Molecular Formula | C26H34O7 |
Molar Mass | 458.54 |
Density | 1.34±0.1 g/cm3(Predicted) |
Melting Point | 259-262° |
Boling Point | 627.3±55.0 °C(Predicted) |
Specific Rotation(α) | D20 +11° |
Solubility | Soluble in DMSO |
Appearance | Powder |
pKa | 14.67±0.70(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD28396383 |
Physical and Chemical Properties | from toad |
Hazard Symbols | T+ - Very toxic |
Risk Codes | 26/27/28 - Very toxic by inhalation, in contact with skin and if swallowed. |
Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1/PG 1 |
WGK Germany | 3 |
RTECS | EI2991000 |
Hazard Class | 6.1(a) |
Packing Group | II |
Reference Show more | 1. Lan Wei, Chen Xi-zhen, Li Yusheng, Wu Yue, Yang Tianming, Tang and bin. Analysis of components and metabolites of alcohol extract of Liushen pills in rat plasma by HPLC-Q-Orbitrap-MS [J]. Journal of Pharmaceutical Analysis, 2020,40(04):633-643. 2. Mao Peizhi, Cao yuetin, Cui cocoa, Lu Zhengyu, Liang, Wang Longhu. A comparative study on the contents of xenobiotics in the serum of Bufo bufo gargarizans from different habitats [J]. Chinese Journal of Modern Applied Pharmacy, 2020, 37(09):1080-1084. 3. Cao Yueting, Cui, cocoa, Wu, Jiheng, et al. Study on the correlation of the components of the venom of Chinese big toad [J]. Chinese Journal of Traditional Chinese Medicine 2019(9). 4. Zhang Mei Li Yu, Sangye Xiaoxue. Study on plasma Medicinal Chemistry of Liushen pills [J]. Green Science and Technology 2017 000(012):237-240. 5. Wu juanping, Xue Tao, Guo Lu, Zhang Yan. HPLC fingerprint and chemical pattern recognition of Huachansu capsules [J]. Journal of Pharmaceutical Analysis, 2020,40(11):1977-1985. 6. [IF = 2.193] Zhang Mei-Tuo et al."Strategic Combination of Isocratic and Gradient Elution for Simultaneous Separation of Polar Compounds in Traditional Chinese Medicines by HPLC."J Anal Methods Chem. 2018;2018:7569283 7. [IF=4.411] Yueting Cao et al."Chemical Profile and Multicomponent Quantitative Analysis for the Quality Evaluation of Toad Venom from Different Origins."Molecules. 2019 Jan;24(19):3595 8. [IF=4.379] Cao Yueting et al."The impact of multiple climatic and geographic factors on the chemical defences of Asian toads (Bufo gargarizans Cantor)."Sci Rep-Uk. 2019 Nov;9(1):1-11 9. [IF=1.902] Ke-ke Cui et al."Quantitative analysis of multicomponents by a single marker and quality evaluation of Venenum Bufonis from different geographical origins."Biomed Chromatogr. 2019 Sep;33(9):e4555 |
Introduction | cinobufagin is an indole total alkaloid extracted from dried toad skin of the Chinese big toad, it has the effects of clearing away heat and toxic substances, relieving swelling and pain, promoting blood circulation and removing blood stasis, and softening and dispersing nodules. Animal experiments show that cinobufacin can improve the body's immune ability and inhibit the synthesis of DNA and RNA in tumor cells. |
efficacy and action | cinobufagin (a water-soluble preparation made from toad skin) it can increase the content of serum IgG in immunosuppressed and sensitized mice, increase the number of peripheral white blood cells in high and low white model mice, and promote the phagocytic function of peritoneal macrophages, cinobufacini can also significantly improve the humoral immunity in mice. The experiment shows that cinobufacini capsule, like the chemotherapeutic drug 5-Fu, acts on the tumor tissue to break, necrosis and degeneration the cancer cell nucleus. The use of cinobufacini capsules showed a significant increase in humoral immune response, cellular immunity has also been enhanced. |
pharmacological effects | 1. Anti-tumor effects. Cinobufotalin 3G crude drug (per kg of body weight) has obvious antitumor effect on transplanted tumor S180 sarcoma and H22 liver cancer in mice, and has obvious tendency to prolong the life of L1210 leukemia mice. The inhibition rate of Huachansu 7.5g crude drug/kg on W256 in rats was 68.7%. In vitro drug test showed that cinobufotalin crude drug 2 mg/mL on three kinds of digestive system tumor strains (human liver cancer SMMC-7721, human gastric cancer MKN45, human colon cancer LOVO) have killing effect, its mechanism is direct killing tumor cell DNA, resulting in tumor cell necrosis. It was observed that cinobufotalin could increase cAMP content in plasma of H22 hepatoma-bearing mice and restore cAMP/cGMP ratio to normal. The inhibition rate of cinobufacine was 35.5% in S180 sarcoma mice, and the inhibition rate was increased to 71% after combined application with CTX, clinical data also showed that cinobufotalin combined with 5-Fu, CTX, MTX, VCR has a synergistic effect, the efficacy of chemotherapy combined with cinobufotalin was significantly improved than the single drug, and can reduce the side effects of radiotherapy and chemotherapy. 2. Immune promoting effect. Cinobufotalin has preventive and therapeutic effects on leukopenia induced by CTX, and can increase the percentage of lymphocytes and the content of IgG and IgM in serum of mice; the experimental data also showed that cinobufacin had the function of enhancing humoral immunity and cellular immunity. 3, antiviral effect. The results showed that cinobufotalin could significantly inhibit the replication of 2215 cells and duck hepatitis B Virus. The clinical data also showed that the effect of cinobufacin on chronic HBsAg carriers was significant. |
Application | cinobufacini can be used for a variety of advanced tumors (lung cancer, breast cancer, cervical cancer, digestive system tumors such as primary liver cancer, gastric cancer, colon cancer, etc.), chronic hepatitis B, especially for chronic hepatitis B Virus carriers is particularly prominent. |
cinobufacin injection | , lung cancer, cervical cancer, skin cancer, etc.|
adverse reactions | if the dosage is too large or the interval between two doses is less than 6-8 hours, about 30 minutes after the administration, there may be a cold Fever phenomenon; A small number of patients with long-term intravenous drip after local irritation or phlebitis, resulting in a slow drop speed, very few patients may also appear urticaria, dermatitis and so on. |
note | Local absorption of this product is slow, with tingling sensation or phlebitis at the injection site, dermatitis, etc., after discontinuation of the reaction disappeared, can still be normal medication; A small number of patients with Nausea, chills reaction, 10 minutes after the return to normal; Should pay attention to the patient's heart function, to avoid aminophylline, isoproterenol and other intense excitement cardiac drugs at the same time. |
Use | for content determination/identification/pharmacological experiments |