Emodin is an orange-yellow long needle-like crystal. It crystallizes in orange in acetone. It crystallizes in methanol and has a melting point of 256 ° C to 257 ° C. It has a special reaction of hydrazine, is almost insoluble in water, and is soluble in ethanol and alkali solution.
Emodin is the dried rhizome and root of Polygonum cuspidatum. The rhizome of palm rhubarb is a plant-type agent.
The physiological activity of emodin determines that it can be used not only in medical treatment but also in health care and household chemicals. If it is used in hair care and skin care products, it is also incorporated into natural pigments. And it can be used as a laxative.
Emodin has inhibitory effects on mouse solid sarcoma S-180, mouse liver cancer, breast cancer, Ehrlich ascites carcinoma, lymphosarcoma, melanoma, and rat Wacker tumor and lung cancer A-549, and its inhibition rate is 30%. the above. The inhibition rate of mouse melanoma growth was 73% at a dose of 50 mg/kg day-1; the inhibition rate of mouse breast cancer at a dose of 75 mg/kg day-1 was 45%. Emodin can prolong the survival of P388 leukemia mice with a prolongation rate of more than 40%. One of its mechanisms of action is to inhibit the biosynthesis of DNA, RNA, and proteins of cancer cells and inhibit the oxidative dehydrogenation of cancer cells.
Emodin has inhibitory effects on Staphylococcus aureus 209P, Streptococcus, Diphtheria, Bacillus subtilis, Paratyphoid bacillus, Shigella, Escherichia coli, Influenza, Pneumococci, and catarrhalis; It has a strong inhibitory effect; its MIC is slightly higher than metronidazole, and the concentration of anaerobic bacteria can be inhibited by 76%~91% at 8μg/ml. The antibacterial mechanism of emodin is related to inhibition of mitochondrial respiratory chain electron transport, inhibition of respiration and oxidation and dehydrogenation of amino acids, sugar and protein metabolism intermediates. The final result of inhibiting the synthesis of nucleic acids and proteins inhibits bacterial growth.
Intraperitoneal injection of emodin at a dose of 70 mg/kg can inhibit the production of rat antibodies, inhibit the clearance of carbon particles, reduce the weight of immune organs, reduce the number of white blood cells, and reduce the phagocytic function of peritoneal macrophages. In vitro, the concentration of [3H]-TdR and [3H]-Urd in lymphocytes was significantly inhibited at a concentration of 10 mg/ml.
Emodin has a strong inhibitory effect on sputum in isolated rat intestinal tract caused by acetylcholine, which is about 4 times that of papaverine. Emodin also has a significant antitussive effect.
Emodin has an excitatory effect on isolated sputum hearts at low doses, while large doses have an inhibitory effect. Emodin also has a hypotensive effect.
Emodin can increase the sodium and potassium levels in the urine, promote ureteral motility, and increase urine output.
Administration of emodin to rats with experimental intestinal obstruction at a dose of 10 μg/kg restored the histamine content in the intestinal mucosa of rats to normal levels, but had no effect on the histamine content in the blood.
Emodin is an inhibitor of 5-lipoxygenase, which inhibits the synthesis of LTB4 in human polynuclear leukocytes and LTB4 in whole blood, and has no inhibitory effect on the synthesis of PGE2.
Emodin can inhibit the transport of sodium and potassium ions from the intestinal lumen to the cells, so that the water stays in the intestinal lumen, stimulates the large intestine, promotes its peristalsis, and thus acts as diarrhea, but the effect is weak.
Oral emodin is easily absorbed in the intestine. After 2 to 3 hours, the blood reaches the highest concentration, and then slowly decreases. The urine and bile reach a peak 4 to 8 hours after taking the drug, and the urine can be discharged for 2 days in the body. The distribution of liver and kidney is the most. It has also been used as an injection for muscle and intravenous injections.
After emodin is absorbed, chrysophanol is excreted from the kidney, which turns the acidic urine into a brownish yellow color, which causes the alkaline urine to turn purple.
Clinically, the treatment of swollen cancer with pure emodin is mainly used for tumors such as leukemia and gastric cancer, and the most commonly used is for inhibition. It is against many bacteria such as various staphylococcus, hemolytic streptococcus, diphtheria bacillus, cholera bacteria, Escherichia coli, Pseudomonas aeruginosa, dermatophytes, Bacillus subtilis, Mycobacterium phlei, Neisseria gonorrhoeae, Bacillus licheniformis, and grassy fungi. , typhoid bacillus, dysentery bacilli, etc. have inhibitory effects. Among them, Staphylococcus, Neisseria gonorrhoeae, Streptococcus are more effective. This product is also effective against fungi, viruses, and protozoa. At the same time, it also has diuretic, choleretic, antispasmodic, lowering blood pressure and suppressing immune function.
Modern clinical use in almost all subjects, such as treatment of Japanese encephalitis and mumps, typhoid fever, dysentery, urinary tract infection, gonorrhea, pneumonia, cellulitis, suppurative skin disease, otitis media, vasculitis, etc., compatible with other drugs Treatment of acute and subacute appendicitis, burns, poliomyelitis, eczema and skin infections caused by several fungi, in addition to treatment of hepatitis, mites, stomatitis, lip ulcers, indigestion, hypertension and arteriosclerosis, therefore, emodin is It is widely used clinically.
The latest data show that emodin can affect the proliferation of keratinocytes in vitro; it can prevent restenosis after coronary interventional therapy. It can inhibit human kidney fibroblasts. Although emodin is less toxic, it is contraindicated in pregnant women because it may cause miscarriage in pregnant women.