Results:The structures of the target compounds have been confirmed by the analytical and spectral analyses.The results showed that the anti-tumor activity of the target compounds was much potent than that of 23-hydroxy betulinic acid.Conclusion:The derivative of 23-hydroxy betulinic acid(6e) is a promising lead compound as the anti-tumor agent worth further investigation.
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Betulinic acid, a natural product, is an anti-HIV and antitumor agent with novel structure and new mechanism of action. Not only it is found abundantly in the nature, but also its semi-synthesis approach has been successful. Betulinic acid is a perfect lead-compound. A lot of betulinic acid derivatives have been synthesized. The structure-activity relationships of Betulimic acid, The mechanisms and the effects of YK-FH312, RPR103611 and IC9564 derivated from Betulinic acid were reviewed in the paper.
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Betulinic acid, a pentacyclic triterpene, is distributed in a variety of plants, such as birch, eucalyptus and plane trees. It shows a wide spectrum of biological and pharmacological properties, such as anti-inflammatory, antibacterial, antiviral, antidiabetic, antimalarial, anti-HIV and antitumor effects. Among them, the antitumor activity of betulinic acid has been extensively studied. However, obtaining betulinic acid from natural resources can no longer meet the needs of medicine and nutrition, so methods such as chemical synthesis and microbial biotransformation have also been used to prepare betulinic acid. At the same time, with the development of synthetic biology and genetic engineering, and the elucidation of the biosynthetic pathways of terpenoid, the biosynthesis of betulinic acid has also been extensively researched. This article reviews the preparation of betulinic acid and its pharmacological activities, in order to provide a reference for the research and utilization of betulinic acid.
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Background: There is evidence that chronic neuroinflammation is involved in the pathogenesis of neurodegenerative disorders, including Alzheimer’s and Parkinson’s diseases. In this regard, animal models are considered important tools for the study of neuroinflammation associated with these diseases. The injection of lipopolysaccharide (LPS) is the most commonly used approach for inducing neuroinflammation in animal models. However, there are limited and inconsistent studies regarding the effect of the chronic administration of LPS on behavioral parameters. Accordingly, this experimental study aimed to compare the effect of the chronic injection of LPS in two different doses on behavioral alterations, including spatial learning and working memory in mice. Methods: Thirty-six male BALB/c mice were used in this study. After acclimatization for a week, mice were randomly divided into three groups. Control mice were intraperitoneally (IP) injected with saline for seven consecutive days, and mice of the second group received 250 μg/kg LPS (IP) dissolved in saline for a week. Finally, mice of the third group were administered 750 μg/kg LPS (IP) dissolved in saline for a week. Morris water maze (MWM) and Y-maze were performed to assess spatial learning and working memory alterations in treated mice, respectively. Results: It was found that LPS treatment with a high dose (750 μg/kg) results in working memory impairment (P=0.0024) and cognitive dysfunction (P=0.0030) based on Y-maze and MWM test results. Conclusion: Our findings suggest that the LPS-induced model of chronic neuroinflammation can be used as an important tool for the investigation of the pathomechanisms of neurodegenerative disorders and the development of new pharmacotherapeutic options.
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