Name | polyinosinic-polycytidylic acid |
Synonyms | Polycytidysic acid polyinosinic-polycytidylic acid Polyinosinic acid-polycytidylic acid |
CAS | 24939-03-5 |
EINECS | 1308068-626-2 |
InChI | InChI=1/C10H13N4O8P.C9H14N3O8P/c15-6-4(1-21-23(18,19)20)22-10(7(6)16)14-3-13-5-8(14)11-2-12-9(5)17;10-5-1-2-12(9(15)11-5)8-7(14)6(13)4(20-8)3-19-21(16,17)18/h2-4,6-7,10,15-16H,1H2,(H,11,12,17)(H2,18,19,20);1-2,4,6-8,13-14H,3H2,(H2,10,11,15)(H2,16,17,18) |
Molecular Formula | C19H27N7O16P2 |
Molar Mass | 671.403 |
Boling Point | 851.4°C at 760 mmHg |
Flash Point | 468.7°C |
Vapor Presure | 7.7E-31mmHg at 25°C |
Storage Condition | 2-8℃ |
Sensitive | Easily absorbing moisture |
MDL | MFCD00131983 |
Use | Antiviral drugs can be used for herpes zoster, hepatitis B, etc |
Reference Show more | 1. Gao Xiaoxiao, Xiang Zhihao, Chen Fuzeng, Zhang Lu, Liu Jun. Preparation of AN Fusion Antigen and Its Effect on Enhancing BCG Immune [J]. Fudan Journal (Natural Science Edition),2020,59(06):677-684. |
This product is a synthetic interferon inducer, which is a double-stranded polynucleotide composed of polyinosinic acid and polycytidine. Because interferon has Species specificity, it is difficult to prepare a large number of interferon for clinical application. Therefore, Interferon inducers are often used to induce interferon. In addition, the role of the immune adjuvant, can stimulate the reticuloendothelial system, enhance the phagocytic function of phagocytes, enhance the formation of antibodies, stimulate the allogeneic transplantation reaction and delayed allergic reaction. Has broad-spectrum antiviral effect, anti-tumor effect.
there is a transient low-grade fever, individual cases of high fever above 38 ° C, more than 1~2 days to eliminate Fatigue, dry mouth, dizziness, Nausea.
overview
Polycytidine acid, also known as polyinosinic acid, polyhypoxanthine nucleotide, polycytosine nucleotide, is one of the polymer polynucleotides (polynucleotides) substances, composed of polyinosinic acid and polycytidine Acid forms a double-stranded polynucleotide chain, which has characteristic color reduction and melting point, and is stable at -20 ℃.
pharmacological action
1. immunoregulation
Immunity is a physiological protective function of the body. It is the body's ability to recognize and eliminate any foreign objects (viruses, bacteria, etc.) that invade, deal with aging, damage, death, and degeneration of its own cells, and recognize and process mutations in the body The ability of cells and virus-infected cells. Modern immunology believes that immunity is the physiological response of the human body to recognize and exclude "dissidents. The immune ability of the body can be roughly divided into specific immunity and non-specific immunity, which are closely related. Non-specific immunity is an immune function formed by organisms in the continuous struggle with pathogenic microorganisms in the process of germline development, and can be passed on to offspring. It is closely related to the tissue structure and physiological function of the human body. Specific immunity is the immune function obtained by the body after being stimulated by internal and external environmental factors. It can recognize the same antigen that is contacted again and respond accordingly. It needs to be completed with the participation of highly differentiated tissues and cells. Polyinosinic cell is the ligand of Toll-like receptor type 3 in animals. After activation of TLR-3, polyinosinic cell can mediate a series of immune responses, such as inducing the secretion of cytokines such as interferon, interleukin and tumor necrosis factor, promoting the proliferation and maturation of cells, monocytes, macrophages, lymphocytes and dendritic cells, and promoting the production of antibodies in vivo. Polyinosinic cells have a good promotion effect on the specific and non-specific immunity of the body.
(1) Polyinosinic cells enhance the activity of immune cells
(2) polyinosinic cells promote the secretion of various cytokines
(3) the induction effect of polyinosinic cells on Mx protein
(4) Polyinosinic cells promote the production of antibodies in vivo
2. antiviral effect of polyinosinic cells
In vitro tests, animal tests and human clinical trials have proved that polyinosinic cells have a wide range of antiviral effects, and are effective against yellow fever virus, encephalomyelitis virus, Lift Valley fever virus, avian influenza virus, hepatitis virus, HIV, foot-and-mouth disease virus, conjunctivitis virus, simple rash virus, Mengo virus, vaccinia virus, encephalomyocarditis virus, Aleutian virus, Coxsack. Experiments have proved that the preventive effect of polyinosinic cells on viral infection is better than the therapeutic effect.
use
A double-stranded homopolymer that can be used as a model RNA to study cell signaling at the TLR3 level to recognize double-stranded RNA. It is also the main effector of the immune response of viral pathogens.
use
Paired with polyinosinic acid to form polyinosinic cells for the treatment of viral hepatitis, herpes zoster, herpes simplex keratitis, herpetic stomatitis, epidemic hemorrhagic fever, etc.
use
It has the function of immune adjuvant, which can stimulate the reticuloendothelial system, enhance the phagocytic function of phagocytes, enhance the formation of antibodies, and stimulate the allograft reaction and delayed allergic reaction. It has broad-spectrum antiviral and anti-tumor effects. Clinically, it is mainly used for: prevention or treatment of viral infection, treatment of herpes zoster, herpetic keratitis, and viral hepatitis. Adjuvant treatment of tumors. Adverse reactions mainly include transient low fever. Some cases have high fever above 38 ℃, which mostly subsides within 1-2 days. If the fever does not subside within 2 days, the drug should be stopped immediately. Still see fatigue, dry mouth, dizziness, nausea, etc.
production method
Using 5 '-nucleotide as raw material
preparation of 5 '-nucleoside diphosphate pyridine salt 5'-nucleotide (5 '-inosinic acid or 5'-cytidine acid) [morpholine, biscyclohexylcarbodiimide] & rarr;[ethanol, 83 ℃]5 '-nucleotide morpholine salt [tri-n-butylamine phosphate, anhydrous pyridine] & rarr;5'-nucleoside diphosphate pyridine salt
Preparation of immobilized polynucleotide phosphorylase
preparation of enzyme escherichia coli 1.683 thallus & rarr; Cell breaking extraction & rarr; Streptox precipitation to remove nucleic acid & rarr; Salting out of amine sulfate & rarr;DEAE-cellulose chromatography & rarr; Collect the part with the highest enzyme activity in 0.35mol/L sodium chloride eluent
preparation of solid phase carrier agar powder melts [toluene, carbon tetrachloride, disk -80]& rarr; After stirring and cooling, it is crosslinked with epichlorohydrin to prepare bead [p-β-sulfate ethylsulfone aniline] & rarr;[etherification] & rarr;[sodium nitrite, hydrochloric acid] & rarr; Solid phase carrier
Add the separated and purified enzyme solution dropwise to the solid carrier in the ice bath to obtain covalently bound immobilized polynucleotide phosphorylase.
Preparation of polyinosinic acid
The substrate IDP pyridine salt is converted into sodium salt, and CDP pyridine salt is converted into lithium salt.
enzymatic reaction, (μmol/L number per ml of reaction solution) IDP or CDP15,Tris150, magnesium chloride 6,EDTA1, polymerase 5U,pH 9.0,37 ℃,3-4h, adjust pH 1.5-2.0 with hydrochloric acid to precipitate polycreatine or polycytidine acid, centrifuge, then dissolve in phosphate buffer, equimolar polycreatine and polycytidine acid are mixed, that is, polyinosinic acid is obtained.
WGK Germany | 3 |
RTECS number | TR0175000 |