| Purpose:This paper is part of the National Natural Science Foundation project "Fructus Polygoni Orientalis function changes before and after processing and the material basis of change-related research (Project No: 30873437) ". Fructus Polygoni Orientalis(FPO)began accepting set on Chinese Pharmacopoeia since 1977, with "dispersing stasis blood and mass gathering in the abdomen, relieving food retention and alleviating pain" effect, clinical students to use with or fry popcorn. FPO has been reported with anti-tumor effect on the primary Liver cancer has a good effect. This paper accords to the " dispersing stasis blood and mass gathering in the abdomen, relieving food retention and alleviating pain" effect of FPO, its raw materials and processed products of different solvent extracts and single compounds in vitro anti-tumor effect, S-180 ascites tumor effect in mice life span, S -180 inhibition of tumor-bearing mice, Taxifolin factor on human cervical cancer Hela inhibition of tumor-bearing nude mice and negatively analgesic efficacy experiments, and conducted anti-tumor mechanism of antioxidant effect and acute toxicity Experimental study. Through this study, pharmacological effects of raw materials and processed products, as well as traditional Chinese medicine theory of science, to provide a scientific basis for clinical therapy; by exploring its antioxidant components of the effective parts, Mechanism of antitumor effect and acute toxicity, can provide a scientific reference Polygonum and Pharmacodynamic Study of Drug Development about FPO.Methods:1.Its raw materials and processed products with different solvent extracts and compounds were screened in vitro efficacy of anti-tumor effects: using crystal violet to detect the difference of its raw materials and processed products with different solvent extracts and purified compounds on Hela cells, MGC cells, HepG-2 cells and Hce-8693 cells proliferation, inhibition rate calculated.2.Its raw materials and processed products with different solvent extracts and compounds on S-180 ascites of mice extend the role of life: the establishment of S-180 ascites sarcoma in mice was observed as its raw materials and processed products with different solvent extracts and purified compounds on S-180 to extend the life of mice with ascites tumor effect, calculated life extension rate.3.Its raw materials and processed products with different solvent extracts and compounds on S-180 inhibition of tumor-bearing mice: the establishment of solid tumor S-180 sarcoma in mice was observed as its raw materials and processed products with different solvent extracts and purified compounds on the S-180 inhibition of tumor-bearing mice, inhibitory rate was calculated.4.Taxifolin on human cervical cancer Hela inhibition of tumor-bearing nude mice: to establish nude mouse model of cervical cancer Hela, testing human cervical carcinoma Hela nude mice inhibited tumor volume calculation and the antitumor rate.5.Taxifolin mechanism of antitumor effect of factors: by inverted microscope and electron microscope,texting the morphological changes and the impact of DNA fragments of HeLa cell with Taxifolin; by RT-PCR method to detect the influence on human Bcl-2 mRNA, Bax mRNA and P53 mRNA, P21 mRNA gene expression.6."Relieving food retention" effect of Pharmacodynamics Study: the isolated rabbit intestine method to detect the influence of its raw materials and processed products with different solvent extracts and compounds on isolated rabbit intestinal tension; mouse small intestine by promoting carbon powder used to detect its raw materials and processed products with different solvent extracts and compounds on the gastrointestinal function of mice was calculated forward rate of carbon powder.7."Alleviating pain" effect of Pharmacodynamics Study: hot plate used to detect its raw materials and processed products with different solvent extracts and compounds from mice stimulated by the thermal effects of pain, pain threshold increased percentage; by writhing, detected acetic acid induced writhing times of mice to calculate the percentage inhibition of writhing.8.Preliminary antioxidant experiment of FPO: DPPH method used to determine the antioxidant activity of its raw materials and processed products with different solvent extracts and compounds.9.Acute toxicity test of FPO: Press the part of "Approval of New Pharmaceuticals", test the determination of LD50 and the maximum amount of test administration, determine acute toxicity of its raw materials and processed products with different solvent extracts and compounds.Results:1.Its raw materials and processed products with different solvent extracts and compounds were screened in vitro efficacy of anti-tumor effects:its raw materials and processed products with different solvent extracts and compounds on the growth inhibition of Hela cells in a concentration and time dependent, and inhibition of raw materials than processed products stronger, raw materials of which the strongest inhibition is ethyl acetate; in addition to raw materials soluble part, the inhibition of cell growth on the MGC cell in a dose and time dependent, in which raw materials the strongest part of the inhibitory effect is ethyl acetate; HepG-2 cell growth inhibition in a dose and time dependent, in which raw materials the strongest inhibition is ethyl acetate; Hce-8693 cell growth inhibition in a dose and time dependent, in which raw materials the strongest inhibition is ethyl acetate; 3,3 '- dimethoxy tanning Spent acid-4-O-β-D-glucopyranoside and taxifolin in 1 ~ 500μg/ml concentration of elements in the range of Hela cells, MGC cells, HepG-2 cells and Hce-8693 cell proliferation, as the dose increases, and the role of time, showing a good dose - time - effect relationship, the same factors under taxifolin than 3,3 '- dimethoxy tanning Spent acid-4-O-β-D-glucopyranoside stronger inhibition.2.Its raw materials and processed products with different solvent extracts and compounds on S-180 ascites of mice extend the role of life: raw water extraction group, raw ethyl acetate group materials, quercetin and taxifolin were extend the role of mice a good life, the strength of the order: taxifolin > quercetin> raw ethyl acetate extract> raw water extract materials> Other.3.Its raw materials and processed products with different solvent extracts and compounds on S-180 inhibition of tumor-bearing mice:raw ethyl group, quercetin, taxifolin on the S-180 study group had a certain inhibition in mice, the strength of the order: taxifolin > raw ethyl acetate extract > quercetin> raw water extract materials > Other.4.Taxifolin on human cervical cancer Hela inhibition of tumor-bearing nude mice: factors in the administration of taxifolin 8d starting tumor volume in nude mice than the saline group started, the quality of taxifolin group was significantly lower than the saline group, suppression Tumor rate was 45.45%, greater than in vivo antitumor efficacy test criteria of solid tumors, 30%, indicating that the certain extent on Hela cell with taxifolin.5.Taxifolin mechanism of antitumor effect of factors: taxifolin hormone treatment of human cervical carcinoma Hela cells after 12h, cells became round and gradually detached from the culture bottle wall down, 24h after the induction of foam cell and present nuclear burst, most of the cells gradually formation of apoptotic bodies; taxifolin prime HeLa cells inducing a multiple of 200 bp DNA fragments, and further description of HeLa cells death induced by apoptosis; taxifolin on the expression of mRNA and Bax mRNA did not change, but can induce P53 mRNA and P21 mRNA increased expression.6."Relieving food retention" effect of Pharmacodynamics Study: the extract of FPO are on isolated rabbit intestinal tension produced different degrees of impact, which provide raw water, the product can excited rabbit intestinal smooth muscle, it contraction accelerated, but the tension of aqueous raw materials become smaller, and the role of long-lasting water extraction products, basically the same amplitude; ethanol effect of raw materials provide raw materials and water equivalent to the role of ethanol products, a very short time, increase the dose showing inhibition; FPO extract on the gastrointestinal promote varying degrees, products, raw materials extraction extract than the stronger, the specific role of the strength of the order: ethanol extract of processed products > water extract of processed products > water extract of raw materials> ethanol extract of raw materials.7."Alleviating pain" effect of Pharmacodynamics Study: hot plate test, the raw materials and products water extract could enhance the pain threshold in mice, while the ethanol extract of analgesic effect was not obvious, the strength of its analgesic effect of the order: water extract of processed products>water extract of raw materials>alcohol extract of raw materials and processed products; writhing test, the water extract products, raw materials and products can reduce the ethanol extract of writhing in mice, resulting in varying degrees of pain effect of water extract of raw materials to increase the number of writhing, analgesic effect was not obvious, the strength of the analgesic effect of extract of the order: water extract of processed products> ethanol extract of raw materials >ethanol extract of processed products > water extract of raw materials.8.Preliminary antioxidant experiment of FPO: raw materials and processed products of FPO extracts from different solvents have different levels of free radical scavenging effect.9.Acute toxicity test of FPO: mice after administration showed reduced activity, and looked burnout, 1h after administration of this phenomenon gradually disappeared, no abnormal jumping behavior, no stimulus-sensitive signs, mouth, eyes, nose, abnormal secretion does not appear , food, water, defecation, breath were normal, no death, could not measure the LD50 value; the maximum amount of drug experiments, the continuous observation 7d found, reduced activity in mice after administration, and looked tired, administration 3h Disappears, all the mice were kept healthy, animal appetite, appearance, behavior, excretion and so are the exception, see, the 7 day average weight increase of 27.61%, were killed after dissection found no abnormal tissues and organs.Conclusions:1.Its raw materials and processed products with different solvent extracts and compounds were screened in vitro efficacy of anti-tumor effects: ethyl acetate extract of raw materials for 4 inhibition of tumor cells are better than others, is the effective inhibition tumor Material group of FPO; 3,3'-dimethoxy ellagic acid-4-O-β-D- glucopyranoside and taxifolin can inhibit the growth of 4 tumor cells ,under the same conditions inhibited prime taxifolin is stronger, probably as FPO the main anti-tumor effective substance.2.Its raw materials and processed products with different solvent extracts and compounds on S-180 ascites of mice extend the role of life: taxifolin, quercetin, water extract of raw materials and ethyl acetate extract of raw materials were well prolongation of life.3.Its raw materials and processed products with different solvent extracts and compounds on S-180 inhibition of tumor-bearing mice: taxifolin, quercetin, water extract of raw materials and ethyl acetate extract of raw materials exhibited a potent inhibition on the proliferation of S-180 mice.4.Taxifolin on human cervical cancer Hela inhibition of tumor-bearing nude mice: taxifolin exhibited a potent inhibition on the proliferation of Hela nude mice.5.Taxifolin mechanism of antitumor effect of factors: the mechanism of cell death induced by taxifolin was related to cell apoptosis. With regard to the molecular mechanism of apoptosis induced by taxifolin, upregulation of P53 mRNA and P21 mRNA might be involved and no relation between Bcl-2 mRNA/Bax mRNA and apoptosis was observed.6."Relieving food retention" effect of Pharmacodynamics Study: the excitement can extract isolated rabbit intestinal smooth muscle, effect of water extract products is stronger than the other groups; and gastrointestinal function of mice have different levels of promotion effect, effect of ethanol extract of processed products stronger than other groups. The results showed that about "consumer product" effect processed products is stronger than raw materials.7."Alleviating pain" effect of Pharmacodynamics Study: hot plate and acetic acid induced pain, both processed products and raw materials extract varying degrees of analgesic effect, water extract of processed products is stronger than the other groups, has a better analgesic effect .8.Preliminary antioxidant experiment of FPO: raw ethyl acetate extract of a better free radical scavenging effect.9.Acute toxicity test of FPO: the test in accordance with the "approval of new pharmaceuticals", the relevant provisions of the LD50 value not detected, indicating that FPO has no acute toxic effects. |
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