Meiyuan Qian, Yheefeng Tan, Bo Xu
Daim Ntawv Thov R & D Center
Lub hauv paus rau phau ntawv
Cov tub txhab nyiaj (cov tub ntxhais mos chinenis lossis Suav Yew) yog cov ntoo tsiaj qus tiv thaiv los ntawm lub teb chaws. Nws yog qhov muaj tsawg thiab muaj kev puas tsuaj cog rau sab laug los ntawm cov pas dej hiav txwv. Nws tseem yog tsob ntoo muaj txiaj ntsig ntuj nyob hauv lub ntiaj teb. Cov tub ceev nyiaj tau faib rau hauv qhov ntsuas kub ntawm sab qaum teb hemisphere mus rau thaj av me me, nrog rau 11 hom nyob hauv lub ntiaj teb. Muaj 4 hom thiab 1 Ntau yam nyob hauv Suav teb, uas yog Yunnan Carnus, Taxus, Tibetan Carnus thiab Yav Qab Teb Crailus. Cov tsib hom no tau faib rau hauv Southwest Suav teb, sab qab teb Tuam Tshoj, Central Tuam Tshoj, Sab Hnub Tuaj, Northeast Suav thiab Taiwan. Cov nroj tsuag tus tub ceev xwm muaj cov khoom siv sib xyaw, flavonoids, ligans, stericics, sesquarpenes thiab glycosides. Lub npe nrov tiv thaiv kev txiav nyiaj se (lossis paclitaxel) yog hom channel. Cov neeg hla hiav txwv muaj cov tshuab anticancer. Cov neeg them se tawm tau "khov" microTubules los ntawm kev sib txuas nrog cov microlotubules thaum lub sijhawm kev tuag, tshwj xeeb tshaj yog muaj kev sib cais kho mob cell, tshwj xeeb tshaj yog cov ntshav tawm suab nrov [1]. Tsis tas li ntawd, los ntawm kev ua kom ua kom haum, cov tsheb se yuav txo qis hauv TNF-α (li kev tawm ntawm TNF-α, yog li tua cov qog nqaij hlwb [2]. Ntxiv mus, cov tsheb thauj khoom tuaj yeem ua rau apoptotic los ntawm kev ua yeeb yam ntawm apoptotic reciat los ntawm Fas / Fasl lossis ua kom lub Cysteine Protteace System [3]. Vim nws ntau lub hom phiaj anticancer nyhuv, seascer cancer, cov qog nqaij hlav cancer, maltrict Melanoma, lub caj dab mob cancer mis, thiab lwm yam [4]. Cancer mis tshwj xeeb yog cov kab mob cancer mis thiab qib siab zes qe menyuam, yog li ntawd nws yog qhov kev tiv thaiv kab mob kawg rau kev kho mob cancer ".
Cov tsheb tavxol yog cov tshuaj tiv thaiv yeeb tshuaj ntau tshaj plaws hauv kev ua lag luam thoob ntiaj teb nyob rau hauv cov tshuaj tsis ntev los no thiab yog ib qho ntawm cov tshuaj anticancer zoo tshaj plaws rau tib neeg 20 xyoo tom ntej. Nyob rau hauv xyoo tsis ntev los no, nrog kev loj hlob tawg ntawm cov pej xeem thiab mob qog noj ntshav, qhov kev thov uas tau nce ntau. Tam sim no, cov se yuav xav tau rau cov kev tshawb fawb lossis kev tshawb fawb yog feem ntau muab rho tawm ncaj qha los ntawm cov tuam txhab. Hmoov tsis zoo, cov ntsiab lus ntawm cov neeg sau se hauv cov nroj tsuag yog tsawg. Piv txwv li, cov ntsiab lus se tsuas yog 0.069% hauv cov tawv ntoo ntawm cov tub ceev xwm Brevifolia, uas yog feem ntau suav tias yog cov ntsiab lus siab tshaj plaws. Rau qhov extraction ntawm 1 g ntawm cov tuam txhab, nws yuav tsum muaj txog 13.6 kg ntawm cov tub ceev xwm bark. Raws li qhov kev kwv yees no, nws yuav siv 3 - 12 tus tub ceev xwm uas muaj ntau tshaj 100 xyoo los kho tus neeg mob zes qe menyuam. Raws li qhov tshwm sim, ntau tus ntawm cov tsheb pob nyiaj ntau tau txiav, ua rau ze tu ncua rau hom tsiaj no. Ib qho ntxiv, tus tub txhab nyiaj tsis zoo heev hauv cov peev txheej thiab maj mam nyob hauv kev loj hlob, uas ua rau nws nyuaj rau kev loj hlob ntxiv thiab siv cov neeg ua se.
Tam sim no, tag nrho cov khoom siv hluav taws xob ntawm cov neeg ua haujlwm tau ua tiav tiav. Txawm li cas los xij, nws txoj kev hluavtaws yog cov nyom heev thiab muaj txiaj ntsig, ua rau nws tsis muaj qhov tseem ceeb. Cov qauv hluavtaws ib nrab ntawm cov neeg ua se tam sim no yog tam sim no tau txiav txim siab tau yog ib txoj hauv kev zoo los nthuav tawm lub chaw sau se ntxiv rau kev cog qoob loo tsim. Luv luv, nyob rau hauv lub syni-synthesis ntawm cov neeg sau se, cov se tau ntau dua thiab tom qab ntawd hloov pauv mus rau hauv cov tuam txhab tshuaj lom neeg. Cov ntsiab lus ntawm 10-dacetylbaccatin ⅲ nyob rau hauv lub koob ntawm Carnus Baccata tuaj yeem nce mus txog 0.1%. Thiab cov koob tau yooj yim rau kev hloov kho dua piv nrog cov tawv ntoo. Yog li ntawd, synthesis ntawm cov neeg sau se raws li 10-deacetylbaccatin ⅲ yog nyiam ntau thiab ntau dua los ntawm cov kws tshawb fawb [5] (raws li muaj nyob hauv daim duab 1).
Daim duab 1. Lub semi-synthetic txoj kev ntawm seol raws li 10-dacetylbaccatin ⅲ.
Hauv cov ntawv tshaj tawm no, lub tsheb ntiav cov nroj tsuag extract tau ua kom huv cov roj chromatograph Lub Hom Phiaj Khoom Sib Tham Lub Rooj Sib Tham Txoj Cai Tau Txais thiab tuaj yeem siv rau hauv kev tshawb fawb tom ntej, muab cov tshuaj zoo rau kev ua kom muaj txiaj ntsig zoo ntawm cov khoom ntuj no.
| Lub cuab tam | Tshuab Ntxhua Tshuab Sepababean | |
| Lub muas txwv | 12 g Sepaflash C18 RP Flash Carica, Spherical Silica, 20 - 45μm, 100 Å, Tus lej xaj: Sw-5222-012-sp) | |
| Lub paj | 254 nm (nrhiav kom tau), 280 nm (saib xyuas) | |
| Txawb theem | Hnyav A: Dej | |
| Cov kuab tshuaj B: Methanol | ||
| Txaus tus nqi | 15 ml / min | |
| Qauv Chaw thau khoom | 20 mg Cov qauv nyoos yaj hauv 1 ml dmo | |
| Grongent | Sijhawm (min) | Cov kuab tshuaj B (%) |
| 0 | 10 | |
| 5 | 10 | |
| 7 | 28 | |
| 14 | 28 | |
| 16 | 40 | |
| 20 | 60 | |
| 27 | 60 | |
| 30 | 72 | |
| 40 | 72 | |
| 43 | 100 | |
| 45 | 100 | |
Cov txiaj ntsig thiab kev sib tham
Lub flash duromatogram rau cov crude extract los ntawm cov tsheb tavxij tau qhia hauv daim duab 2. Los ntawm kev tshuaj xyuas cov chromatogram, cov khoom lag luam thiab qhov tsis sib xws ua tiav cov hauv kev sib cais. Tsis tas li ntawd, qhov zoo replucibilibility kuj tau pom los ntawm ntau cov piv txwv txhaj tshuaj (cov ntaub ntawv tsis tau qhia). Nws yuav siv li 4 teev kom ua tiav cov kev sib cais hauv phau ntawv chromataphy txoj kev nrog iav kab. Piv nrog cov phooj ywg cov qauv chromatogy, lub hom phiaj tsis siv neeg tsuas yog xav tau 44 feeb kom ua tiav tag nrho cov haujlwm (raws li qhia hauv daim duab 3). Ntau tshaj 80% ntawm lub sijhawm thiab ntau npaum li cas ntawm cov kuab tshuaj tuaj yeem txuag tau los ntawm kev coj cov qauv tsis siv neeg, uas tuaj yeem txo cov nqi tsis siv neeg ntxiv, uas tuaj yeem txo tus nqi ntxiv nrog rau kev ua haujlwm tau zoo.
Daim duab 2. Lub Flash ChromoGram ntawm cov ntawv sib txawv los ntawm cov tsheb tavxij.
Daim duab 3. Qhov sib piv ntawm phau ntawv cov qauv chromatography nrog cov qauv tsis siv neeg.
Hauv kev xaus, ua ke sepaflash c18 RP Flash Cartridges nrog Sepabean tau muab cov tshuaj ntxuav cov khoom siv hluav taws xob zoo li cov tub ceev xwm extract.
Ntawv Sawv cev
1. Alushin GM, Lander GC, Kellogg Eh, Zhang D thiab Nog-Ris Microtuble hloov pauv hauv αβ-tubulin thaum gtp hydrolysis. Cell, 2014, 157 (5), 1117-1129.
2. Burkhart Ca, Rerman JW, Swindell CS thiab Horwitz SB. Kev sib raug zoo ntawm cov qauv ntawm cov neeg them se thiab lwm tus neeg them se ntawm Induction Nechabose Factor-α gene keeb thiab cyotoxicity. Kev tshawb fawb cancer, 1994, 54 (22), 5779-5782.
3. Chaw nres SJ, wu ch, gordon jd, zhong x, emami a thiab safa ar. Cov neeg them se tawm caspase caspase-10-nyob rau hauv apoptosis, J. Biol. Chem., 2004, 279, 51057-51067.
4. Paclitaxel. Miskas koom txoos ntawm kev noj qab haus huv-system kws muag tshuaj. [Lub Ib Hlis 2, 2015]
5. Bruce Ganem thiab Roland R. Franke. Paclitael los ntawm cov neeg sau se xub thawj: Lub tswv yim ntawm kev tsim muaj tswv yim hauv Organozonium Chemistry. J. ORG. Chem., 2007, 72 (11), 3981-3987.
Muaj cov koob c18 RP Flash cartridges nrog cov sib txawv los ntawm cov thev naus laus zis sib txawv (raws li qhia hauv Table 2).
| Yam khoom | Kem li | Txaus tus nqi (ml / min) | Max.pressure (psi / bar) |
| Sw-52222-004-sp | 5.4 g | 5-15 | 400 / 27.5 |
| Sw-5222-012 -0-sp | 20 g | 10-25 | 400 / 27.5 |
| Sw-5222-025-sp | 33 g | 10-25 | 400 / 27.5 |
| Sw-5222-040-sp | 48 g | 15-30 | 400 / 27.5 |
| Sw-5222-080-sp | 105 g | 25-50 | 350 / 24.0 |
| Sw-5222-120-sp | 150 g | 30-60 | 300 / 20.7 |
| Sw-5222-220-sp | 300 g | 40-80 | 300 / 20.7 |
| SW-522-330-sp | 420 g | 40-80 | 250 / 17.2 |
Rooj 2. Sepaflash C18 RP Flash cartridges.
Cov ntaub ntawv ntim: High-efficiency spherical c18-bonded silica, 20 - 45 μ5 μm, 100 å
Yog xav paub ntxiv txog cov ncauj lus kom ntxaws ntawm Sepabean, lossis cov ntaub ntawv xaj ntawm Sepafash series nyem cartridges, thov mus saib peb lub vev xaib
Sijhawm Post: Sep-20-2018