Ntuj Artemisinin Hmoov 63968-64-9

1. Taw qhia

Ntuj Artemisinin Powder 63968-64-9 yog cov nroj tsuag tshuaj uas siv rau hauv cov tshuaj suav tshuaj rau ntau tshaj 2000 xyoo los kho ntau yam kab mob xws li malaria. Artemisinin yog cov khoom tseem ceeb ntawm Artemisia annua extract. Kev rho tawm ntawm artemisinin los ntawm Artemisia annua L. thiab tus cwj pwm ntawm nws cov tshuaj tiv thaiv kab mob hauv xyoo 1970 tau pib los ntawm Suav cov kws tshawb fawb, uas tau suav tias yog ib qho tseem ceeb tshaj plaws hauv kev tswj hwm malaria nyob rau niaj hnub no. Artemisinin hmoov yog siv dav hauv kev lag luam khoom noj, tshuaj thiab tshuaj pleev ib ce.

Artemisin yog ib qho organic compound nrog molecular mis ntawm C15H22O5 thiab txheeb ze molecular hnyav ntawm 282.34. [1]

Artemisinin yog ib tug tsis muaj kob koob siv lead ua nrog ib tug melting point ntawm 156 ~ 157 degree. Nws yog yooj yim soluble nyob rau hauv chloroform, acetone, ethyl acetate thiab benzene, soluble nyob rau hauv ethanol thiab ether, me ntsis soluble nyob rau hauv txias petroleum ether, thiab yuav luag insoluble nyob rau hauv dej. Vim tias nws cov pab pawg tshwj xeeb peroxy, nws tsis ruaj khov rau cov cua sov thiab yooj yim rau decompose nyob rau hauv lub zog ntawm ya raws, cua sov thiab txo cov khoom. [1]

Artemisinin yog cov tshuaj zoo tshaj plaws los kho cov tshuaj tiv thaiv malaria. Kev kho mob ua ke raws li artemisinin kuj yog txoj hauv kev zoo tshaj plaws thiab tseem ceeb tshaj plaws los kho malaria tam sim no. Tab sis nyob rau xyoo tas los no, nrog rau kev tshawb fawb tob zuj zus, lwm yam kev cuam tshuam ntawm artemisinin kuj tau tshawb pom thiab siv ntau dua, xws li tshuaj tiv thaiv qog, kev kho mob ntsws pulmonary, tiv thaiv ntshav qab zib, embryotoxicity, tshuaj tua kab mob, kev tiv thaiv kab mob, tshuaj tiv thaiv kab mob [{{ 1}}], anti-inflammatory, anti pulmonary fibrosis, antibacterial, mob plawv thiab lwm yam pharmacological teebmeem [2].

Thaum Lub Kaum Hli 2015, Tu Youyou yeej 2015 Nobel nqi zog hauv Physiology lossis Tshuaj nrog ob tus kws tshawb fawb txog nws txoj kev koom tes rau kev tsim cov tshuaj tiv thaiv kab mob tshiab - artemisinin thiab dihydroartemisinin. [5

Tshawb nrhiav keeb kwm yav dhau

Malaria yog ib yam kab mob loj tshaj plaws ntawm tib neeg, thiab nws tseem yog ib qho teeb meem tseem ceeb ntawm pej xeem kev noj qab haus huv uas muaj kev txhawj xeeb loj thiab yuav tsum tau daws sai sai hauv ntiaj teb.

Xyoo 1631, tus tub txib Italian Agostino Salumbrino tau txais cov tshuaj zoo rau kev kho mob kub taub hau los ntawm Peruvians hauv South America - cinchonabark, thiab coj nws rov qab mus rau Tebchaws Europe los kho kub taub hau. Tsis ntev, nws tau pom tias cov tshuaj muaj txiaj ntsig zoo rau kev ua npaws tsis sib xws.

Xyoo 1820, Pierre Joseph, kws tshuaj Fab Kis Fab Kis, thiab Joseph Bienaim é Caventou, kws tshawb fawb tshuaj, cais cov khoom muaj txiaj ntsig zoo rau kev kho mob malaria los ntawm cov tawv ntoo ntawm Cinchona thiab muab nws lub npe quinine.

Xyoo 1944, American organic chemists Robert Woodward thiab William Doering tau ua tiav cov tshuaj quinine thawj zaug. Txij thaum ntawd los, cov kws tshawb fawb tau txhim kho cov tshuaj tiv thaiv kab mob tsis tu ncua, tsim cov tshuaj tsw qab thiab heterocyclic methanols sawv cev los ntawm quinine, 4-aminoquinolines sawv cev los ntawm chloroquine, thiab heterocyclic aminophenols sawv cev los ntawm amodiaquine. Cov tshuaj tiv thaiv kab mob malaria no tau ua lub luag haujlwm tseem ceeb hauv kev tswj tib neeg malaria. Txawm li cas los xij, nrog kev siv tshuaj ntau thiab ntev, qhov teeb meem ntawm kev siv tshuaj tiv thaiv kab mob malaria tau maj mam tshwm sim.

Thaum xyoo 1960, Plasmodium falciparum tau tsim kev tiv thaiv chloroquine hauv qee thaj tsam, tshwj xeeb tshaj yog nyob rau sab hnub tuaj Asia. Thaum lub sijhawm ntawd, nrog kev nce zuj zus ntawm Tsov Rog Nyab Laj, kev tawm tsam ntawm chloroquine - resistant falciparum malaria plagued ob tog sib ntaus sib tua, ua rau muaj coob tus txo qis hauv kev sib ntaus sib tua rog. Txog qhov kawg no, Tebchaws Meskas tau nqis peev ntau ntawm tib neeg thiab cov khoom siv los kawm malaria, nrog rau lub hom phiaj tseem ceeb ntawm kev nrhiav tshuaj tiv thaiv kab mob tshiab. Ntawm lawv, Walter Reed Army lub koom haum tshawb fawb ntawm Tebchaws Meskas tau tshuaj xyuas ntau dua 200000 qhov sib txuas txij li xyoo 1960s. Vim muaj qee qhov xwm txheej, Nyab Laj tsis tuaj yeem tsim cov tshuaj tshiab, yog li nws tau thov kom Tuam Tshoj los pab daws cov teeb meem ntawm kev tswj tus kab mob malaria. Sab Suav tau xa cov kws tshawb fawb los ua qhov kev tshawb nrhiav thiab kev pabcuam teb rau ze li ob xyoos, paub txog qhov ceev thiab nyuaj ntawm kev tswj tus kabmob malaria.

Kev tshawb nrhiav ntawm artemisinin

Txij lub Tsib Hlis 21 txog Lub Rau Hli 1, 1971, National Symposium on Malaria Control and Prevention tau tuav hauv Guangzhou. Tom qab lub rooj sib tham, lub koom haum Beijing Institute of Traditional Chinese Medicine reorganized the research team. Tu Youyou tseem yog pab pawg thawj coj, thiab pab pawg Zhong Yurong txuas ntxiv mus rho cov tshuaj suav tshuaj. Lang Linfu thiab Liu Jufu tau ua tsiaj sim. Raws li cov ntaub ntawv soj ntsuam tshuaj ntawm Beijing Institute of Traditional Chinese Medicine, qhov inhibition ntawm artemisinin yog 12 feem pua ​​​​ntawm Lub Xya Hli 26, 1971 (No. 16), 40 feem pua ​​​​ntawm lub Cuaj Hlis 1 (No. 114), thiab 100 feem pua ​​​​ntawm Lub Kaum Hli 4. (No. 191). Txij li thaum Lub Ib Hlis Ntuj xyoo 1971, Tu Youyou pab neeg tau pib rho tawm ntau ntawm ether extract ntawm artemisia annua, thiab ua tiav qhov kev kuaj toxicity ntawm cov dev thaum kawg ntawm lub Rau Hli xyoo ntawd. Txhawm rau ua tiav qhov kev sim tshuaj sai li sai tau, thaum cov txiaj ntsig ntawm kev kuaj tshuaj lom ntawm artemisinin ether extract ntawm cov dev hauv xyoo ntawd tseem muaj kev tsis sib haum xeeb, Tu Youyou, Lang Linfu, Yue Fengxian thiab Zhang Guozhen, Yan Shuchang, Pan Hengjie , Zhao Aihua thiab Fang Wenxian tau ua tiav cov txiaj ntsig nruab nrab ntawm artemisinin ether hauv ob pawg ntawm cov koob tshuaj sib txawv, yam tsis muaj tshuaj lom thiab cov kev mob tshwm sim.

Thaum Lub Peb Hlis 8, 1972, Tu Youyou, uas yog ib tus neeg sawv cev ntawm Beijing Institute of Traditional Chinese Medicine, tau tshaj tawm tsab ntawv ceeb toom hu ua "Siv Mao Zedong Xav Qhia Txog Kev Tshawb Fawb Txog Tshuaj Tiv Thaiv Kab Mob Suav Tshuaj" ntawm lub rooj sib tham ntawm "National 523 Office" hauv Nanjing, thiab tau tshaj tawm cov txiaj ntsig ntawm 100 feem pua ​​​​ inhibition tus nqi ntawm nas malaria thiab liab malaria ntawm qhov nruab nrab crude extract ntawm artemisinin ether, uas nyiam cov neeg tuaj koom. Raws li cov ntaub ntawv, Tu Youyou tau tshwm sim los ntawm cov tshuaj suav tshuaj thiab cov pej xeem hais tias "wring kua txiv". Xav tias cov khoom xyaw zoo tuaj yeem yog nyob rau hauv lipophilic ib feem, nws hloov mus rau ether extraction, uas txhim kho cov tsiaj potency ntawm Artemisia annua los ntawm 30 feem pua ​​​​rau 40 feem pua ​​​​rau ntau dua 95 feem pua.

Thaum Lub Yim Hli 1972, Tu Youyou tau coj ib pab neeg los ua qhov kev sim tshuaj ntsuam xyuas ntawm artemisinin ether neutral extract hauv Hainan Island. Nyob rau lub sijhawm no, Ni Muyun tau tsim kho ua ntej ntawm chromatographic kem sib cais los txhim kho cov nyhuv antimalarial ntawm qhov nruab nrab ntawm ether extract ntawm Artemisia annua dua. Zhong Yurong tau kawm los ntawm cov ntaub ntawv hais tias silica gel kem ua haujlwm zoo dua hauv kev sib cais nruab nrab, yog li nws thiab nws tus pab Cui Shulian siv silica gel kem chromatography thiab gradient elution ntawm roj av ether-ethyl ether (tom qab hloov mus rau roj av ether-ethyl acetate) raws li mus rau txoj kev muab nyob rau hauv cov ntaub ntawv los cais cov nruab nrab ether extract raws li Ni Muyun txoj kev kho mob ua ntej.

Thaum lub Kaum Ib Hlis 8, 1972, silica gel kem uas tsim los ntawm Shanghai Reagent Factory tau siv rau kev sib cais, thiab tom qab ntawd roj av ether thiab ethyl acetate-petroleum ether (sib txawv proportions) tau siv rau elution rau ntau zaus. Ib qho me me ntawm koob zoo li cov muaju yog thawj zaug tau txais, suav nrog "koob siv lead ua kuv" (No.1 lossis koob 1); Tus naj npawb ntawm cov koob zoo li cov muaju eluted tom qab yog "needle crystal II" (No. 2 lossis koob 2); Tom qab ntawd, tau txais lwm cov square siv lead ua, suav "Crystal III" (No.3 lossis square crystal). Thaum pib ntawm lub Kaum Ob Hlis ntawm tib lub xyoo, qhov kev kuaj mob malaria nas tau ua pov thawj tias "koob siv lead ua II" tsuas yog siv tau zoo monomer nrog cov nyhuv antimalarial. Txij thaum ntawd los, thaum lub koom haum Beijing Institute of Traditional Chinese Medicine tau tshaj tawm rau "National 523 Office", nws tau hloov cov khoom muaj txiaj ntsig ntawm kev tiv thaiv kab mob malaria "needle crystal II" rau "artemisinin II", qee zaum kuj hu ua artemisinin. Tom qab ntawd, Beijing Institute of Traditional Chinese Medicine hu ua "artemisinin II" artemisinin.

2.Main Function

1. Antimalarial, artemisinin hmoov muaj kev tua cov kab mob hauv cov qe ntshav liab, nws tuaj yeem cuam tshuam cov kab mob kom loj hlob sai;

2. Antibacterial, artemisinin muaj kev tiv thaiv kab mob khaub thuas;

3. Anti-parasite, artemisinin rau lub luag hauj lwm ntawm anti-schistosomiasis thiab leptospirosis.

3. Daim ntawv thov

1. Ntuj Artemisinin Powder 63968-64-9 siv rau hauv cov zaub mov, artemisinin hmoov tuaj yeem ua cov khoom siv raw ntawm tshuaj yej kom txo qis phlegm;

2. Siv rau hauv kev lag luam tshuaj, nws dhau los ua tshuaj tiv thaiv kab mob qog noj ntshav tshiab uas muaj tshuaj lom tsawg;

3. Siv rau hauv cov tshuaj pleev ib ce, nws tuaj yeem ua kom cov ntshav ncig thiab tshem tawm cov dej haus.

4.Specification

5. Flow Chart

Raw khoom → Ntxuav → Crash → Extract → Lim → Concentrate → Spray qhuav → Test → Packing

Tshuaj synthesis

Synthesis ntawm artemisinin los ntawm R - (ntxiv) - citronellal

Synthesis ntawm artemisinin los ntawm R - (ntxiv) - citronellal [11]

Nyob rau hauv 1983, chemist HofheinzW thiab lwm tus tau tshawb pom cov tshuaj synthesis ntawm artemisinin los ntawm kev tshawb fawb tshuaj. Siv (-) - 2-isobutanol ua raw khoom, qhov nruab nrab tau txais los ntawm kev qhia cov pa oxygen los ntawm cov tshuaj tiv thaiv photooxidation, thiab tom qab ntawd cov khoom kawg tau raug tsim los ntawm cov tshuaj tiv thaiv cyclization. Muaj ob txoj hauv kev txwv tus nqi tseem ceeb hauv kev sib txuas ntawm sesquiterpene lactones: folding thiab cyclization ntawm sesquiterpene niam txiv nuclei; Cov txheej txheem tsim ntawm sesquiterpene lactones uas muaj peroxy txuas hniav.

Xyoo 1986, Suav tus kws tshawb fawb Zhou Weishan tau tsim cov artemisinin los ntawm R - (ntxiv) - citronellal. Txawm li cas los xij, vim muaj cov txheej txheem sib xyaw ua ke nyuaj thiab cov txiaj ntsig qis tag nrho, txawm tias tsawg dua 1 feem pua, qhov kev ntsuas qhov ua tau zoo ntawm kev lag luam tseem tsis tau paub.

Biosynthesis

Artemisinin muaj nyob rau hauv paj thiab nplooj ntawm Suav tshuaj ntsuab Artemisia annua, tab sis tsis nyob rau hauv stems. Nws yog terpene compound nrog cov ntsiab lus tsawg heev, thiab nws txoj kev biosynthetic yog qhov nyuaj heev.

Tam sim no paub tias biosynthesis ntawm artemisinin tuaj yeem ua tau peb txoj hauv kev. Ib qho yog txhawm rau txhim kho cov ntsiab lus ntawm artemisinin los ntawm kev tswj cov enzymes tseem ceeb tswj cov biosynthesis ntawm artemisinin thiab ntxiv cov precursors ntawm biosynthesis; Qhov thib ob yog ua kom cov noob tswj los ntawm cov enzymes tseem ceeb, thiab nce cov ntsiab lus ntawm artemisinin; Qhov thib peb yog siv genetic engineering los hloov cov noob tseem ceeb los txhim kho kev ua haujlwm ntawm cov enzymes lawv tswj.

Nyob rau hauv cov txheej txheem ntawm biosynthesis, cov ntsiab lus ntawm artemisinin yog heev cuam tshuam los ntawm physiological thiab ecological yam xws li lub teeb, exogenous cov tshuaj hormones, bud sib txawv, thiab lwm yam. Kub kuj muaj kev cuam tshuam zoo rau biosynthesis. Los ntawm kev sim kev tshawb fawb, nws pom tias artemisinin cov ntsiab lus ntawm artemisinin seedlings nce mus rau 68 feem pua ​​​​ntawm 40 degree tom qab 36h kho.

Ntxiv nrog rau artemisinin, lwm cov nroj tsuag kuj tuaj yeem tsim cov artemisinin. Hauv xyoo 2011, cov kws tshawb fawb tau tsim cov artemisinin los ntawm kev haus luam yeeb. Piv nrog rau cov txheej txheem tshuaj ib txwm siv, cov tshuaj reagents siv rau hauv txoj kev no tau txo qis heev, uas muaj txiaj ntsig zoo rau kev tiv thaiv ib puag ncig. Lub receptor ntawm no biosynthesis txoj kev yog luam yeeb, uas yog kuj dav nyob rau hauv Tuam Tshoj. Yog li ntawd, lub hauv paus ntawm raw cov ntaub ntawv yog kuj nplua nuj. Txawm li cas los xij, qee cov tshuaj tiv thaiv substrates hauv cov txheej txheem ntawm synthesizing artemisinin los ntawm kev haus luam yeeb tsis meej, thiab yuav tsum tau tsim. Txawm li cas los xij, txoj kev siv hluavtaws no tseem muaj cov ntawv thov kev lag luam zoo. [11]

Ib qho artemisinin noob tau cog rau hauv Escherichia coli, thiab hloov pauv Escherichia coli tsim cov khoom nruab nrab, uas tuaj yeem dhau los ua cov khoom siv raw ntawm artemisinin - artemisinin acid tom qab ob peb kauj ruam ntawm kev kho mob. Tom qab tso cov enzyme tshwj xeeb rau hauv cov poov xab, cov poov xab hloov cov khoom nruab nrab uas tau hais los saum toj no rau hauv artemisinin. Cov saw thev naus laus zis ntawm artemisinin ntau lawm los ntawm kev lag luam microbial tau pib ua cov duab. Qhov no txhais tau hais tias tus nqi ntawm artemisinin yuav poob los ntawm 90 feem pua. [12]

Extraction thiab purification

Kev sib cais thiab kev ua kom huv huv feem ntau suav nrog cov kuab tshuaj pab rho tawm, rho tawm recrystallization, supercritical CO2 extraction thiab hnyav extraction chromatography.

Cov kuab tshuaj extraction thiab recrystallization txoj kev feem ntau yog siv cov kuab tshuaj roj txoj kev, ethanol txoj kev thiab alkali dej extraction thiab acid los nag txoj kev rau ntau lawm, uas ho nce tus nqi siv zoo ntawm artemisinin nroj tsuag.

Alkali dej extraction thiab acid nag lossis daus txoj kev: coj ib tug npaum li cas ntawm qhuav hmoov ntawm Artemisia annua ceg thiab nplooj thiab ntxiv rau ethanol rau nplawm thiab extraction kom tau cov ethanol extraction tov, qhuav nws nyob rau hauv txo siab, thiab yaj nyob rau hauv lub ether- dej ob-theem daws kom tau artemisinin thiab artemisinin feem. Cov txiaj ntsig ntawm artemisinin nyob rau hauv txoj kev no yog 90 feem pua, thiab tus nqi rho tawm ntawm artemisinin yog 57 feem pua.

Txoj kev Ethanol: noj cov hmoov qhuav ntawm Artemisia annua ceg thiab nplooj, tsau nws hauv dilute ethanol rau 24 teev, tau txais cov ethanol extract, txhaj rau hauv cov khoom siv txuas ntxiv, thiab tom qab ntawd muab rho tawm nrog cov roj hnyav uas muaj benzene thiab ethyl. acetate kom tau txais cov dej cawv theem thiab lub sijhawm rho tawm, uas tuaj yeem rov ua dua tshiab, cov txheej txheem rho tawm yog decolored nrog cov pa roj carbon activated, lim, thiab cov kuab tshuaj tau zoo, thiab tom qab ntawd tau txais cov tshuaj concentrated, thiab tom qab ntawd txias thiab crystallize kom tau txais cov siv lead ua ntxhib. ntawm artemisinin, thiab tom qab ntawd recrystallize nrog ethanol kom tau cov artemisinin tiav. Txoj kev no muaj qhov zoo ntawm cov txiaj ntsig siab, tus nqi qis, cov kauj ruam tsawg, kev ua haujlwm yooj yim thiab kev nyab xeeb.

Txoj kev roj av hnyav: noj qee yam ntawm cov hmoov qhuav ntawm Artemisia annua ceg thiab nplooj, tsau nws hauv 8 ~ 10 zaug ntawm 120 # hnyav roj av rau 3 zaug, tau txais cov roj av hnyav, tom qab ntawd decompress thiab mloog zoo rau nws thiab muab tso rau crystallization. , tau txais cov artemisinin crude, ntxuav nws nrog me me ntawm 120 # hnyav roj av rau ntau zaus, thiab crystallize 50 feem pua ​​​​ethanol cawv rau 2 ~ 3 zaug, thaum kawg tau txais cov koob dawb siv lead ua ntawm artemisinin. Txoj kev no yog qhov yooj yim thiab siv tau yooj yim hauv kev tsim khoom loj.

Muaj peb txoj kev rho tawm rau cov kuab tshuaj extraction chromatography, uas yog, acetone - silica gel kem chromatography, qis boiling roj av - ultra-luv coarse spherical expanded silica gel chromatography, thiab ethane extraction - ethane / acetonitrile - silica gel kem chromatography.

6. Kev tsim nyog

Tom qab xyoo ntawm kev tsim khoom, peb lub tuam txhab tau txais cov ntawv tso cai tsim khoom tsim nyog.

7 Patent cov ntsiab lus

Tom qab ntau xyoo ntawm kev ua haujlwm nyuaj, Kono Chem Co., Ltd tau txais ntau cov patented technologies.

Hauv qab no yog tus lej patent:

CN113527166A

CN112934445A

CN213006706U

CN212731128U

CN212576285U

CN212467595U

CN212467207U

PIB CN112961024A

8 Tus khub

Peb muaj ntau tus neeg koom tes mus sij hawm ntev thoob plaws ntiaj teb.

9 Cov neeg siv khoom xyuas

Peb tau txais kev qhuas ntau ntawm lwm lub platform, thiab peb cov neeg siv khoom tau zoo siab heev ntawm cov khoom tsim los ntawm peb lub tuam txhab.

10 Chav kuaj thiab lub Hoobkas ib puag ncig

11 Exhibition

Peb lub tuam txhab koom nrog ntau yam kev nthuav qhia hauv tsev thiab txawv teb chaws txhua xyoo, thiab sib txuas lus nrog cov neeg siv khoom ntsej muag.

Cim npe nrov: ntuj artemisinin hmoov 63968-64-9, manufacturers, lwm tus neeg, Hoobkas, lag luam wholesale, yuav, nqe, zoo tshaj plaws, tej, kev muag khoom