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ʻO ka hoʻomaʻemaʻe ʻana i nā haumia polar kiʻekiʻe i nā lāʻau antibiotic e nā kolamu C18AQ

ʻO ka hoʻomaʻemaʻe ʻana i nā haumia polar kiʻekiʻe i nā lāʻau antibiotic e nā kolamu C18AQ

Mingzu Yang, Bo Xu
Ka Papahana R&D Center

Hoʻolauna
ʻO nā lāʻau antibiotic kahi papa o nā metabolites lua i hana ʻia e nā microorganism (me ka bacteria, fungi, actinomycetes) a i ʻole nā ​​mea like like i hoʻohui ʻia a i ʻole semi-synthesized.Hiki i nā lāʻau antibiotic ke kāohi i ka ulu ʻana a me ke ola ʻana o nā microorganism ʻē aʻe.ʻO ka lāʻau antibiotic mua i ʻike ʻia e ke kanaka, ʻo ka penicillin, ua ʻike ʻia e ka microbiologist Pelekania ʻo Alexander Fleming i ka makahiki 1928. Ua ʻike ʻo ia ʻaʻole hiki ke ulu ka bacteria ma kahi kokoke i ka mold i loko o ke kīʻaha moʻomeheu staphylococcus i haumia i ka pala.Ua manaʻo ʻo ia he pono e hūnā ka ʻōpala i kahi mea antibacterial, āna i kapa ai i ka penicillin i ka makahiki 1928. Akā naʻe, ʻaʻole i hoʻomaʻemaʻe ʻia nā mea hana i kēlā manawa.I ka makahiki 1939, ua hoʻoholo ʻo Ernst Chain lāua ʻo Howard Florey o ke Kulanui o Oxford e hoʻomohala i kahi lāʻau lapaʻau e hiki ai ke mālama i nā maʻi bacterial.Ma hope o ka hoʻopili ʻana iā Fleming no ka loaʻa ʻana o nā kānana, ua hoʻomaʻemaʻe maikaʻi lākou i ka penicillin mai nā kānana.No ko lākou holomua ʻana o ka penicillin ma ke ʻano he lāʻau lapaʻau, ua hāʻawi ʻo Fleming, Chain a me Florey i ka makana Nobel i ka lāʻau lapaʻau i ka makahiki 1945.

Hoʻohana ʻia nā lāʻau antibiotic ma ke ʻano he mea antibacterial e mālama a pale i nā maʻi bacterial.Aia kekahi mau ʻano nui o nā lāʻau antibiotic i hoʻohana ʻia ma ke ʻano he antibacterial agents: β-lactam antibiotics (me ka penicillin, cephalosporin, etc.), aminoglycoside antibiotics, macrolide antibiotics, tetracycline antibiotics, chloramphenicol (total synthetic antibiotic), a me nā mea ʻē aʻe. fermentation biological, semi-synthesis a me ka huina hoʻohui.Pono e hoʻololi ʻia nā lāʻau antibiotic i hana ʻia e ka biological fermentation e nā ʻano kemika ma muli o ke kūpaʻa kemika, nā hopena ʻino, nā antibacterial spectrum a me nā pilikia ʻē aʻe.Ma hope o ka hoʻololi kemika, hiki i nā lāʻau antibiotic ke hoʻonui i ka paʻa, hoʻemi i nā hopena ʻino, hoʻonui i ka spectrum antibacterial, hoʻemi i ka pale ʻana i ka lāʻau, hoʻomaikaʻi i ka bioavailability, a laila hoʻomaikaʻi i ka hopena o ka lāʻau lapaʻau.No laila, ʻo nā antibiotic semi-synthetic i kēia manawa ke alakaʻi kaulana loa i ka hoʻomohala ʻana i nā lāʻau antibiotic.

I ka hoʻomohala ʻana i nā lāʻau antibiotic semi-synthetic, loaʻa i nā lāʻau antibiotic nā waiwai o ka maʻemaʻe haʻahaʻa, ka nui o nā huahana a me nā mea paʻakikī mai ka loaʻa ʻana mai o nā huahana fermentation microbial.I kēia hihia, he mea koʻikoʻi ka nānā ʻana a me ka mālama ʻana i nā haumia i nā antibiotic semi-synthetic.I mea e ʻike pono ai a ʻike i nā mea haumia, pono e loaʻa ka nui o nā haumia mai ka huahana synthetic o semi-synthetic antibiotics.Ma waena o nā ʻano hana hoʻomākaukau haumia maʻamau, ʻo ka chromatography flash he ʻano kumu kūʻai me nā mea maikaʻi e like me ka nui o ka hoʻouka ʻana o ka laʻana, ke kumu kūʻai haʻahaʻa, mālama manawa, a me nā mea ʻē aʻe.

Ma kēia pou, ua hoʻohana ʻia ka haumia nui o ka semi-synthetic aminoglycoside antibiotic ma ke ʻano he laʻana a hoʻomaʻemaʻe ʻia e kahi pahu pahu SepaFlash C18AQ i hui pū ʻia me ka mīkini chromatography flash SepaBean™.Ua loaʻa maikaʻi ka huahana i hoʻokō ʻia i nā koi, e hōʻike ana i kahi hopena kūpono loa no ka hoʻomaʻemaʻe ʻana i kēia mau pūhui.

Māhele hoʻokolohua
Hāʻawi maikaʻi ʻia ka laʻana e kahi hui lāʻau lapaʻau kūloko.ʻO ka hāpana he ʻano amino polycyclic carbohydrates a ua like kona ʻano molekala me nā lāʻau antibiotic aminoglycoside.ʻOi aku ka kiʻekiʻe o ka polarity o ka hāpana, hiki ke hoʻoheheʻe ʻia i ka wai.Ua hōʻike ʻia ke kiʻikuhi schematic o ka molecular structure o ka hāpana ma ka Figure 1. ʻO ka maʻemaʻe o ka hāpana maka ma kahi o 88% e like me ka nānā ʻana e HPLC.No ka hoʻomaʻemaʻe ʻana i kēia mau pūhui o ka polarity kiʻekiʻe, e paʻa ʻole ka hāpana ma nā kolamu C18 maʻamau e like me kā mākou ʻike mua.No laila, ua hoʻohana ʻia kahi kolamu C18AQ no ka hoʻomaʻemaʻe laʻana.

Kiʻi 1. ʻO ke kiʻikuhi schematic o ke ʻano mole o ka hāpana.
No ka hoʻomākaukau ʻana i ka hāpana hāpana, ua hoʻoheheʻe ʻia ʻo 50 mg crude sample i loko o 5 mL wai maʻemaʻe a laila ultrasonicated i mea e lilo ai i mea maopopo loa.A laila, hoʻokomo ʻia ka hāpana hāpana i loko o ke kolamu uila e kahi injector.Ua helu ʻia ka hoʻonohonoho hoʻokolohua o ka hoʻomaʻemaʻe uila ma ka Papa 1.

Mea hana

Mekini SepaBean™ 2

Nā pahu pahu

12 g SepaFlash C18AQ RP pahu pahu uila (spherical silica, 20 - 45μm, 100 Å, Helu kauoha:SW-5222-012-SP(AQ))

Loʻihi nalu

204 nm, 220 nm

Māhele kelepona

Solvent A: Wai

Mea hoʻoheheʻe B: Acetonitrile

Kahe kahe

15 mL/min

Hoʻouka laʻana

50 mg

Gradient

Manawa (min)

Mea hoʻoheheʻe B (%)

0

0

19.0

8

47.0

80

52.0

80

Nā hualoaʻa a me ke kūkākūkā
Ua hōʻike ʻia ka chromatogram flash o ka hāpana ma ka pahu pahu C18AQ ma ke Kiʻi 2. E like me ka hōʻike ʻana ma ka Figure 2, ua paʻa pono ka hāpana polar nui ma ka pahu pahu C18AQ.Ma hope o ka lyopholization no nā hakina i hōʻiliʻili ʻia, loaʻa ka maʻemaʻe o ka huahana i koho ʻia he 96.2% (e like me ka hōʻike ʻana ma ke Kiʻi 3) e ka nānā ʻana HPLC.Ua hōʻike ʻia nā hopena e hiki ke hoʻohana hou ʻia ka huahana i hoʻomaʻemaʻe ʻia i ka hana noiʻi a me ka hoʻomohala ʻana.

Kiʻi 2. ʻO ka chromatogram flash o ka hāpana ma kahi pahu pahu C18AQ.

Kiʻi 3. ʻO ka chromatogram HPLC o ka huahana i koho ʻia.

I ka hopena, ʻo SepaFlash C18AQ RP pahu pahu uila i hui pū ʻia me ka ʻōnaehana chromatography flash hiki iā SepaBean™ mīkini ke hāʻawi i kahi hopena wikiwiki a kūpono no ka hoʻomaʻemaʻe ʻana i nā laʻana polar loa.

E pili ana i nā pahu pahu uila SepaFlash C18AQ RP
Aia kekahi pūʻulu o nā pahu uila SepaFlash C18AQ RP me nā kikoʻī like ʻole mai Santai Technology (e like me ka hōʻike ʻana ma ka Papa 2).

Helu 'ikamu

Ka nui o ke kolamu

Kahe Kahe

(mL/min)

Max.Pressure

(psi/pa)

SW-5222-004-SP(AQ)

5.4 g

5-15

400/27.5

SW-5222-012-SP(AQ)

20 g

10-25

400/27.5

SW-5222-025-SP(AQ)

33 g

10-25

400/27.5

SW-5222-040-SP(AQ)

48 g

15-30

400/27.5

SW-5222-080-SP(AQ)

105 g

25-50

350/24.0

SW-5222-120-SP(AQ)

155 g

30-60

300/20.7

SW-5222-220-SP(AQ)

300 g

40-80

300/20.7

SW-5222-330-SP(AQ)

420 g

40-80

250/17.2

Papa 2. SepaFlash C18AQ RP pahu pahu flash.Mea hoʻopili: High-efficiency spherical C18(AQ)-hoʻopaʻa silica, 20 - 45 μm, 100 Å.

No ka ʻike hou aku e pili ana i nā kikoʻī kikoʻī o ka mīkini SepaBean™, a i ʻole ka ʻike kauoha ma nā pahu pahu uila SepaFlash series, e ʻoluʻolu e kipa i kā mākou pūnaewele.


Ka manawa hoʻouna: Oct-26-2018