Investigation On The Chemical And Bioactive Constituents Of Isodon Excise

Isodon is a genus of the Labiatae family.About 150 species were found in the world,but there are 111 species in China.I excise(maxim)hara is one of the Isodon and is mainly distributed in Northeast region of China,North Korea and far east region of Russia.The whole plant is mainly used for treatment of antifeberile and stomachic.The main chemical compositions from Isodon excise are diterpenoids constituents.Since 1981,11 diterpnoids were separated from Isodon excisa.The study of pharmacology tests in vitro showed that diterpenoid constituents from isodon excisa can markedly inhibit KB cells(human rhinopharyngocele)and hela cells(human venter cancer).Aslo the pharmacology tests in vivo showed that they have obvious effect in anti S-180(sarcoma 180),EAC(ascites cancer)and PS(P388 lymph leucocythemia).In order to thoroughly study on chemical and biology activity of Isodon excisa, chemical constituents from Isodon excisa of this paper were extracted,separated and identified chemical structure.And their pharmacological activities were researched by vitro and vivo.This paper had six chapters.The first is simply summarized that chemical constituents from Isodon and Isodon excisa had pharmacological activity and the chemical analysis technology applied in herbal medicine.From 1954,Japanese researchers isolated enmein which was showed activity against bacteria.With isolating many ent-kaurane diterpenoids from Isodon,except againsting tumour,bacteria, inflammatory and oxidation,,many diterpenoids have effect of cytotoxicity,inhibited oxiodative phosphorylation of mitochondria,insect antifeedant,plant growth regulators, anti-inflammatory and cardiovascular system.Isodon excisa is the popular folk medicine which is use of stomach and helminthic and treats traumatic injuries,snake bite,toxin,anti anti-inflammatory and defervescence.It can cure enteritis,diarrhea, ague,icterus- hepatitis,throat-gall,amygdalae etc.Especially,Rabdosia rubescens are produced henan province,which are not only treatment of antibacteria and anti-inflammtory but also gullet cancer and cardiac cancers.With more studying biology activity,human centralizedly researched isolating chemical constituents and identifying structure of constituents,but less researched pharmacology activities.Second chapter is that volatile and other chemical constituents were extracted from Isodon excisa and studied anti-inflammatory and analgesic of them.Volatile oil was extracted by water-steam distillation from different month of Isodon excisa.Chemical compositions of volatile oil were separated and identified by gas chromatography-mass spectrometry(GC-MS).Every constituent was got by Xcalibur MS workstation and NIST02 datebase at the same time to refer relative literature.The relative contents in the oil were determined by area normalization.68 peaks were separated and 27 compounds were identified,constituting 43.30%of the total peak area.The major components of their volatile oils were mainly oxy-derivative and minority of hydrocarbon. Pharmacological results:(1)Aspirin group and volatile oil groups(0.028mL/kg, 0.055mL/kg,0.100mL/kg)had markedly signified to compare blank group by t-test. Inhibition rates were 35.31%,40.83%and 52.66%and pharmacology effect enhanced by adding dose of volatile oil;(2)Cortisol group and volatile oil groups(0.028mL/kg, 0.055mL/kg)had markedly signified to compare blank group by t-test and inhibition rates were 44.36%and 26.72%.This is indicated that the volatile oil from Isodon excisa have anti-inflammatory and analgesic marked effects.In addition,material of the stems and leaves of Isodon excisa,there were five constituents by TLC,silica gel columniation and HPLC.The three ent- ent-kaurane diterpenoid compounds are Kamebakaurin,Kamebanin and Ursolic acid,which were identified by NMR and IR and refer to some literatures.Third chapte,nine inorganic elements from Isodon excisa were mensurated by inductively coupled plasma mass spectroscopy(ICP-MS).Nine inorganic elements are Al,K,Ca,Mg,V,⁵⁶Fe,⁵⁷Fe,Zn.The content of elements Separated 0.318,0.264,0.129, 0.072,0.025,0.0102,0.0187,0.0744(μg·g^-1)etc(picked benxi city).To extract amylase from Isodon excisa by chemical method,which was studied pharmacology by xylene-induced ear edema and HAC-induced peritoneal in mice.Amylase pharmacology compared with the total of diterpenoid,solution extracted by water and ethanol.Result found that amylase,the total of diterpenoid,solution extracted by water and ethanol had remarkable anti-inflammatory effect.But solution extracted by water had more remarkable anti-inflammatory effect and can inhibit primeval inflammatory,amylase, the total of diterpenoid,solution extracted by ethanol had no difference inhibition effect.Fourth chapter,anti-tumour effect of the total diterpenoids from Isodon excisa was tested by MTT method in vitro.It is showed that 100mg·kg^-1and 200mg·kg^-1(correspond to mice acute toxicity LD50 of 1/25,1/12.5)can inhibit mice Lewis lung cancer and melanoma B₁₆in a dose-dependent manner.Therefore,more research Isodon excisa have exploitation foreground to antitumour medicine.Fifth chapter,different place of Isodon excisa compared their pharmacology effect. At the same time,choosing the part of extracted by methanol,constructing A fingerprint of Isodon excisa decoction pieces was established by HPLC and linearity method calculated character peaks of similarity.Herb fingerprint is developing to control herb quality mode.Comparing with single or minority of main components as control herb quality index,fingerprint can systemically,holistically,stably,roundly reflect vivo quality of medicine plant.The resource of Isodon excisa disturbs widely,which result in nonstandard,various quality of medicine plant.In order to avoid affecting exploitation owing to quality difference of Isodon excisa,it need build technology method which seriously controls medicine plant quality.Similarity standards to similar range between sample and contrast fingerprint and synthesizes quality and quantity message of sample. According to test result,every time Isodon excisa have similarity fingerprints to contrast, which reflects homology and can study qualitatively.Compared with contrast,the similarity of every time was(from big to small)0.9908(wulong mountain in Aug)＞0.9888(xibing mountain in Sep)＞0.9822(tanggou mountain in Aug)＞0.9798(tanggou mountain in Sep)＞0.9728(xinbing mountain in Aug)＞0.9681(tanggou mountain in Jul)＞0.9629(qi mountain in Aug)＞0.9435(fenghuang mountain in Aug).They relate to their activity content and reflect vivo quality difference of different place(different month).Sixth chapter,at premise of tradition theories and taking medicine,at base of prime clinic,we combined modern pharmacology fruit and developed pure herb preparation-yanbixiao capsule.Yanbixiao capsule used to treat tussis,purging fire, effusion,anti-inflammatory and anti-virus effect.By applying eight years of No 202 people liberation army of the hospital,it have gained satisfaction curative effect of treatment periodontitis,gingivitis,throat gall,mouth inflammation and upper respiratory tract inflammation.For the sake of more systemically observing clinic effect,(1)Treatment acute amygdalae inflammation contrasts Penicillin;(2)treatment acute pharynx inflammation contrasts yanhouling.Compare to clinic cases,it have obtained well satisfaction.It is main characters that it has swift sorbability,remarkable effect,true curative effect,no badness reflection,economy,convenience and strong clinic practicality.Therefore,it has value in application of anti-inflammatory herb medicine.