Development of composition based on echinochrome a with ascorbic acid and α-tocopherol for oral administration

Joint Event on 12^th International Conference and Exhibition on Pharmacovigilance & Drug Safety & 22^nd International Conference and Exhibition on Pharmaceutical Formulations & 21^st Euro-Global Summit on Toxicology

July 04-06, 2019 Valencia, Spain

Elena A. Vasileva, Natalia P. Mishchenko, Sergey A. Fedoreyev and G. B. Elyakov

Pacific Institute of Bioorganic Chemistry, Russian Federation

Posters & Accepted Abstracts: J Formul Sci Bioavailab

Abstract :

Secondary metabolites specific to sea urchins are known as spinochromes. The most well-known sea urchin pigment echinochrome A exhibit a wide range of pharmacological activities, for example antioxidant, anti-diabetic [1], antiallergic [2], cardioprotective [3], and also protects mitochondrial functions against cardiotoxic drugs [4]. In addition, echinochrome A is the active substance in the cardioprotective and ophthalmic drug Histochrome®, produced in Russia from the sand dollar Scaphechinus mirabilis [5]. One of the main obstacles to the wide use of echinochrome A is its insolubility in water. Histochrome is available only in ampoules in the form of echinochrome A sodium salts for intravenous injections. To expand area of echinochrome A application, it is very important to investigate abilities of echinochrome A to form complexes with substances that can increase its solubility, protect its hydroxyl groups from oxidation, preserving or enhancing its pharmacological properties. Very recently, we obtained a powder composition of echinochrome A (Ech) with other well-known antioxidants â?? ascorbic acid (Asc) and alpha-tocopherol (Toc). Ratio of components was chosen based on the results of lipids peroxidation inhibition assay. The most strong antioxidant effect demonstrated composition Ech-Asc-Toc 5:5:1 [6]. We established that this composition containing bulk media is stable for 1 year and that addition of antioxidants and excipients does not affect echinochrome A permeability through artificial membrane imitating gastrointestinal tract (PAMPA assay). The developed composition showed in vitro antiviral activity against RNA-containing tick-borne encephalitis virus and DNA-containing herpes simplex virus type 1 [6]. The studied composition of antioxidants exhibits more potent antioxidant and antiviral properties than Ech itself, thus opening perspectives of its medical application as tablets and capsules. This study was supported by the grant of the Ministry of Higher Education and Science of Russian Federation (project RFMEFI61317X0076).

Recent Publications

1. Mohamed AS, Soliman AM, Marie MAS (2016) Mechanisms of echinochrome potency in modulating diabetic complications in liver. Life Sci 151: 41â??49.

2. Itoh T, Fujiwara A, Ninomiya M, Maeda T, Ando M, Tsukamasa Y, Koketsu M (2016) Inhibitory effects of echinochrome A, isolated from shell of the sea urchin Anthocidaris crassispina, on antigen-stimulated degranulation in rat basophilic leukemia RBL-2H3 cells through suppression of Lyn activation. Nat Prod Commun 11:1303â??1306.

3. Kim HK, Youm JB, Jeong SH, et al (2015) Echinochrome A regulates phosphorylation of phospholamban Ser16 and Thr17 suppressing cardiac SERCA2A Ca2+ reuptake. Pflügers Arch 467:2151â??2163.

4. Jeong SH, Kim HK, Song IS, et al (2014) Echinochrome A protects mitochondrial function in cardiomyocytes against cardiotoxic drugs. Mar Drugs 12: 2922â??2936.

5. Elyakov GB, Maximov OB, Mischenko NP, et al. Histochrome and its Therapeutic Use in Acute Myocardial Infarction and Ischemic Heart Disease. US Patent 2001, 6,410,601.

6. Fedoreyev SA, Krylova NV, Mishchenko NP, et al (2018) Antiviral and Antioxidant Properties of Echinochrome A. Mar Drugs 16: 509.

Biography :

Elena A. Vasileva is Junior Researcher in the Laboratory of the Chemistry of Natural Quinonoid Compounds, G. B. Elyakov Pacific Institute of Bioorganic Chemistry, Vladivostok, Russia. She has an experience in identification, isolation and structure elucidation of natural quinonoid compounds from plants, their cell cultures and sea urchins.