青霉素【CAS 61-33-6】

青霉素(Benzylpenicillin,61-33-6)概述：
1.Penicillin G is a broad-spectrum, beta-lactam naturally occurring penicillin antibiotic with antibacterial activity. Penicillin G binds to and inactivates the penicillin binding proteins (PBPs) located inside the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and eventually causing cell lysis.
2.Penicillin G is narrow spectrum antibiotic used to treat infections caused by susceptible bacteria. It is a natural penicillin antibiotic that is administered intravenously or intramuscularly due to poor oral absorption. Penicillin G may also be used in some cases as prophylaxis against susceptible organisms. Natural penicillins are considered the drugs of choice for several infections caused by susceptible gram positive aerobic organisms, such as Streptococcus pneumoniae, groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus. Aminoglycosides may be added for synergy against group B streptococcus (S. agalactiae), S. viridans, and Enterococcus faecalis. The natural penicillins may also be used as first or second line agents against susceptible gram positive aerobic bacilli such as Bacillus anthracis, Corynebacterium diphtheriae, and Erysipelothrix rhusiopathiae. Natural penicillins have limited activity against gram negative organisms; however, they may be used in some cases to treat infections caused by Neisseria meningitidis and Pasteurella. They are not generally used to treat anaerobic infections. Resistance patterns, susceptibility and treatment guidelines vary across regions.
3.Penicillin G and V are first generation penicillins that are used widely to treat infections due to susceptible organisms and have been linked rarely and only weakly with idiosyncratic liver injury.

1.Effect of penicillin G on the biliary excretion of cholephilic compounds in rats /Masako Fukami Atsushi Tanka Hajime Takikawa
Abstract:
Aim:Penicillin G is reported to increase bile flow by increasing biliary glutathione excretion, as well as the biliary excretion of penicillin G itself. In order to study the effect of penicillin G on the hepatic excretory pathway, the effect of colchicine and genipin on the increase of biliary glutathione excretion induced by penicillin G was studied in rats. The effect of penicillin G on the biliary excretion of sulfobromophthalein and erythromycin was also studied, together with the effect of penicillin G on cholestasis induced by estradiol‐17β‐glucuronide.
Methods:After bile duct cannulation, penicillin G was administered to rats at the rate of 0.5 μmol/min/100 g. The effect was examined of colchicine pretreatment (0.2 mg/100 g) and genipin administration (0.5 μmol/min/100 g) on biliary glutathione excretion increased by penicillin G infused at the rate of 0.5 μmol/min/100 g. The effect of penicillin G on the biliary excretion of sulfobromophthalein and erythromycin (0.2 and 0.1 μmol/min/100 g for 90 min, respectively) was studied, together with the effect of penicillin G on cholestasis induced by estradiol‐17β‐glucuronide (0.075 μmol/min/100 g for 20 min).
Results:Penicillin G increased bile flow and biliary glutathione excretion, which were not inhibited by colchicine or genipin. Biliary penicillin G excretion was markedly reduced in Eisai hyperbilirubinemic rats (EHBR) and Mrp2‐deficient rats. Biliary sulfobromophthalein and erythromycin excretion was unchanged by penicillin G. Cholestasis induced by estradiol‐17β‐glucuronide was not relieved by penicillin G.
Conclusions:It was shown that colchicine‐sensitive vesicular transport has no role on the penicillin G‐induced insertion of Mrp2 into the canalicular membrane, as has been observed with genipin. Although the choleresis of penicillin G is thought to be due to the increased biliary excretion of glutathione and penicillin G itself by Mrp2, the mechanism of Mrp2 insertion by penicillin G is thought to be partly different from that by genipin.
2.Facilitated Transport of Penicillin G by Bulk Liquid Membrane with TBP as Carrier/Zhongqi Ren, Yuanyuan Lv & Weidong Zhang Applied Biochemistry and Biotechnology volume 152, pages286–294 (2009)
2.Facilitated Transport of Penicillin G by Bulk Liquid Membrane with TBP as Carrier/Zhongqi Ren, Yuanyuan Lv & Weidong Zhang Applied Biochemistry and Biotechnology volume 152, pages286–294 (2009)
Abstract:The facilitated transport of penicillin G from aqueous solutions to the stripping phase through bulk liquid membrane (BLM) containing TBP in 3% iso-octanol and n-butyl acetate was studied. Na2CO3 solution was used as the stripping phase. Experiments were performed as a function of stirring rate, TBP concentration and type of diluent in the liquid membrane phase, pH, and initial penicillin G concentration in the feed phase, Na2CO3 concentration in the stripping phase, etc. The results showed that the BLM process could carry out the simultaneous separation and concentration of penicillin G from dilute aqueous solutions, and arise “up-hill” effect due to the characteristic of non-equilibrium mass transfer. The diffusion of penicillin G complex in the liquid membrane phase played an important role in BLM process. The mass transfer mechanism of BLM for this system was also discussed.