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Kwezwa kwa tagisi ya sepabenaan ™ imashini

Gukuramo tagisi

Meiyian Qian, Yuefeng Tan, bo xu
Porogaramu R & D Centre

Intangiriro
Tagisi (chinensis cyangwa igishinwa yego) ni igihingwa cyo mu gasozi kirinzwe n'igihugu. Nibihingwa bidasanzwe kandi byangiritse byasigaye inyuma nabarafu bakuru. Nibintu bikumbi byumuti mu isi. Tagito ikwirakwizwa mu karere k'ubushyuhe mu majyaruguru mu karere ka subtropical hagati, hamwe n'amoko agera kuri 11 ku isi. Hano hari amoko 4 n'ubwoko butandukanye mu Bushinwa, ni ukuvuga tagisi y'Amajyaruguru, ni ukuvuga tagisi y'Amajyaruguru, ya tagisi y'Amajyaruguru, Tapisi, tagisi, tagisi, tagisi yo mu majyepfo. Aya moko atanu akwirakwizwa mu majyepfo y'uburengerazuba bw'Ubushinwa, Ubushinwa bwepfo, Ubushinwa bwo Hagati, Ubushinwa bw'Uburasirazuba, mu majyaruguru y'uburengerazuba bw'Ubushinwa, mu majyaruguru y'uburengerazuba bw'Ubushinwa, mu majyaruguru y'uburasirazuba bw'Ubushinwa na Tayiwani. Ibimera bya tagisi birimo ibice bitandukanye by'imiti, harimo na tagitaka, flavonoide, ibitambo, steroid, acide, acide, iGLaCenes. Umusore uzwi cyane wo kurwanya ibiyobyabwenge (cyangwa PAClitaxel) ni ubwoko bwa tagisa. Umusoreshwa ufite uburyo budasanzwe. Taxol irashobora "gukonjesha" ihuza na bo kandi ikabuza microtubules kuva kutandukanya chromosomes mugihe cyo kugabana karutu, bityo biganisha ku rupfu rwagabana selile, cyane cyane ikwirakwira mu kagari ka kanseri [1]. Byongeye kandi, mugukora macroppages, tagile ikora igabanuka muri TNF-α (ikibyimba cya necrosis) cyakira kandi ukuremo tnf-α, bityo bisohora cyangwa bibuza selile zo kwibinya [2]. Byongeye kandi, taxom irashobora gutera apoptose akurikiza inzira ya apoptotike yatangajwe na es / fasl cyangwa gukora sisitemu yo kurinda cysteine ​​[3]. Kubera ingaruka zayo nyinshi zidateganya, Taxol yakoreshwaga cyane ku kuvura kanseri ya ovarian, kanseri y'ibere, kanseri y'inkuta, kanseri y'imigozi, guhagarika kanseri ya Esonate, n'ibindi [4]. By'umwihariko kuri kanseri y'ibere hamwe na kanseri ya ovarian yateye imbere, tapi tax ifite ingaruka zikomeye, bityo izwi ku izina rya "umurongo wa nyuma wo kwirwanaho mu kuvura kanseri".

Taxol ni ibiyobyabwenge bizwi cyane byo kurwanya isoko mpuzamahanga mumyaka yashize kandi bifatwa nkimwe mubiyobyabwenge byifashe nabi kubantu mumyaka 20 iri imbere. Mu myaka yashize, hamwe no gukura guturika kw'abaturage no gukumira kanseri, byiyongereye cyane. Kugeza ubu, tagisi isaba ubushakashatsi cyangwa ubumenyi bwa siyansi yakuweho cyane muri tagisi. Kubwamahirwe, ibikubiye muri tagisi mubimera biri hasi cyane. Kurugero, ibirimo birimo tagisi ni 0.069% gusa mubishishwa bya tagisi Brevifolia, muri rusange bifatwa nkibirimo byinshi. Kugirango usuzume 1 g ya tagisi, bisaba kg hafi 13.6 ya tagisi. Hashingiwe kuri iki kigereranyo, bisaba ibiti 3 - 12 bya tagisi birenga 100 gufata umurwayi wa kanseri ya ovarian. Kubera iyo mpamvu, ibiti byinshi bya tagisi byaciwe, bituma habaho kuzimira ubu bwoko bw'agaciro. Byongeye kandi, tagisi ni umukene cyane mubutunzi kandi itinda gukura, bituma bigora iterambere no gukoresha taxpol.

Kugeza ubu, Synthesis ya tagisi yarangiye neza. Ariko, inzira yayo yuburyo iragoye cyane kandi ikiguzi kinini, bigatuma itagira ingamba zinganda. Uburyo bwa kimwe cya kabiri cya tagisi ubu ntikurakuze kandi ifatwa nkaho ari inzira nziza yo kwagura isoko yinyongera yinyongera. Muri make, muri kimwe cya kabiri cya tagisi, ikigo cyibanze cya tagisi kiba kinini mu bimera bya tagisi hanyuma gihinduka mu bicuruzwa bya Synthesis. Ibiri muri 10-Deacetylbaccatin ⅲ mu nshinge za tagitari za tagitari zirashobora kugera kuri 0.1%. Kandi inshinge ziroroshye kuvugurura ugereranije nigeri. Kubwibyo, igice cya kimwe cya kabiri cya tagisi gishingiye kuri 10-diacettylbaccatin ⅲ akurura abantu benshi kandi benshi mubashakashatsi [5] (nkuko bigaragara ku gishushanyo 1).

Igishushanyo 1. Inzira ya Semi-synthique ya tagisi ishingiye kuri 10-deacetylbaccatin ⅲ.

Muri iyi nyandiko, ibihingwa by'ibihingwa byasabwe na flarom itegura flash ya sepabetografi ™ imashini ihuza na tarridges yahinduwe na cartridge ya Santai. Ibicuruzwa bigamije kuzuza ibisabwa byera byera kandi birashobora gukoreshwa mubushakashatsi bwa siyansi, gutanga igisubizo cyiza cyo kwezwa kwihuta muribi bicuruzwa bisanzwe.

Icyiciro cyageragejwe
Muri iyi nyandiko, ibinyuranyo bya tagisi byakoreshejwe nkurugero. Icyitegererezo kibisi cyabonetse mugukuramo ibishishwa bya tagisi hamwe na Ethanol. Noneho icyitegererezo cya mbisi cyashonga muri DMSO kandi cyuzuye kuri karitsiye. Gukora igerageza rya flash ryerekanwe ku mbonerahamwe ya 1.
Igikoresho

Igikoresho

Sepabean ™ imashini

Karitsiye

12 G DissFlash C18 Rp Flash Cartridge (SPERICACT SILICA, 20 - 45μm, 100 å, Inomero ya 100 å, sw-5222-012-sp)

Uburebure

254 nm (gutahura), 280 nm (gukurikirana)

Icyiciro cya mobile

Gukemura a: amazi

Yamazaki B: methanol

Igipimo

15 ml / min

Icyitegererezo

20 mg raw icyitegererezo cyashenywe muri 1 ml dmso

Gradient

Igihe (Min)

Yamazaki B (%)

0

10

5

10

7

28

14

28

16

40

20

60

27

60

30

72

40

72

43

100

45

100

Imbonerahamwe 1. Gushiraho ubushakashatsi kuri flash.

Ibisubizo n'ibiganiro
Flash chromatogram kugirango ikuremo ubugome kuva tagisi yerekanwe ku gishushanyo cya 2. Mugusesengura chromatogram, ibicuruzwa byagenewe hamwe numwanda wageze gutandukana no gutandukana. Byongeye kandi, kubyara byiza nabyo byagaragaye no gutera inshinge nyinshi (amakuru atagaragajwe). Bizatwara amasaha agera kuri 4 kugirango urangize gutandukana muburyo bwa chromatografi hamwe ninkingi yikirahure. Kugereranya nuburyo bwimfashabusi ya chromatografiya, uburyo bwo kweza bwikora muriyi nyandiko bisaba iminota 44 kugirango urangize umurimo wo kweza (nkuko bigaragara ku gishushanyo cya 3). Kurenga 80% byigihe hamwe nubunini bunini burashobora gukizwa no gufata uburyo bwikora, bushobora kugabanya neza ikiguzi kimwe no kunoza cyane akazi.

Igishushanyo cya 2. Flash chromatogram yo gukuramo ubugome kuva tagisi.

Igishushanyo cya 3. Kugereranya uburyo bwa chromatografiya hamwe nuburyo bwo kweza mu buryo bwikora.
Mu gusoza, guhuza gutandukanya C18 RP Flash Cartridges hamwe na soxabean ™ imashini irashobora gutanga igisubizo cyihuse kandi cyiza cyo kwezwa byihuse nkibisohoka.
INGINGO

1. Alushin Gm, Lander GC, Kellogg Eh, Zhang R, Baker D, Bater D na Nogales Akagari, 2014, 157 (5), 1117-1129.
2. Burkhart ca, Berman JW, Swindell CS na Horwitz SB. Umubano hagati yimiterere ya tagisi hamwe nabandi tagisa zijyanye no kwinjiza ibibyimba bya necrosis-α gene imvugo na cytotoxigine. Ubushakashatsi bwa Kanseri, 1994, 54 (22), 5779-5782.
3. Parike Sj, Wu ch, Gordon JD, Zhong X, Emami A na Safa ar. Taxol yinjiza Caspase-10-itunzwe na apoptose, J. BIOL. Chem., 2004, 279, 51057-5067.
4. PAClitaxel. Umuryango w'Abanyamerika wa sisitemu y'ubuzima. [Mutarama 2, 2015]
5. Bruce Ganem na Roland R. Franke. Paclitaxel kuva tagisasiyo yibanze: icyerekezo cyo guhanga umutwe muri Ordozirium chimie. J. org. Chem., 2007, 72 (11), 3981-3987.

Kubijyanye na etaplash c18 rp flash cartridges

Hano hari urukurikirane rwa Startflash C18 rp flash cartrige hamwe nuburyo butandukanye kuva tekinoroji ya Santai (nkuko bigaragara mu mbonerahamwe ya 2).

Umubare w'ikintu

Ingano y'inkingi

Igipimo

(ML / Min)

Max.kwishimira

(PSI / BAR)

SW-5222-004-SP

5.4 g

5-15

400/1 27.5

Sw-5222-012-sp

20 g

10-25

400/1 27.5

SW-5222-025-SP

33 g

10-25

400/1 27.5

Sw-5222-040-SP

48 g

15-30

400/1 27.5

Sw-5222-080-sp

105 g

25-50

350 / 24.0

Sw-5222-120-SP

155 g

30-60

300 / 20.7

SW-5222-220-SP

300 g

40-80

300 / 20.7

SW-5222-330-SP

420 G.

40-80

250 / 17.2

Imbonerahamwe 2. Gutandukanya C18 RP Flash Cartridges.
Ibikoresho byo gupakira: Gukora neza-Imikorere ya Spherical C18-Umuyoboro wa Silica, 20 - 45 μm, 100 å

Ukeneye ibisobanuro birambuye kubijyanye nimashini zirambuye za sepabean ™ imashini, cyangwa amakuru yo gutumiza kuri DissFlash Urukurikirane rwa Flash Cartridges, nyamuneka sura urubuga rwacu


Igihe cya nyuma: Sep-20-2018