Camptothecinyog ib yam khoom ntuj nrog broad antitumor kev ua. Nws yog Ameslikas cais los ntawm Himalayan parasang snowberry (Camptotheca acuminata) nyob rau sab qab teb Tuam Tshoj, thiab txij li ntawd tau pom nyob rau hauv ib co lwm yam nroj tsuag thiab microorganisms. Cov qauv molecular ntawm camptothecin yog ib qho alkaloid nrog tsib lub nplhaib, suav nrog lub heterocycle thiab coumaric acid molecular uas muaj cov pab pawg hydroxyl. Hauv daim ntawv thov kev kho mob, Camptothecin feem ntau yog siv los kho ntau yam qog nqaij hlav xws li mob qog noj ntshav, mob qog noj ntshav, mob qog noj ntshav, thiab mob qog noj ntshav, tshwj xeeb tshaj yog cov qog uas tiv taus ntau yam tshuaj kho mob.
1. Molecular qauv thiab lub cev thiab tshuaj muaj zog:
Camptothecin muaj cov qauv tshwj xeeb nrog tsib lub nplhaib, suav nrog cov nplhaib sib txawv ntawm pyrrole, azine, pyrroloazine, furan thiab benzofuran. Cov qauv molecular complex no ua rau nws nyuaj heev rau synthesize, tab sis kuj pab txhawb rau nws cov yam ntxwv pharmacological. Cov mis mos molecular ntawm Camptothecin yog C20H16N2O4, thiab nws qhov hnyav molecular yog 348.35 g / mol. Ntawm qhov kub thiab txias, nws yog cov hmoov dawb rau me ntsis daj, yooj yim soluble hauv cov kuab tshuaj organic xws li chloroform, ethanol, dichloromethane, acetone thiab ethyl acetate, tab sis yuav luag insoluble hauv dej. Tsis tas li ntawd, Camptothecin yuav decompose nyob rau hauv lub teeb, yog li nws yuav tsum tau kev tiv thaiv thaum lub sij hawm tsim khoom, tswj kom zoo thiab siv.
2. Tshuaj tiv thaiv:
Cov qauv tshwj xeeb ntawm Camptothecin txiav txim siab nws cov tshuaj lom neeg tshwj xeeb. Nws tuaj yeem hloov kho los ntawm oxidation, txo, esterification, phosphorylation, rearrangement thiab lwm yam. Ntawm lawv, feem ntau cov tshuaj tiv thaiv yog hydrolysis thiab oxygen coupling. Hauv cov tshuaj tiv thaiv hydrolysis, lub nplhaib lactone ntawm Camptothecin qhib los ntawm cov dej molecules los tsim lub nplhaib qhib hydroxy acids thiab qhib-chain 6- thiab 10-hydroxyl derivatives, xws li SN-38 thiab SN -22. Cov derivatives no feem ntau muaj zog antitumor zog dua Camptothecin nws tus kheej, thiab muaj txiaj ntsig los txo cov tshuaj lom. Txawm li cas los xij, lawv kuj tsis ruaj khov thiab xav tau kev saib xyuas thaum npaj thiab khaws cia. Oxygen coupling yog lwm qhov kev hloov kho cov tshuaj tiv thaiv, feem ntau yog siv aldehyde los yog ketone ua haujlwm pab pawg los cuam tshuam nrog pawg hydroxyl ntawm Camptothecin los tsim cov khoom sib txuas sib txawv. Cov tshuaj tiv thaiv no tuaj yeem txhim kho cov khoom siv tshuaj ntawm Camptothecin, xws li nce nws cov dej solubility, txo toxicity, suppressing multidrug resistance, thiab lwm yam.
3. Kev ruaj ntseg thiab tshuaj kho:
Camptothecin muaj kev ruaj ntseg tsis zoo thiab yooj yim cuam tshuam los ntawm yam xws li oxidation, lub teeb, thiab acid-base, yog li cov xwm txheej yuav tsum tau tswj nruj me ntsis thaum npaj, cia, thiab siv. Txhawm rau txhim kho nws cov tshuaj pharmacological, ntau txoj kev hloov kho tau raug kawm, xws li nanoparticles, kev hloov kho cov qauv, ntim cov ntaub ntawv polymer, thiab lwm yam. Cov ntaub ntawv hloov kho no tuaj yeem ua rau cov dej solubility, stability thiab lub hom phiaj ntawm Camptothecin, thiab tseem tuaj yeem ua kom luv luv ntawm ib nrab- lub neej, nce tus nqi metabolic, thiab txo cov tshuaj toxicity.
Camptothecin yog ib yam tshuaj uas muaj zog heev antitumor thiab muaj cov qauv molecular tshwj xeeb thiab cov tshuaj pharmacological. Txawm hais tias nws qhov kev ruaj ntseg tsis zoo, nws cov nyhuv pharmacological thiab kev nyab xeeb tuaj yeem txhim kho los ntawm kev npaj tshuaj tsim nyog thiab kev hloov kho. Nyob rau hauv lub neej yav tom ntej, nrog rau kev kawm tob ntawm nws cov txheej txheem ntawm kev ua thiab kev hloov kho, nws ntseeg tias Camptothecin yuav ua lub luag haujlwm tseem ceeb hauv kev kho mob qog noj ntshav.
Camptothecin yog ib qho tshuaj lom neeg lom neeg alkaloid, uas muaj cov tshuaj pharmacological xws li tshuaj tiv thaiv kab mob thiab kev tiv thaiv kab mob, thiab tau siv dav hauv kev tsim cov tshuaj tiv thaiv kab mob. Nyob rau hauv xyoo tas los no, nrog rau kev kawm tob ntawm cov tshuaj tiv thaiv kab mob, kev cia siab ntawm Camptothecin rau kev kho mob qog noj ntshav tau dhau los ua ntau thiab dav.
Daim ntawv thov kev cia siab ntawm camptothecin
1. Kev tshawb fawb txog tshuaj tiv thaiv kab mob:
Camptothecin yog ib qho tshuaj lom neeg lom neeg alkaloid, uas ua lub luag haujlwm tseem ceeb hauv kev tshawb fawb ntawm cov tshuaj tiv thaiv kab mob. Ntau cov kev tshawb fawb tshuaj tau pom tias Camptothecin thiab nws cov derivatives muaj kev tiv thaiv qog noj ntshav zoo heev, thiab cov derivatives sib txawv muaj qhov sib txawv los tiv thaiv qog, thiab muaj ntau yam kev tshawb fawb muaj txiaj ntsig rau cov tshuaj tiv thaiv kab mob.
2. Kev tshawb fawb txog tshuaj tiv thaiv kab mob tshiab:
Txawm hais tias Camptothecin tau ua tiav cov txiaj ntsig zoo hauv kev kho cov qog thiab lwm yam kab mob, nws daim ntawv thov kev kho mob raug txwv los ntawm nws cov tshuaj lom thiab cov ntsiab lus ntawm cov noob. Yog li ntawd, cov kws tshawb fawb tau nrhiav cov tshuaj Camptothecin tshiab nrog cov txheej txheem zoo sib xws los txhim kho cov nyhuv tiv thaiv qog thiab txo cov tshuaj lom.
3. Kev tsim kho ntawm tes:
Camptothecin muaj ntau txoj hauv kev rau kev kho mob ntawm tes. Synthesizing Camptothecin rau hauv nanoparticles tuaj yeem txo nws cov toxicity thiab tib lub sij hawm ua kom muaj kev tiv thaiv kab mob zoo dua. Qhov no qhib qhov muaj peev xwm tshiab rau kev txhim kho kev kho ntawm tes.
4. Kev kho tshuaj yeeb tshuaj:
Camptothecin yog siv ua ke nrog lwm cov tshuaj tiv thaiv qog, xws li cisplatin, paclitaxel, thiab lwm yam, los tsim cov nyhuv synergistic ntawm cov tshuaj thiab txhim kho cov nyhuv tiv thaiv qog. Yog li, kev txhim kho kev sib xyaw ua ke ntawm Camptothecin thiab lwm yam tshuaj yog ib qho tseem ceeb hauv kev kho mob qog noj ntshav yav tom ntej.
5. Khoom noj khoom haus mis thiab muaj nuj nqi:
Camptothecin kuj muaj ntau yam kev siv hauv cov khoom noj. Cov kev tshawb fawb tau pom tias Camptothecin tuaj yeem cuam tshuam kev loj hlob ntawm cov qog hlwb, thiab tib lub sijhawm muaj cov haujlwm ntawm kev tiv thaiv oxidation thiab tiv thaiv kab mob. Yog li ntawd, kev sib koom ua ke Camptothecin nrog rau lwm cov khoom noj tuaj yeem tsim ntau yam khoom noj uas muaj txiaj ntsig zoo, muab lub sijhawm tshiab rau kev txhim kho tib neeg kev noj qab haus huv.
Camptothecin kev loj hlob cov nyom
1. Txhawm rau tiv thaiv qhov tsis ruaj khov ntawm Camptothecin:
Thaum lub sijhawm npaj, kev thauj mus los thiab khaws cia ntawm Camptothecin, nws yooj yim rau protonate los ntawm 5-hydroxymethyl txoj hauj lwm mus rau 5-hydroxy nplhaib-qhib methoxy tshuaj, yog li cuam tshuam rau nws cov tshuaj pharmacological. Yog li ntawd, nrhiav kev ruaj khov ntawm Camptothecin thiab txo qhov tsis ruaj khov ntawm Camptothecin yuav yog qhov tseem ceeb ntawm nws txoj kev tshawb fawb.
2. Txo cov tshuaj lom ntawm Camptothecin:
Raws li cov tshuaj tua kab mob muaj zog, Camptothecin's toxicity tsis tuaj yeem tsis quav ntsej. Yog li ntawd, thaum nrov tshuaj tiv thaiv kab mob, nws yog ib qho tseem ceeb txoj kev loj hlob kev taw qhia ntxiv mus kawm cov tshuaj lom ntawm Camptothecin thiab txo nws cov toxicity.
3. Nrhiav kev siv tshiab rau Camptothecin:
Ntxiv nrog rau cov tshuaj tiv thaiv kab mob, Camptothecin tseem muaj ntau lwm yam tshuaj. Cov kev tshawb fawb yav tom ntej yuav tsum tau tshawb nrhiav ntxiv txog kev siv Camptothecin hauv kev kho mob ntawm ntau yam kab mob thiab txhim kho cov tshuaj ua haujlwm thiab cov khoom noj ntxiv.
Camptothecin yog ib qho tshuaj lom neeg lom neeg alkaloid, thiab cov kws tshawb fawb tau ua tiav zoo hauv nws txoj kev tshawb fawb. Nyob rau hauv lub neej yav tom ntej, nrog rau maj mam nce nyob rau hauv qhov kev thov rau cov tshuaj tiv thaiv qog nqaij hlav, txoj kev loj hlob zeem muag ntawm Camptothecin yuav ua ntau thiab dav. Txhawm rau kom txhawb nqa kev kho mob zoo dua ntawm Camptothecin, nws yog ib qho tsim nyog yuav tsum tau ntxiv dag zog rau kev tshawb fawb ntawm nws cov tshuaj lom thiab tsis ruaj khov, tshawb nrhiav nws cov kev siv tshiab hauv kev kho mob lwm yam kab mob, txhim kho cov tshuaj zoo dua thiab cov khoom noj khoom haus, thiab siv rau hauv ntau qhov chaw, Pab. txoj kev loj hlob, kev vam meej thiab kev noj qab haus huv ntawm tib neeg.