Camptothecin Structure
Extract hmoov camptothecin(CPT) cais tawm ntawm cov tawv ntoo thiab ceg ntawm Campotheca acuminata ( tsob ntoo muaj hmoo). Nws cov hauv paus bark muaj cov teebmeem ntawm tshem tawm cov cua sov thiab detoxifying, dispersing nodules, thiab txo o. Nws cov txiv hmab txiv ntoo txhawb cov ntshav ncig thiab tshem tawm cov ntshav stasis, thiab nws feem ntau siv los kho cov tsos mob xws li psoriasis thiab mob. CPT muaj cov qauv tshuaj tshwj xeeb uas muaj tsib lub nplhaib. Nws cov qauv muaj tsib fused rings: A, B, C, D, thiab E. A yog ib lub nplhaib uas muaj ntxhiab (benzene nplhaib) fused rau nplhaib B, nplhaib C yog lub nplhaib pyrrole fused rau nplhaib B, nplhaib D yog rau-tus tswv cuab. Lub nplhaib lactone fused rau lub nplhaib C, thiab lub nplhaib E yog lub nplhaib rau-tus tswv cuab uas muaj pawg hydroxyl (-OH) thiab quinoline nitrogen. Nws yog ib qho nruab nrab alkaloid, insoluble hauv acid thiab dej, thiab soluble tsis zoo nyob rau hauv cov organic solvents. Nws yog rhiab heev rau lub teeb thiab kub. Lub teeb cuam tshuam rau kev nqus ntawm camptothecin. Nws tseem ruaj khov thaum khaws cia deb ntawm tshav ntuj, thiab cua sov ua rau nws decompose. Nws yog cytotoxic quinoline alkaloid uas inhibits DNA topoisomerase (TOPO I).
Cov kws tshawb nrhiav pom tias cov alkaloid tau pom muaj zog tiv thaiv kab mob hauv vitro tiv thaiv Hela hlwb (ib kab ntawm lub ncauj tsev menyuam), L1210 hlwb (nas lymphocytic leukemia hlwb), thiab nas, uas ua rau muaj kev tshawb fawb ntawm cov nroj tsuag camptothecin thiab camptothecin compounds. nyob rau hauv lub zej zog scientific. Tsis txog thaum tom qab ntawd tib neeg pom tias nws thiab nws cov derivatives siv lawv cov kev tiv thaiv kab mob los ntawm inhibiting DNA synthesis los ntawm kev tsom mus rau topoisomerase I (Topoisomerase I). Txij li thaum pom tias CPT inhibits topoisomerase I, tib neeg tau cog lus los nrhiav cov txiaj ntsig zoo thiab tsis muaj tshuaj lom CPT derivatives. Txog tam sim no, ib qho ntawm semisynthetic thiab tag nrho hluavtaws CPT derivatives tau tshwm sim thiab nkag mus rau hauv daim ntawv thov kev kho mob lossis kev sim tshuaj theem. Yog tias koj txaus siab rau cov khoom no, thov hu rau Xi'an Sonwu. Xi'an Sonwu tuaj yeem muab phenibut nootropics rau lub sijhawm ntev.
Dab tsi yog Lub Mechanism Ntawm Kev Ua Ntawm Camptothecin Analogues
CPT yog ib qho cytotoxic alkaloid uas ua haujlwm feem ntau los ntawm inhibiting cov enzyme topoisomerase I. Topoisomerase I yog ib qho tseem ceeb ntawm cov enzymes uas yog indispensable nyob rau hauv DNA metabolism. DNA molecules yuav ua kom muaj kev ntxhov siab superhelical thaum rov ua dua, hloov pauv, thiab kho dua vim qhov tsis sib xws ntawm ob chav helix qauv. Yog tias qhov kev ntxhov siab no tsis tau txo qis rau lub sijhawm, nws yuav cuam tshuam kev nce qib ntawm DNA replication diav rawg thiab cuam tshuam rau kev ua haujlwm ntawm DNA. Lub luag haujlwm tseem ceeb ntawm topoisomerase kuv yog los tsim ib qho kev hloov pauv ib zaug ib zaug los ntawm kev txiav ib txoj hlua ntawm DNA, tso cai rau DNA tig thiab tso cov kev ntxhov siab superhelical, thiab tom qab ntawd rov txuas cov DNA tawg kom tswj tau cov qauv kev ruaj ntseg ntawm DNA. Nws tuaj yeem khi rau thiab inhibit topoisomerase I, ua rau kev ua haujlwm ntawm cov enzyme no cuam tshuam.
Nyob rau hauv DNA unwinding tsav los ntawm topoisomerase I, lub enzyme tsim ib tug enzyme-DNA complex los ntawm kev txiav ib strand ntawm DNA, tso cai rau DNA tig los txo superhelical kev nyuaj siab. Nws lub hom phiaj tseem ceeb yog txhawm rau txhawb nqa lub sijhawm so ib ntus tsim los ntawm topoisomerase I thiab DNA. Feem ntau, cov enzyme reconnects cov DNA uas tau muab tshem tawm tom qab ua tiav cov hauj lwm unwinding. Thaum nws ua, txawm li cas los xij, nws tsim ib qho chaw ruaj khov ternary nrog topoisomerase I thiab cov DNA tawg, tiv thaiv DNA los ntawm kev sib koom ua ke. Thaum lub sij hawm DNA replication, lub replication diav rawg ntsib cov topoisomerase I-DNA complexes stabilized los ntawm camptothecin. Txij li thaum DNA strand breaks tsis tuaj yeem txuas rov qab tau, qhov kev sib txuas ntawm rab rawg tsis tuaj yeem dhau los ntawm cov kev tawg no kom zoo, uas ua rau muaj kev cuam tshuam kev cuam tshuam. Qhov kev cuam tshuam no ua rau muaj kev cuam tshuam ntawm cellular teb mechanism, thaum kawg ua rau tiam DNA ob-strand so (DSBs). Ob txoj hlua tawg yog ib daim ntawv ua kom tuag taus ntawm DNA kev puas tsuaj uas, yog tias tsis kho raws sijhawm, yuav ua rau muaj kev tuag ntawm tes. CPT ua rau cov hlwb no nkag mus rau apoptosis los ntawm kev cuam tshuam nrog DNA replication thiab ua rau muaj kev puas tsuaj DNA ntau heev, tshwj xeeb tshaj yog nyob rau hauv cov kab mob sai sai. Vim tias cov kab mob muaj cov kab mob DNA ntau zaus, lawv raug cuam tshuam rau cov teebmeem ntawm camptothecin.
Dab tsi yog Camptothecin siv rau
Kev kho mob ntawm cov kab mob loj
1. Kab mob plab hnyuv
Semisynthetic CPT derivatives tuaj yeem kho cov kab mob hauv plab, tshwj xeeb tshaj yog nyob rau hauv cov mob hnyav lossis rov tshwm sim dua.
2. Kab mob zes qe menyuam
CPT thiab nws cov derivatives tau dav siv los kho cov kab mob zes qe menyuam. Nws feem ntau yog siv los ua kab thib ob rau cov neeg mob uas muaj kab mob zes qe menyuam tiv taus cov tshuaj platinum.
3. Mob ntsws me me
Tsis tas li ntawd, cov kab mob ntsws me me tau kho nrog CPT thiab nws cov txiaj ntsig, tshwj xeeb tshaj yog thaum tus kab mob rov qab los yog tsis teb rau thawj qhov kev kho mob.
4. Kab mob ncauj tsev menyuam
CPT thiab nws cov derivative topotecan ua ke nrog cisplatin tau pom zoo los kho cov kab mob hauv ncauj tsev menyuam rov qab los yog qib siab. Qhov kev sib xyaw ua ke no tau qhia qee qhov zoo hauv kev ua kom tus neeg mob muaj sia nyob ntev.
5. Lwm yam kab mob
CPT thiab nws cov derivatives kuj tau pom tias muaj peev xwm kho tau hauv lwm cov kab mob, suav nrog pancreatic, gastric, siab, thiab kab mob hauv lub mis. Txawm hais tias cov ntawv thov no tseem tsis tau lees paub dav dav, kev tshawb fawb soj ntsuam txuas ntxiv tuaj yeem nthuav dav ntxiv ntawm kev siv tshuaj camptothecin.
Lwm yam kev siv muaj peev xwm
1. Kev kho mob antiviral
CPT qhia qee yam tshuaj tiv thaiv kab mob vim nws muaj peev xwm cuam tshuam nrog DNA replication. Cov kev tshawb fawb tau pom tias camptothecins tuaj yeem tiv thaiv qee yam kab mob los ntawm inhibiting viral DNA replication. Kev tshawb fawb hauv cheeb tsam no tseem nyob rau theem pib tab sis muab cov kev taw qhia tshiab rau kev txhim kho tshuaj tiv thaiv kab mob yav tom ntej.
2. Cov kab mob neurodegenerative
Raws li qee qhov kev tshawb fawb thaum ntxov, nws yuav pab tau rau kev kho mob ntawm cov kab mob neurodegenerative, suav nrog Parkinson's thiab Alzheimer's disease. Nws cov txheej txheem tuaj yeem ua rau qeeb neuronal puas thiab tuag los ntawm kev tswj hwm DNA kho txoj hauv kev. Txawm li cas los xij, cov kev tshawb pom no tseem xav tau kev tshawb fawb ntxiv los txheeb xyuas lawv cov txiaj ntsig thiab kev nyab xeeb.
Cov ntawv thov kev tshawb fawb yooj yim
Kev tshawb nrhiav DNA topology
Raws li ib tug muaj zog inhibitor ntawm topoisomerase I, nws yog dav siv los kawm DNA superhelical qauv thiab nws lub luag hauj lwm nyob rau hauv gene qhia thiab chromatin remodeling.
Kev tshawb nrhiav lub voj voog ntawm tes
Los ntawm kev tiv thaiv DNA replication, camptothecins yog siv los kawm txog cell voj voog tswj mechanisms, tshwj xeeb tshaj yog cell voj voog deregulation txuam nrog cov kab mob pathological.
Thov tsis txhob yig tiv tauj Xi'an Sonwu yog tias koj muaj lus nug txog cov khoom, xav paub tus nqi CPT, lossis xav paub hauv Xi'an Sonwu.
Email:sales@sonwu.com