Advances in the Discovery of Anthraquinone-Based Anticancer Agents

Тихомиров, А. С.; Shtil, Alexander А.; Shchekotikhin, Andrey E.

doi:10.2174/1574892813666171206123114

Cited by 75 publications

(36 citation statements)

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“…An array of secondary metabolites is produced by living organisms under different conditions, which are beneficial to the organisms and have a variety of applications for humans [4]. Anthraquinones is one of secondary metabolites that are produced by various plants and are applied in a wide range of applications, for example, as coloring agents in the food and textile industries and as therapeutic agents for various diseases [5,6]. They are derived from 9,10-anthracenedione.…”

Section: Introductionmentioning

confidence: 99%

Chrysophanol: A Natural Anthraquinone with Multifaceted Biotherapeutic Potential

et al. 2019

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Chrysophanol is a unique anthraquinone having broad-spectrum therapeutic potential along with ecological importance. It is the first polyketide that has been reported to be biosynthesized in an organism-specific manner. The traditional Chinese and Korean medicinal systems provide evidence of the beneficial effects of chrysophanol on human health. The global distribution of chrysophanol encountered in two domains of life (bacteria and eukaryota) has motivated researchers to critically evaluate the properties of this compound. A plethora of literature is available on the pharmacological properties of chrysophanol, which include anticancer, hepatoprotective, neuroprotective, anti-inflammatory, antiulcer, and antimicrobial activities. However, the pharmacokinetics and toxicity studies on chrysophanol demand further investigations for it to be used as a drug. This is the first comprehensive review on the natural sources, biosynthetic pathways, and pharmacology of chrysophanol. Here we reviewed recent advancements made on the pharmacokinetics of the chrysophanol. Additionally, we have highlighted the knowledge gaps of its mechanism of action against diseases and toxicity aspects.

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Section: Introductionmentioning

confidence: 99%

Chrysophanol: A Natural Anthraquinone with Multifaceted Biotherapeutic Potential

et al. 2019

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“…Natural products are the most versatile source of new compounds with biologicals effects, since the majority of drugs currently in use are derived or synthesized from natural molecules and their products [22]. Anthraquinones, a natural class of compounds used as laxative, antimalarial [23, 24], anticancer [25], and antiviral [26] treatments, recently demonstrated anti-inflammatory action by interfering in the intracellular signaling related to the activation of STAT proteins [27]. It is not unexpected that signaling conducted by various STATs, particularly STAT3, will be closely interconnected with NF- κ B signaling—the nuclear factor responsible for managing the production of proinflammatory mediators in ALI, sepsis, and systemic shock [28–30].…”

Section: Discussionmentioning

confidence: 99%

Evidence That the Anti-Inflammatory Effect of Rubiadin-1-methyl Ether Has an Immunomodulatory Context

Mohr

Nascimento

Rosa

et al. 2019

Mediators of Inflammation

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Background In spite of the latest therapeutic developments, no effective treatments for handling critical conditions such as acute lung injuries have yet been found. Such conditions, which may result from lung infections, sepsis, multiple trauma, or shock, represent a significant challenge in intensive care medicine. Seeking ways to better deal with this challenge, the scientific community has recently devoted much attention to small molecules derived from natural products with anti-inflammatory and immunomodulatory effects. Aims In this context, we investigated the anti-inflammatory effect of Rubiadin-1-methyl ether isolated from Pentas schimperi, using an in vitro model of RAW 264.7 macrophages induced by LPS and an in vivo model of acute lung injury (ALI) induced by LPS. Methods The macrophages were pretreated with the compound and induced by LPS (1 μg/mL). After 24 h, using the supernatant, we evaluated the cytotoxicity, NOx, and IL-6, IL-1β, and TNF-α levels, as well as the effect of the compound on macrophage apoptosis. Next, the compound was administered in mice with acute lung injury (ALI) induced by LPS (5 mg/kg), and the pro- and anti-inflammatory parameters were analyzed after 12 h using the bronchoalveolar lavage fluid (BALF). Results Rubiadin-1-methyl ether was able to inhibit the pro-inflammatory parameters studied in the in vitro assays (NOx, IL-6, and IL-1β) and, at the same time, increased the macrophage apoptosis rate. In the in vivo experiments, this compound was capable of decreasing leukocyte infiltration; fluid leakage; NOx; IL-6, IL-12p70, IFN-γ, TNF-α, and MCP-1 levels; and MPO activity. In addition, Rubiadin-1-methyl ether increased the IL-10 levels in the bronchoalveolar lavage fluid (BALF). Conclusions These findings support the evidence that Rubiadin-1-methyl ether has important anti-inflammatory activity, with evidence of an immunomodulatory effect.

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“…Разработанный в ФГБНУ «НИИНА» оригинальный противоопухолевый препарат антрафуран (ЛХТА-2034) является потенциальным противоопухолевым агентом, относящимся к новому классу противоопухолевых гетероциклических производных антрахинона [12]. Антрафуран обладает высокой эффективностью на различных моделях сингенных опухолей мышей [13,14].…”

Section: Key Words: аNthrafuran Lcta-2034 Preclinical Studies Neuunclassified

Neurotoxic properties of new antitumor agent anthrafuran

Голибродо

Treshchalin

Shchekotikhin

et al. 2019

Rossijskij bioterapevtičeskij žurnal

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Introduction . Currently, the study of the neurotoxic properties of new drugs is an indispensable step towards the promotion of the medicine to clinical practice. The original antitumor drug anthrafuran (LCTA-2034), obtained in Gause Institute of New Antibiotics, has demonstrated high activity against transplantable mice tumors. Previous studies have shown that the drug in high doses causes brain tissues damage.Objective: a pilot investigation of anthrafuran neurotoxicity.Materials and methods . The study was carried out on 52 female outbred rats. The suspension of drug in water for injection was administrated per os at a single maximum tolerated dose of 170 mg/kg. The testing was performed on “open field” setting 1, 4 and 8 h and repeated on day 1 and 30 post treatment.Results . It was found that the administration of the drug reduced both motor (covered distance, average speed) and research (the number of rearings, contacts with the “burrow”) activity as compared to control. These effects were manifested to the greatest extent 4 h post treatment. A day later, when rats re-visit “open field”, the parameters under study increased in this group, while in the control group these indicators decreased.Conclusion . Anthrafuran exhibits a reversible inhibitory effect on the motor and research activity of rats.

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Advances in the Discovery of Anthraquinone-Based Anticancer Agents

Cited by 75 publications

References 0 publications

Chrysophanol: A Natural Anthraquinone with Multifaceted Biotherapeutic Potential

Chrysophanol: A Natural Anthraquinone with Multifaceted Biotherapeutic Potential

Evidence That the Anti-Inflammatory Effect of Rubiadin-1-methyl Ether Has an Immunomodulatory Context

Neurotoxic properties of new antitumor agent anthrafuran

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