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Biotransformation of Sesquiterpenoids, Ionones, Damascones, Adamantanes, and Aromatic Compounds by Green Algae, Fungi, and Mammals
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Yoshinori Asakawa, Yoshiaki Noma
From hinesol (384), two allylic alcohols (386, 387) and their oxygenated derivative (385) and three unique metabolites (388–390) having oxirane ring were obtained. The metabolic pathway is very similar to that of oral administration of hinesol since the same metabolites (395–387) were obtained from the urine of rabbits (Hashimoto et al., 1998a, 1999b, 2001a,b) (Figure 23.110).
Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
Microbial epoxide hydrolases (EHs) catalyse the addition of one molecule of water to epoxides, allowing their hydrolysis for the formation of the corresponding vicinal diols (Widersen et al., 2010; Bala and Chimni, 2010). The EH from Candida viswanathii has been reported to be an effective enzyme for the non-selective hydrolysis of 2-(phenoxymethyl)oxirane to form the racemic 3-phenoxy-1,2-propanediol, which is a useful precursor of β-adrenoblockers, cardiovascular drugs and anti-bacterial agents, among others (Meena and Banerjee, 2010). Whole cell form of the microorganism provided over 90% conversion after 15 h at 30°C using a mixture of a buffer pH 7 and ethanol (Scheme 9.16). Hydrolysis of 2-(phenoxymethyl)oxirane with a whole cell EH from Candida viswanathii
Hits and Lead Discovery in the Identification of New Drugs against the Trypanosomatidic Infections
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Theodora Calogeropoulou, George E. Magoulas, Ina Pöhner, Joanna Panecka-Hofman, Pasquale Linciano, Stefania Ferrari, Nuno Santarem, Ma Dolores Jiménez-Antón, Ana Isabel Olías-Molero, José María Alunda, Anabela Cordeiro da Silva, Rebecca C. Wade, Maria Paola Costi
In recent years, naphthoquinone has drawn much attention as a scaffold with potential antitrypanosomatidic activity. Carneiro et al. (2012) reported the synthesis of new oxirane derivatives using naphthoquinones as starting materials. Even though most of the synthesized compounds proved more active than the reference drug benznidazole (IC50 = 11.5 μM, CC50 = 48 μM) against epimastigote forms of T. cruzi, only compound 27 (Figure 14) exhibited comparable cytotoxicity (IC50 = 0.09 μM, CC50 = 44 μM). Structure of the most active oxirane derivative 27.
Fluorinated vectors for gene delivery
Published in Expert Opinion on Drug Delivery, 2022
Yu Wan, Yuhan Yang, Mingyu Wu, Shun Feng
There are many other cationic polymeric gene carriers which had employed fluorination modification to improve gene transfection efficacy. For example, Gong and coworkers prepared a series of degradable poly(β-amino ester) with fluorinated side chains, which had excellent gene transfection efficacy and low toxicity [83]. It has been reported that fluorination modification for improving transfection efficacy also worked well on poly(propylene imine) dendrimers [29]. Besides, some fluorinated copolymers have been designed to deliver genes as well. For instance, a fluoropolymer composed of bis(oxirane) and dimethyldipropylene triamine was used for the co-delivery of miRNA and fluorine-containing drug sorafenib in the treatment of liver fibrosis [84]. Another block fluoropolymers of poly(2-dimethylaminoethyl methacrylate) (pDMAEMA) and poly(heptafluorobutyl methacrylate) (pHFMA) also exhibited excellent performance in DNA delivery [49]. Furthermore, Oupicky’s group designed a series of fluorinated copolymers containing N, N’-hexamethylenebisacrylamide and AMD3100, a C-X-C chemokine receptor type 4 antagonist, used in the preparation of PFC nano-emulsions to improve the siRNA delivery efficacy for cancer treatment [85–88].
Intravenous fosfomycin for the treatment of multidrug-resistant pathogens: what is the evidence on dosing regimens?
Published in Expert Review of Anti-infective Therapy, 2019
George Dimopoulos, Despoina Koulenti, Suzanne L. Parker, Jason A. Roberts, Kostoula Arvaniti, Garyphalia Poulakou
Plasmid- or transposon-mediated resistance mechanisms cause enzymatic inactivation of fosfomycin [8,20]. Fosfomycin resistance proteins that cause fosfomycin modification are FosA, FosB, and FosX. They are all members of the same metalloenzyme superfamily, the divalent metal-ion dependent enzymes, and, although different in terms of chemical mechanism, they all catalyze and open the oxirane ring of fosfomycin, resulting to inactivation of the antibiotic [18]. While the contribution of fosfomycin inactivating enzymes in emergence and spread of fosfomycin resistance does not seem worrisome at present (considered low to moderate), their presence in transferable plasmids represents a potential risk of resistance spread in the future [19].
Covalent immobilization of oxylipin biosynthetic enzymes on nanoporous rice husk silica for production of cis(+)-12-oxophytodienoic acid
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Thu Bao Le, Chong Soo Han, Kyoungwon Cho, Oksoo Han
RHS was activated with APTES as described above. Polyethylene glycol (PEG) (20 mg) was activated by incubating with 4 ml 50% v/v epichlorohydrin (ECH) for 12 h at 25 °C followed by bubbling with N2 for 6 h, which resulted in the introduction of highly reactive oxirane groups at both ends of the PEG molecules [19]. The ECH-PEG complexes (≈ 20 mg) were coupled to 10 mg activated RHS by gentle shaking at 25 °C for 12 h. Proteins were immobilized onto the ECH-PEG-linked RHS following the same protocol described above for immobilizing enzymes onto the GDA-linked RHS.