Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm d-tetrandrine cas 518-34-3 hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo d-tetrandrine cas 518-34-3 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
D-Tetrandrineyog ib qho tshuaj lom neeg muaj zog dianilide isoquinoline alkaloid nrog cov haujlwm tseem ceeb ntawm cov tshuaj. Nws yog tsuas yog muab rho tawm los ntawm cov hauv paus hniav ntawm cov tsoos suav tshuaj cog Aconitum dianthum. Nws cov qauv molecular yog complex, tus yam ntxwv los ntawm kev sib txuas ntawm ob isoquinoline units los ntawm ib tug ether daim ntawv cog lus, nthuav qhia ib tug tshwj xeeb stereoconfiguration, uas ncaj qha txiav txim qhov tshwj xeeb ntawm nws pharmacological teebmeem. Cov tshuaj no feem ntau tshwm sim ua dawb rau tawm -dawb crystalline hmoov, tsis muaj ntxhiab tsw thiab iab me ntsis hauv saj, thiab muaj kev ua haujlwm zoo hauv cov kuab tshuaj organic xws li chloroform lossis ethanol.Apart from nws cov peev xwm kho tau ncaj qha, nws kuj tseem suav tias yog cov cuab yeej siv tshuaj rau kev kawm calcium ion- kho kom haum xeeb ntawm lub cev, xws li daim siab ua haujlwm. thiab lub raum toxicity, qhia txog qhov nyuaj ntawm cov txiaj ntsig thiab kev pheej hmoo thaum cov khoom ntuj siv los ua tshuaj.
|
Tshuaj Formula |
C38H42N2O6 |
|
Exact Mass |
622 |
|
Molecular Luj |
623 |
|
m/z |
622 (100.0%), 623 (41.1%), 624 (8.2%), 624 (1.2%) |
|
Elemental Analysis |
C, 73.29; H, 6.80; N, 4.50; O, 15.41 |
D-powafimazine yog qhov paub zoo tshaj plaws rau nws cov uas tsis yog - xaiv calcium channel blockade pharmacological nyhuv, uas tuaj yeem cuam tshuam cov calcium ion influx, yog li ua kom cov leeg nqaij du thiab txo qis peripheral vascular kuj. Qhov no ua rau nws yog ib qho tseem ceeb hauv kev kho mob ntshav siab. Tsis tas li ntawd, kev tshawb fawb dav dav tau nthuav tawm nws cov kev ua haujlwm tshuaj muaj peev xwm xws li tshuaj tiv thaiv- mob, tiv thaiv-fibrotic, immunosuppressive, thiab tiv thaiv- qog cov teebmeem, nrog rau cov txheej txheem cuam tshuam nrog kev tswj hwm ntawm ntau lub xov tooj ntawm tes taw qhia txoj hauv kev, xws li NF-κB thiab MAPK txoj hauv kev.
D-TetrandrineSiv:
1. Siv cov kab mob hauv lub cev
Raws li lub ntuj alkaloid nrog kev ua haujlwm ntawm immunomodulatory, D-tetrandrine nthuav tawm cov teebmeem cuam tshuam tseem ceeb ntawm kev mob ntawm kev mob caj dab. Nws tuaj yeem txo qhov o ntawm qhov sib koom ua ke, txo cov lus teb inflammatory, thiab txhim kho cov tsos mob hauv cov xwm txheej. Cov kev tshawb fawb Pharmacodynamic tau pom tias nws txoj kev kho mob muaj zog dua li cov tshuaj aspirin, txhawb nqa nws daim ntawv thov kev kho mob raws li ib qho ntxiv los yog lwm tus neeg sawv cev rau kev kho mob rheumatoid mob caj dab thiab lwm yam kev tiv thaiv kab mob - cuam tshuam txog kev sib koom tes.
2. Siv nyob rau hauv cov kab mob plawv
D-tetrandrine muaj cov calcium antagonistic tseem ceeb hauv cov hlab plawv. Nws tuaj yeem cuam tshuam ob qho tib si T- hom thiab L- hom calcium channels hauv ventricular myocytes, cuam tshuam nrog M receptors, thiab thaiv cov calcium- qhib cov poov tshuaj. Los ntawm cov txheej txheem ntau- lub hom phiaj no, nws pab tswj lub plawv hluav taws xob ua haujlwm thiab ua kom lub plawv dhia tsis zoo, muab lub tswv yim zoo thiab muaj txiaj ntsig zoo rau kev tswj hwm ntawm paroxysmal supraventricular tachycardia.
3. Siv nyob rau hauv cov kab mob digestive system
Hauv kev zom zaub mov, D-tetrandrine tiv thaiv cov kab mob hepatocytes thiab tiv thaiv kev hloov pauv ntawm daim siab pathological. Nws tuaj yeem txo qhov kev puas tsuaj ntawm hepatocyte los ntawm ntau yam kab mob, inhibit qhov ua kom lub siab ntawm cov hlwb, thiab txo cov collagen deposition. Yog li ntawd, nws ua lub luag haujlwm zoo hauv kev tiv thaiv daim siab fibrosis thiab tswj lub siab lub cev thiab kev ua haujlwm, uas qhia txog qhov muaj txiaj ntsig ntawm kev tiv thaiv lub siab ntev.
4. Siv cov kab mob Ocular Inflammatory
D-tetrandrine kuj tseem siv rau hauv kev kho mob ntawm ntau yam kab mob ntawm lub qhov muag. Nws tuaj yeem cuam tshuam cov tshuaj tiv thaiv hauv zos, txo cov ntaub so ntswg edema thiab exudation, thiab txhim kho ocular microcirculation. Cov ntawv thov kev kho mob suav nrog kev tswj hwm ntawm uveitis, keratitis, thiab qee yam retinopathies vim yog qhov ua rau mob, pab txo qhov tsis xis nyob thiab tiv thaiv kev ua haujlwm ntawm qhov muag.
5. Lwm yam kev siv tshuaj kho mob
D-tetrandrine qhia pom tseeb qhov kev tawm tsam tiv thaiv tus mob nephrotoxicity tshwm sim los ntawm streptomycin. Nws tuaj yeem txo cov apoptosis thiab kev loj hlob txawv txav ntawm lub raum tubular epithelial hlwb, yog li tiv thaiv lub raum ua haujlwm thiab txo lub raum raug mob los ntawm mob ischemia-reperfusion. Tsis tas li ntawd, nws txo qis cov ntshav creatinine thiab urea nitrogen ntau ntau, txhim kho glomerular pom tus nqi thiab lub raum plasma ntws, thiab ncua kev loj hlob ntawm glomerulosclerosis, nthuav tawm qhov tseem ceeb hauv kev tiv thaiv lub raum.
Synthesis ntawmD-tetrandrine:
Tus txheej txheem belongs rau kev teb ntawm cov tsoos suav tshuaj extraction, thiab tshwj xeeb tshaj yog muaj feem xyuam rau txoj kev npaj ntawm tetrandrine. Txoj kev npaj ntawm tetrandrine yog raws li nram no: tom qab cov tshuaj crude ntawm tetrandrine yog crushed, nws yog muab rho tawm los ntawm ethanol reflux, ua ke nrog cov extract, thiab purified los ntawm AB - 8 resin kem chromatography tom qab txo siab concentration, ua raws li elution chromatography nrog purified dej, 50% ethanol, 9% thiab 80% ethanol, ces 80% ethanol. 80% ethanol thiab 95% ethanol elution yog sau thiab concentrated nyob rau hauv lub siab txo, thiab ces ntxiv purified los ntawm nruab nrab alumina kem chromatography, thiab cov elution yog tau los ntawm dichloromethane elution chromatography kem, Cov purified tetrandrine tau los ntawm recrystallization nrog acetone tom qab concentration. Txoj kev npaj ntawm tetrandrine muab los ntawm txoj kev no yog qhov yooj yim, ua haujlwm tau zoo, thiab muaj txiaj ntsig siab extraction. Nws tuaj yeem tau txais cov ntshiab tetrandrine nrog purity ntau dua 99%, thiab tsis siv cov kuab tshuaj organic xws li benzene thiab chloroform. Nws yog ntsuab thiab lub zog-txuag, thiab tsis muaj kev pheej hmoo ua mob rau tib neeg noj qab haus huv.
Extraction thiab cais ntawmd-tetrandrine:
1. Extraction ntawm tag nrho alkaloids thiab kev sib cais ntawm lipophilic thiab hydrophilic alkaloids
Tetrandrine yog alkaloid, thiab cov khoom siv cog yog tetrandrine (hauv paus). Lub hauv paus ntsiab lus ntawm kev rho tawm thiab kev sib cais yog cov ntsiab lus siab lossis cov khoom tseem ceeb thiab kev sib cais sib txawv, uas yog hu ua acid water percolation. Txoj kev sib cais yog raws li nram no:
2. Kev sib cais ntawm tetrandrine A thiab B los ntawm qis qis qis chromatography
Nyob rau hauv lub siab tsis tshua muaj siab (0.5 ~ 3kg / cm2, feem ntau 0.3 ~ 1.2kg / cm2), particle inch ntawm tsis tshua muaj siab kem chromatography yog nyob nruab nrab ntawm 100 ~ 200 μ m) Thiab HPLC (- 37 μ m) Silica gel (los yog alumina) H los yog G (50 - 75 μ m) Raws li ib tug sib cais tus neeg sawv cev kem, ib tug sib cais kem, ib tug LC. kuj tseem nyob nruab nrab ntawm kab ke classical thiab HPLC. Lub kem yog ntim los ntawm txoj kev qhuav ntawm decompression, txheej yog nruj thiab sib xws, thiab kev faib tawm ntawm chromatographic bands yog centralized thiab zoo huv si. Nyob rau tib lub sij hawm, qhov zoo tshaj plaws kev sib cais hnyav system ntawm nyias txheej chromatography tuaj yeem siv ncaj qha rau qis qis qis chromatography. Nws yog ib txoj kev uas muaj kev sib cais zoo, cov cuab yeej siv yooj yim, ua haujlwm yooj yim thiab ceev. Haum rau kev npaj tsis tu ncua sib cais ntawm cov khoom ntuj tsim.
(1) Kem mounting
Decompression qhuav packing txoj kev, chromatographic kem specification: kem ntev yog 30cm, puab txoj kab uas hla yog 2cm, tag nrho silica gel yog hais txog 30g (qhov siab yog hais txog 22cm), 2.2 qauv sib tov thiab coj mus kuaj ntxiv txog 150mg ntawm tetrandrine, ntxiv ib me me ntawm acetone rau kub dissolution ntawm 1 degrees (just). gel nrog ib tug dropper, ua tib zoo sib tov, evaporate nyob rau hauv dej da dej, grind nws, ua tib zoo ntxiv nws mus rau sab saum toj ntawm kem los ntawm ib tug ntev - caj dab funnel, maj mam thiab vertically ntaus nws, thiab npog nws nrog txog 1 ~ 2cm siab dawb paug silica gel thaum lub nto ntawm tus qauv yog tiaj tus thiab tsis do, ces npog ib ncig daim ntawv lim thiab nias nws nruj nreem.
(2) Kev ntseeg
Ua ntej xyuas seb cov raj xa dej los ntawm lub tshuab cua compressor mus rau chromatographic kem yog qhov qub, kaw tag nrho cov li qub, thiab pib lub tshuab cua compressor rau qhov ntsuas siab (5.8kg / cm2) rau kev siv. Ua tib zoo ntxiv me me ntawm eluent (cyclohexane-ethyl acetate-diethylamine/6:2:0.8) rau sab phab ntsa ntawm kem nrog lub dropper. Thaum cov kua qib nce mus txog qhov siab, ntxiv cov khoom seem ntxiv (txog 250ml hauv tag nrho), ceev nrooj nruab ib lub iav txheem ntsaws txuas rau sab saum toj ntawm kem, nias nws nruj nreem nrog cov hlua hlau (kom tiv thaiv lub qhov txuas los ntawm dej ntws tawm thaum lub zog), ua tib zoo qhib lub tshuab cua compressor valve, thiab tom qab ntawd qhib lub koob valve thiab cua lim reducer, (Ceeb toom: Lub iav siab yuav ua rau muaj kev nyab xeeb heev. daim npog qhov ncauj yog tias tsim nyog.) Kho qhov xav tau siab rau 0.6 ~ 1.2 kg / cm2, thiab nws yuav ntws tawm tom qab li 40 feeb. Tswj tus nqi ntws ntawm 1 ml / min, thiab sau 12 ~ 15 feem txhua 10 feeb. Tag nrho cov txheej txheem ntawm elution yog li 3 teev.
(3) Tshawb xyuas
Txhua tus kwj tau raug xa mus rau hauv lub khob me me evaporator, tsom rau ntawm lub da dej, thiab dhau TLC tshuaj xyuas raws li. Adsorbent: silica gel G, txhim kho tus neeg sawv cev: cyclohexane ethyl acetate diethylamine / 6: 3: 1, hloov kho bismuth potassium iodide reagent xim xim, tetrandrine A thiab B tau siv los ua tus qauv tswj, thiab cov khoom qub tau muab tso ua ke kom tau cov khoom nyoos A thiab B, recrystallized nrog acetone, thiab
Xyoo 1951, Suav cov kws tshawb fawb tau cais ib qho chaw nrog kev ua haujlwm tshuaj los ntawm Chuanwu, thiab tom qab kawm nws, txiav txim siab nws cov qauv thiab hu ua "Tetrandrine". Lub npe los ntawm lub npe ntawm botanist TT Yu thiab Latin lub hauv paus 'andr -', lub ntsiab lus 'txiv neej', qhia tias nws yog muab rho tawm los ntawm txiv neej cov ntaub so ntswg.
Tom qab ntawd, cov kws tshawb fawb tau tshawb pom muaj ob lub teeb pom kev zoo ntawm Tetrandrine:D-Tetrandrinethiab L-Tetrandrine. Cov qauv molecular ntawm ob isomers yog tib yam, tab sis lawv cov kev ua haujlwm kho qhov muag txawv. D-cov khoom muaj cai-xa khoom, thaum L-Tetrandrine tau sab laug- cov khoom siv tes.
Txhawm rau kom paub qhov txawv ntawm ob isomers no, lub zej zog kev tshawb fawb tau pib ua ntej lawv nrog "D -" lossis "L -" los qhia lawv cov khoom siv kho qhov muag. Yog li ntawd, nws yog txoj cai -tes Tetrandrine, thaum L-Tetrandrine yog sab laug-tes Tetrandrine.
Lub hom phiaj ntawm kev ntxiv cov khoom siv kho qhov muag ua ntej hauv kev naming yog piav qhia cov qauv thiab cov khoom ntawm cov tebchaw kom raug thiab zam kev tsis meej pem. Txoj kev naming no muaj nyob rau hauv cov organic chemistry thiab tuaj yeem pab cov kws tshawb fawb thiab cov kws tshawb fawb kom paub meej thiab piav qhia txog cov tebchaw sib txawv.
Hauv cov ntsiab lus, nws yog dextral isomer ntawm Tetrandrine, thiab nws cov npe keeb kwm tshwm sim los ntawm kev sib cais thawj zaug thiab kev txheeb xyuas ntawm qhov sib xyaw no. Los ntawm kev paub qhov txawv ntawm qhov kev sib hloov kho qhov muag, lub zej zog kev tshawb fawb tuaj yeem piav qhia meej dua thiab kawm txog cov yam ntxwv thiab kev ua haujlwm tshuaj ntawm ob isomers.
Cov kev mob tshwm sim ntawm cov tshuaj no yog dab tsi?
Gastrointestinal tsis xis nyob:Cov tshuaj no tuaj yeem ua rau cov tsos mob digestive xws li xeev siab, ntuav, thiab tsis xis nyob hauv plab. Qhov no tej zaum yuav yog vim lub stimulating nyhuv ntawm cov tshuaj nyob rau hauv lub plab hnyuv mucosa.
Neurological cov tshuaj tiv thaiv:Qee cov neeg mob tuaj yeem ntsib cov tsos mob xws li kiv taub hau, mob taub hau, thiab tsaug zog tom qab siv cov tshuaj no. Qhov no tej zaum yuav muaj feem xyuam rau inhibitory nyhuv ntawm cov tshuaj nyob rau hauv lub paj hlwb.
Lub ntsej muag pigmentation:Lub sij hawm ntev los yog siv ntau dhau ntawm qhov sib xyaw no tuaj yeem ua rau lub ntsej muag pigmentation, cuam tshuam rau kev zoo nkauj ntawm daim tawv nqaij. Qhov no tej zaum yuav muaj feem xyuam rau cov tshuaj ntawm daim tawv nqaij thaum lub sij hawm metabolism thiab excretion nyob rau hauv lub cev.
Cov teebmeem ntawm lub siab thiab lub raum ua haujlwm:Cov tshuaj no yuav tsum tau metabolized thiab tawm los ntawm daim siab thiab ob lub raum, yog li nws yuav muaj qee yam cuam tshuam rau daim siab thiab lub raum ua haujlwm. Tshwj xeeb tshaj yog rau cov neeg mob uas muaj lub siab thiab lub raum tsis ua haujlwm, yuav tsum tau them nyiaj ntxiv thaum siv nws.
Kev tsis haum tshuaj:Cov neeg mob tsawg heev tuaj yeem ntsib kev tsis haum rau cov tshuaj no, tshwm sim ua pob liab liab, khaus khaus, ua pa nyuaj, thiab lwm yam tsos mob. Thaum muaj kev tsis haum tshuaj tshwm sim, cov tshuaj yuav tsum tau nres tam sim ntawd thiab yuav tsum tau nrhiav kev kho mob.
Lwm yam kev mob tshwm sim:Ntxiv nrog rau cov kev mob tshwm sim uas tau hais los saum toj no, cov tshuaj no kuj tseem tuaj yeem ua rau lwm yam kev mob tshwm sim, xws li palpitations, hauv siab nruj, thiab txo cov ntshav siab. Cov kev mob tshwm sim no tuaj yeem cuam tshuam nrog kev cuam tshuam ntawm cov tshuaj ntawm cov hlab plawv.
D-Tetrandrine yog bisbenzylisoquinoline alkaloid nrog ntau hom tshuaj ua haujlwm thiab muaj peev xwm siv tshuaj kho mob. Nws cov calcium channel- thaiv, tiv thaiv- mob, tiv thaiv- mob qog noj ntshav, tiv thaiv-fibrotic, thiab cov teebmeem neuroprotective ua rau nws muaj txiaj ntsig zoo rau kev kho mob ntawm ntau yam kab mob, suav nrog cov kab mob plawv, kab mob inflammatory thiab autoimmune, mob qog noj ntshav, mob fibrotic, thiab cov kab mob neurological. Txawm li cas los xij, kev tshawb fawb ntxiv yog xav tau los ntsuas nws txoj kev ua tau zoo thiab kev nyab xeeb hauv tib neeg, nrog rau kev daws teeb meem xws li bioavailability tsis zoo, muaj peev xwm toxicity, thiab kev cuam tshuam tshuaj. Raws li kev tshawb fawb ntawm D-tetrandrine txuas ntxiv mus, nws yuav zoo li tias peb yuav nkag siab tob txog nws cov txheej txheem ntawm kev ua thiab cov kev siv muaj peev xwm, ua rau txoj hauv kev rau kev txhim kho cov tswv yim kho tshiab.
Cim npe nrov: d-tetrandrine cas 518-34-3, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom