Taw qhia
Tetrandrineyog ib tug natural bisbenzylisoquinoline alkaloid cais los ntawm lub hauv paus ntawmStephania tetrandra(tseem hu ua Han Fang Ji), cov nroj tsuag feem ntau hais txog hauv Suav Pharmacopoeia rau nws cov kev siv ib txwm siv ua analgesic, diuretic, thiab antihypertensive agent.[1][4]. Thawj zaug pom nyob rau hauv 1928, qhov no bioactive compound tau txij li thaum lub ntsiab lus ntawm nws kim heev pharmacological kev tshawb fawb vim nws multifaceted kho muaj peev xwm.[4].
Raws li ib tug zoo-tus cwj pwm calcium channel blocker, tetrandrine nthuav tawm ntau yam kev ua ub no lom neeg, suav nrog kev tiv thaiv- mob, tiv thaiv kab mob, tiv thaiv-fibrotic, thiab tiv thaiv- qog nqaij hlav.[1][2][4]. Nws tau raug tshawb xyuas hauv cov chaw kho mob rau cov xwm txheej xws li silicosis thiab kub siab mus rau mob qog noj ntshav, qhia tau tias muaj txiaj ntsig zoo yam tsis muaj tshuaj lom.[4]. Peb lub siab -purity tetrandrine yog muab raws li kev tshawb fawb -qib reagent rau qib siab tshuaj tshuaj thiab biomedical tshawb nrhiav.
Physical & Chemical Parameters
| Parameter | Specification / Tus nqi | Sau ntawv / Reference |
|---|---|---|
| Lub cev lub xeev | Khoom | Crystalline hmoov |
| Xim | Dawb rau tawm -dawb; dawb -daj | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 98.0% | |
| Melting Point | 217.5-223 ° C | Cov ntaub ntawv sib txawv |
| Molecular Formula | C₃₈H₄₂N₂O₆ | |
| Molecular Luj | 622.75 - 622.76 g / mol | |
| Kev sib hloov kho qhov muag | Cov ntaub ntawv sib hloov tshwj xeeb muaj thaum thov | |
| Solubility | Soluble hauv cov kuab tshuaj organic; hu rau pab neeg technical rau cov ntaub ntawv solubility tshwj xeeb | |
| UV Absorption (MeOH) | λ max 214 nm (4.78), 283 nm (3.91) | |
| IR (KBr) | 1608, 1585, 1505, 1273, 1235, 1213, 1135, 1128, 1113, 1070, 1028, 845 cm⁻¹ | |
| Kev cia khoom | 2-8 degree, tiv thaiv los ntawm lub teeb | |
| InChI Key | WVTTKBKWTSCPRNU-KYJUHHDHSA-N |
Mechanism ntawm Action
Tetrandrine exerts nws ntau yam pharmacological teebmeem los ntawm ntau interconnected molecular mechanisms, nrog rau nws lub luag hauj lwm raws li ib tugcalcium channel blockerua tus yam ntxwv tshaj plaws.
1. Calcium Channel Antagonism[1][4]
- Blocks voltage-gated calcium channels (L-type, T-type, N-type) hauv vascular, cardiac, thiab adrenal cells
- Inhibits vascular contraction, inducing vasodilation thiab antihypertensive teebmeem
- Pab txhawb rau antiarrhythmic zog los ntawm cardiac calcium channel inhibition
2. Kev tiv thaiv -Kev ua mob thiab kev tiv thaiv kab mob[1][4]
- Inhibits nitric oxide (NO) tso tawm thiab iNOS qhia
- Modulates inflammatory cytokine ntau lawm
- Txhawb nqa prostaglandin thiab leukotriene tiam
- Kev ua tau zoo hauv cov mob xws li mob caj dab rheumatoid thiab silicosis
3. Anti-Tumor Mechanisms[2][4]
- Induces apoptosis ntawm caspase activation
- Ua rau autophagy thiab cell voj voog ntes hauv cov qog nqaij hlav cancer
- Tshem tawm cov qog nqaij hlav qog nqaij hlav, kev ntxeem tau, thiab kev loj hlob
- Reverses multidrug resistance los ntawm inhibiting P-glycoprotein
- Active tiv thaiv lub ntsws, mis, hnyuv, siab, thiab lwm yam mob qog noj ntshav
- Qhia cytotoxicity xaiv (IC₅₀ siab dua hauv cov uas tsis yog- mob qog noj ntshav thiab qog noj ntshav)[3]
4. Los tiv thaiv-Fibrotic thiab lub cev-Cov teebmeem tiv thaiv[1][4]
- Remodels hypertrophied cardiac cov ntaub so ntswg
- Inhibits angiogenesis
- Tiv thaiv fibrosis hauv silicosis thiab daim siab cirrhosis qauv
5. Cov dej num ntxiv
- Kev cuam tshuam nrog -adrenergic thiab muscarinic receptors
- Tshuaj tua kab mob (Ebola), tshuaj tua kab mob (M. tuberculosis), antifungal (C. albicans), thiab antimalarial kev ua haujlwm[4]
Cov txiaj ntsig tseem ceeb & qhov zoo
- Multi-Parget Pharmacological Profile:Tshaj tawm ntau yam ntawm bioactivities, suav nrog calcium channel blockade, tiv thaiv -inflammatory, immunosuppressive, anti- qog, tiv thaiv-fibrotic, thiab tshuaj tua kab mob, ua rau nws muaj ntau yam kev tshawb fawb cuab yeej[1][2][4].
- Clinically Validated Efficacy:Tau raug sim hauv kev sim tshuaj thiab pom tias muaj txiaj ntsig zoo tiv thaiv silicosis, kub siab, mob, thiab mob ntsws cancer yam tsis muaj tshuaj lom.[4].
- Zoo -Characterized Mechanism of Action:Kev tshawb fawb dav dav tau piav qhia nws cov kev sib cuam tshuam ntawm molecular nrog calcium channels, receptors, thiab kev taw qhia txoj hauv kev, muab lub hauv paus ruaj khov rau kev tshawb nrhiav ntxiv.[1][4].
- Selective Cytotoxicity:Ua kom pom qhov muaj txiaj ntsig ntau dua IC₅₀ rau cov tsis yog- cov qog nqaij hlav cancer piv rau cov kab mob qog noj ntshav, qhia txog qhov muaj peev xwm ua tus neeg sawv cev tiv thaiv kab mob nrog kev xaiv zoo[3].
- Kev tshawb fawb dav dav:Muaj feem xyuam rau ntau yam kev tshawb fawb, suav nrog oncology, tshuaj kho plawv plawv, kev tiv thaiv kab mob, kab mob sib kis, thiab kev tshawb fawb fibrosis[2][4].
- High Purity thiab Consistency:Muab ntawm Ntau dua lossis sib npaug rau 98.0% purity nrog cov ntaub ntawv txheeb xyuas dav dav, kom ntseeg tau cov txiaj ntsig kev sim ua dua tshiab.
Cov ntawv thov tseem ceeb
| Kev tshawb fawb teb | Piv txwv daim ntawv thov | Mechanism/Rationale |
|---|---|---|
| Kev tshawb nrhiav Oncology | Mob ntsws cancer, mob cancer mis, mob qog noj ntshav, mob qog noj ntshav prostate, mob qog noj ntshav siab; Kev tshawb nrhiav tshuaj tiv thaiv; multidrug resistance kev tshawb fawb | Induces apoptosis, autophagy, thiab cell voj voog ntes; inhibits proliferation, migration, thiab ntxeem tau[2][3] |
| Cardiovascular Pharmacology | Cov qauv kub siab; kev tshawb fawb antiarrhythmic; kev tshawb nrhiav vascular function | Calcium channel thaiv; vasodilation; inhibition ntawm L- thiab T- hom calcium channels[1] |
| Inflamation & Immunology | Cov qauv mob caj dab; Kev tshawb nrhiav kab mob inflammatory; cytokine kev tswj xyuas | Inhibits TSIS MUAJ ntau lawm; modulates prostaglandin / leukotriene tiam; tiv thaiv -cov teebmeem cytokine[1][4] |
| Kev tshawb nrhiav Fibrosis | Silicosis qauv; kev tshawb fawb daim siab cirrhosis; Kev tshawb nrhiav pulmonary fibrosis | Anti-fibrogenic ua; cov ntaub so ntswg kho cov teebmeem; inhibition ntawm angiogenesis[1][4] |
| Kev Tshawb Fawb Kab Mob | Kev tshawb nrhiav kab mob Ebola; kev tshawb fawb tuberculosis; malaria thiab candidiasis qauv | Direct antimicrobial / tshuaj tiv thaiv kab mob; modulation ntawm host cell pathways[4] |
| Kev Tshawb Fawb Txog Neurological | Calcium channel kev tshawb fawb hauv cov hlwb neuronal; Cov kab mob neurodegenerative qauv | N- hom calcium channel thaiv; modulation ntawm neuronal calcium signaling[1] |
| Pharmacokinetic Studies | Kev faib tshuaj, metabolism, thiab kev tshawb fawb bioavailability; formulation kev loj hlob | Kev ntsuam xyuas ntawm cov ntshav plasma protein khi (2-5% tsis muaj feem cuam tshuam); erythrocyte partitioning; lysosomal cuab |
FAQ: Cov lus nug nquag nug
Q: Puas yog Tetrandrine muaj kev nyab xeeb rau tib neeg siv?
A: Tetrandrine yog npaj rau kev tshawb fawb siv nkaus xwb thiab tsis pom zoo rau tib neeg noj raws li tshuaj lossis ntxiv. Hauv cov chaw tshawb fawb soj ntsuam, nws tau raug sim thiab pom muaj txiaj ntsig zoo tiv thaiv silicosis, kub siab, mob, thiab mob ntsws cancer yam tsis muaj tshuaj lom. Txawm li cas los xij, kev tswj xyuas mob ntev hauv kev tshawb fawb tsiaj tau pom tias muaj peev xwm ua rau lub siab necrosis ntawm cov koob tshuaj siab (LD₅₀ (nas, ip) 41.3 mg / kg).
Q: Qhov txawv ntawm Tetrandrine thiab Fangchinoline yog dab tsi?
A: Ob leeg yog bisbenzylisoquinoline alkaloids pom hauv Stephania tetrandra. Tetrandrine thiab fangchinoline yog cov qauv analogues uas zoo sib xws tab sis txawv pharmacological profiles. Lawv nthuav tawm qhov sib txawv ntawm cov khoom pharmacokinetic, suav nrog cov ntshav plasma protein khi thiab cellular uptake.
Ua tam sim no
Ua ntej koj qhov kev tshawb fawb tshuaj nrog peb qhov siab -purityTetrandrine hmoov.
Hu rau peb pab neeg muag khoom hnub no rau:
- Thov ib qho piv txwv rau koj qhov kev tshuaj ntsuam xyuas thiab kev txhim kho txoj kev.
- Tau txais cov lus sib tw rau R&D, pilot- nplai, lossis ntau qhov ntau.
Tau txais cov ntaub ntawv nthuav dav, suav nrog Daim Ntawv Pov Thawj Kev Ntsuam Xyuas (CoA) thiab Daim Ntawv Qhia Txog Kev Nyab Xeeb (SDS).
Thov hu rau peb ntawmella.zhang@huilinbio-tech.com.
Cov ntaub ntawv
- Kwan, CY, & Achike, FI (2002). Tetrandrine thiab lwm yam bis-benzylisoquinoline alkaloids los ntawm cov tshuaj ntsuab: cov teebmeem ntawm lub plawv thiab cov txheej txheem ntawm kev ua.Acta Pharmacologica Sinica, 23(12), 1057-1068.
- Luan, F., He, X., & Zeng, N. (2020). Tetrandrine: kev tshuaj xyuas ntawm nws cov peev xwm tiv thaiv kab mob, chaw kho mob, chaw muag tshuaj thiab tshuaj xa tshuaj.Phau ntawv Journal of Pharmacy thiab Pharmacology, 72(11), 1491-1512.
- Gibbs, L. (2013). Tetrandrine: Ib Tus Neeg Saib Xyuas Kev Tiv Thaiv Novel. UNTHSC Scholar.
- Bhagya, N., & Chandrashekar, KR (2016). Tetrandrine - ib tug molecule ntawm dav bioactivity.Phytochemistry, 125, 5-13.
Tsis lees paub:Cov ntaub ntawv khoom lag luam no yog npaj rau kev lag luam - rau - kev lag luam (B2B) siv los ntawm cov kws tshaj lij tshawb fawb thiab cov koom haum tsim nyog. Cov nqe lus uas muaj nyob hauv no yog ua raws li cov ntaub ntawv tshawb fawb tam sim no thiab cov ntaub ntawv xa khoom thiab muab rau cov ntaub ntawv xov xwm nkaus xwb. Cov khoom no tsuas yog siv rau kev tshawb nrhiav. Tsis yog rau tib neeg noj, kev siv tshuaj ntsuam xyuas, lossis kev siv tshuaj kho mob. Nws yog tib lub luag haujlwm ntawm tus neeg yuav khoom kom ua raws li tag nrho cov kev cai hauv zos, teb chaws, thiab thoob ntiaj teb rau kev tshawb fawb siv. Cov lus qhia tshwj xeeb tuaj yeem hloov pauv yam tsis tau ceeb toom; ib txwm thov daim ntawv pov thawj tseeb ntawm Kev Ntsuam Xyuas ua ntej xaj xaj.
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