Craig] [rules polygoni cuspidati and 80%, 98% (50%) and m.d.

emodin
[editor this segment] basic information
The product name emodin]
[English] Emodin names
[a] Ephraim: don't Frangula emodin t. Rheum, a meal Archin emodin, Frangulic, acid
[1] the learning of the 8-3 ' 'three hydroxyl - 6 - methyl anthraquinone
The sons of C15H10O5]. Points
The child is 270.23]. Points
[C] A S 518-82 - no. 1
[to] for polygonaceae plant source of Polygonum cuspidatum polygoni cuspidati Sieb. Et Zucc. Dry roots and root, Palm leaves palmatum L Rheum rhubarb roots.
Craig] [rules polygoni cuspidati and 80%, 98% (50%) and m.d.
The physical properties to orange long needle crystal (acetone crystallization of methanol to orange, yellow in color), melting crystallization c ~ 256 257 degrees. With the special anthraquinone reaction. Hardly soluble in water, but soluble in ethanol and alkali solution.
The pharmacological effects] emodin used for laxative, though lapactic activity, due to the body susceptible to oxidative damage lapactic action, in fact, very weak, such as sugar into nucleoside, can play lapactic action. Emodin - 1 -o-galloylhyperin beta D - isothiocyanante and emodin - 8 -o-galloylhyperin beta D - isothiocyanante emodin is combined with glucose, the combination between different locations, but also exists in large HuangZhong. Antibacterial, cough, otherwise the anti-tumor, fall blood pressure, etc.
Emodin role
[editor this segment] pharmacological effects
Oral emodin in intestinal absorption, 2 ~ 3 hours after the highest concentrations of blood, urine, slowly drops and bile after 4-8 hours of peak, the urine sustainable 2 days, the distribution of in vivo in most kidney. It also made for injection, muscles and intravenous.
Emodin absorbed by renal eduction, color, it can cause acidic urine into yellowish-brown alkaline urine into that.
In the clinical treatment of emodin, tasted, mainly used in cancer is swollen gastric cancer, leukemia, etc. And the most commonly used for bacteriostatic. It for many bacteria staphylococcus aureus, such as various hemolytic streptococcus, diphtheria bacili, cholera bacteria isolated, escherichia coli, pseudomonas aeruginosa, skin fungus, bacillus subtilis, mycobacterium phlei, drench coccus, carbon appropriate bacili, grass shape, typhoid bacillus, dysenteric bacili, etc. One of staphylococcus aureus, streptococcus pneumoniae, drench coccus is more effective. This product of fungi, viruses, protozoon also effectively. At the same time, it also has the diuretic, bravery, spasm, lower blood pressure, suppresses the immune function, etc.
Almost everybody with modern clinical treatment, such as encephalitis, typhoid fever, diarrhea and mumps and urinary tract infections, gonorrhea, pneumonia, cellulitis, suppurative otitis media, such skin, vasculitis, and other drug treatment of acute and subacute appendicitis compatibility, burns, polio, eczema and several caused by fungus infections of the skin, also can cure hepatitis, pinworm and stomatitis, oral ulcer, indigestion, hypertension and atherosclerosis, therefore, emodin in clinical application widely.
The latest data shows, emodin can affect keratin cells in vitro proliferation, Can prevent coronary post-interventional workup restenosis after treatment. Can restrain human kidney fibroblasts. Emodin, although small toxicity, but women, because it can be disabled by milk into their babies.
Emodin physiological activity, it not only can be used to decide, also can be used in medical care and daily chemicals, such as it used to protect hair and skin, also somebody put it into the natural pigment. Abroad, people regard it as a laxative.
(a) antitumor activity
Emodin in mice entity sarcoma S - 180, mouse liver, breast, adenauer ascties cancer, lymphatic caruncle, melanoma and rats, and lung cancer tumors were - 549 inhibition, its inhibition rate in more than 30%. In 50mg/kg - 1 doses of mice melanoma growth inhibition rate to 73%, In 75mg/kg - 1 dose of mice under the inhibition rate for 45% of breast cancer. Emodin can prolong P388 leukemia, extend the mice bred in 40%. Its mechanism is one of the restrain cancer cell DNA, RNA and protein synthesis, restrain cancer cell oxidation dehydrogenase.
(2) antimicrobial action
Emodin 209P against staphylococcus aureus, streptococcus, diphtheria bacili, bacillus subtilis, paratyphoid, dysenteric bacili, escherichia coli, influenzae, pncumonia coccus, he had coccus inhibition, For clinical common anaerobic bacteria had a stronger inhibitory effect, The MIC slightly higher than in eight mu g and metronidazole/ml concentration can make 76% ~ 91 anaerobic bacteria growth inhibition. Emodin antibacterial mechanism and inhibit mitochondrial suppression electron-transport chain, with amino acids, and the breath of the metabolic protein oxidation and dehydrogenation and so on. Restrain the nucleic acid and protein synthesis, make the final results of bacteria growth inhibition.
(3) immunosuppression
According to 70mg/kg doses of rats intraperitoneal injection of emodin, can inhibit rats, inhibition antibody carbon clearance capacity, reduce weight, lower immune organs of white blood cell count, lower abdominal macrophage phagocytosis function. In vitro 10mg/ml in the concentration of [with]] - TdR 3H []] - 3H Urd participation in the lymphocyte has obvious inhibition.
(4) spasmolysis, cough
Emodin caused to acetylcholine from rat loops have strong inhibition spasm, about four times expose alkali. Emodin and obvious effect. Cough
(5) on the cardiovascular system
Emodin in small doses of toad, and heart are excited to have large doses of inhibition. Emodin and function.
(6) diuresis function
Emodin can make the urine sodium potassium content, promote and urine volume increased, ureteral peristalsis.
(7) of histamine role
By 10 mu g/kg doses obstruction of experimental rat gastric lavage emodin, can make rats intestinal mucosa histamine content return to normal levels of blood, but had no effect on the content of histamine.
(8) to LTB4 synthesis
Emodin is 5 - enzyme inhibitors, lipid oxygen can inhibit one type of nuclear LTB4 leukocytes and blood LTB4 synthesis of synthesis of PGE2 without inhibition.
(9) lapactic action
Emodin can inhibit sodium potassium ion and then transfer to cells from the moisture retention, then, in the intestine, promote its peristalsis, thus plays lapactic action, but weaker.
[editor this segment] drug kinetics
According to 50mh/kg doses of gastric lavage rats 14C - emodin, 24 hours of urine is given dose of 18% longterm within 72 hours, is to give doses of 22 percent. The discharge of urine rhubarb acid most in 24 hours. Within 72 hours after, urine, mainly free metabolites rarely emodin, combined with the acid for rhubarb gives 16% of emodin, dosage of glucose aldehyde content of sulfuric acid esters were or only 3%, for other radioactive residue 3%. After 24 hours, and 120 hours of feces, emodin, mainly for pre-columri respectively given dose of 48 percent and 68%. After six hours, bile in the excretion of the highest concentrations of emodin in 15 hours for the excretion of 49%, to give dose acid ester or acid ester glucose forms of existence, emodin, 70% after 3 ~ 5 days, most of the organs of radiation activity, but until the first five days, the high remains in the kidney radiation activity. After 72 ~ 120 hours of adipose tissue, mesenteric and radiation activity increase greatly.
According to 91mg/kg doses of gastric lavage mice emodin 0 ~ 48 hours after the urine, feces and excretion of total anthrquinone is given dose 53%. Among them, in 0 ~ 24 hours of excrement and urine and 2% sum excretion. After four hours, bile in total anthrquinone peak, then gradually decreases. Bile emodin is one of the main ways for excretion.