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prodrugs incorporated into nanotechnology-based drug delivery systems for possible improvement in bioavailability of ocular drugs delivery

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Asian Journal of Pharmaceutical Sciences 2013年第4期8卷 207-217页

作者： Tiantian Ye Kun Yuan Wenji Zhang Shuangshuang Song Fen Chen Xinggang Yang Shujun Wang Jianwei Bi Weisan Pan School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China Shangdong Wego Pharmaceutical Co.Ltd Weihai 264209China

Numerous systems have been designed during the past three decades to improve bioavailability of ophthalmic drug delivery,including:ocular prodrugs and nanotechnology-based drug delivery *** former can improve the efficacy of ocular drug via enhancing corneal penetration of ocular drugs,prolonging their duration of action and/or reducing the systemic side-effects,unfortunately,some characteristics of the pro-drugs,such as poorly aqueous stability,poorly aqueous solubility and severe eye irritation probably,limit their clinical practice and cannot be *** we all know,nanotech-nology for ocular drug delivery can carry poorly soluble drugs,protect the encapsulated molecules from hydrolysis,control the rate of drug delivery and prolong the precorneal retention of *** of these merits may solve the problems in the utilization of ocular prodrugs and increase the bioavailability of ocular drug *** reviewing recent ad-vances of prodrugs and nanostructures in ocular drug delivery,this paper focus specifically on the promising prospects of nanocarriers overcoming the drawbacks of prodrugs for ophthalmic drug delivery by precorneal routes.

关键词： Ocular/ophthalmic drug delivery prodrugs Nanocarriers Penetration Precorneal retention Bioavailability

Triphenylmethanol Conjugates of Triptorelin as Anti-Lipid Peroxidation prodrugs

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Open Journal of Medicinal Chemistry 2019年第3期9卷 49-62页

作者： Samiyah Alhamed Jawzah Alnakhli William Boadi Ryan Beni Department of Chemistry Tennessee State University Nashville TN USA

Antioxidants are substances that can prevent or slow damage to cells caused by free radicals, unstable molecules that the body produces as a reaction to environmental and other pressures. Free radicals may play a role in heart disease, cancer and other diseases. If the body cannot process and remove free radicals efficiently, oxidative stress can result. This can harm cells and body function. Free radicals are also known as reactive oxygen species (ROS). In this research, Triptorelin®(TRP) conjugates of triphenylmethanol derivatives (TPMs) were synthesized to evaluate their in vitro lipid peroxidation potency. Comparative lipid peroxidation assays between TRP-TPMs conjugates and the corresponding TPMs derivatives were measured using thiobarbituric reactive substance (TBARS) in a dose- and time-dependent manner following the Fenton’s pathway. Overall, TBARS decreased between 20% - 30% for the treated samples of synthesized conjugates compared to their respective control physical mixtures. These data suggest that TRP-TPMs derivatives can be used to improve the biological activity of TRP.

关键词： Antioxidants prodrugs Triptorelin Polyphenols Lipid Peroxidation Triphenylmethanol

Enzyme-mediated hydrolytic activation of prodrugs

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Acta Pharmaceutica Sinica B 2011年第3期1卷 143-159页

作者： Yan-hui Yang Herve Aloysius Daigo Inoyama Yu Chen Long-qin Hun Department of Medicinal Chemistry Ernest Mario School of PharmacyRutgersThe State University of New JerseyPiscatawayNJ 08854USA

Prodrug design is an important part of drug *** can offer many advantages over parent drugs such as increased solubility,enhanced stability,improved bioavailability,reduced side effects,and better *** prodrugs have been used successfully in the clinic;examples include oseltamivir in anti-influenza therapy,enalapril in anti-hypertension therapy,capecitabine in cancer therapy,and omeprazole in the treatment of peptic ulcer.A key step in prodrug design is the incorporation of an activation mechanism that can convert the prodrug into the active species in an efficient and/or controlled manner to meet the needs of a given medical *** activation can be achieved through enzyme-mediated hydrolytic or oxidoreductive processes while activation of some prodrugs may proceed through pure chemical nonenzymatic *** review focuses on the hydrolytic enzymes that have been used in prodrug activation,including transferases,hydrolases,and lyases.

关键词： prodrugs Hydrolytic activation Transferase Hydrolase Lyase

Triphenylmethanol Conjugates of Triptorelin as Cell-Penetrating Anti-Cancer prodrugs

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Journal of Biosciences and Medicines 2023年第11期11卷 208-218页

作者： Jawzah Alnakhli Samiyah Alhamed William Boadi Ryan Beni Department of Chemistry Tennessee State University Nashville USA

Some Triptorelin® (TRP) conjugates of triphenylmethanol derivatives (TPMs) with optimized hydrophobicity were synthesized by reacting 2-substituted methoxy benzenes with 1,3,5-trioxane, followed by the conjugation with TRP and sebacic acid to produce TRP-TPMs derivatives. Comparative antiproliferative assays between TRP-TPMs conjugates and the corresponding non-covalent physical mixtures of the TPMs derivatives and TRP were used to treat human acute lymphoblastic leukemia (CCRF-CEM), human ovarian adenocarcinoma (SK-OV-3) and mouse preadipocytes (3T3-L1) cells. TRP-TPMs conjugates at the 50 μM inhibited cell proliferation in CCRF-CEM, SK-OV-3 and 3T3-L1 cells by 21% - 37%, 24% - 73%, 37% - 56%, respectively following incubation for 72 h. These findings indicate that TRP-TPMs derivatives have the potential to enhance the biological activity of TRP.

关键词： prodrugs Triptorelin Polyphenols Prostate Cancer Triphenylmethanol

Synthesis and Evaluation of Glyceride prodrugs of Naproxen

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Open Journal of Medicinal Chemistry 2013年第3期3卷 87-92页

作者： Vivekkumar K. Redasani Sanjay B. Bari H. R. Patel Institute of Pharmaceutical Education and Research Shirpur India R. C. Patel Institute of Pharmaceutical Education and Research Shirpur India

The glyceride ester derivatives 6a and 6b were prepared by reacting 1,2,3-trihydroxy propane 1,3-dipalmitate/stearate with (S)-naproxen as potential prodrugs. The synthesis was achieved successfully with the aid of N,N’-dicyclohexyl- carbodiimide. These prodrugs were evaluated for anti inflammatory, analgesic and gastroprotective activity. It was found that prodrugs 6a and 6b showed less irritation to gastric mucosa as indicated by ulcer index. The synthesized glyceride esters were found to possess good pharmacological profile as shown by results of anti inflammatory and analgesic activity. The aqueous studies were performed in order to ensure the release of prodrugs. Both prodrugs were found to stable at acidic pH while undergoes hydrolysis at pH 7.4. These findings suggest that the glyceride prodrugs 6a and 6b might be used as potential biolabile derivatives.

关键词： Naproxen Glyceride prodrugs Anti-Inflammatory Analgesic Gastroprotective Hydrolysis Kinetics

Paclitaxel-lipid prodrug liposomes for improved drug delivery and breast carcinoma therapy

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Chinese Chemical Letters 2024年第2期35卷 335-340页

作者： Xin Wu Xinmei Chen Xinyu Wang Haisheng He Jianming Chen Wei Wu Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China Department of Pharmacy Fujian University of Traditional Chinese MedicineFuzhou 350122China Shanghai Wei Er Lab Shanghai 201707China Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China

Paclitaxel(PTX)is widely applied for the treatment of unresectable and metastasis breast carcinoma as well as other cancers,whereas its efficacy is always impeded by poor *** are one kind of the most successful drug carriers which are capable of solubilizing PTX and improving patients’tolerance owing to excellent biocompatibility and ***,poor compatibility between PTX and liposomes compromises the stability,drug loading and anti-tumor capacity of liposomal *** address this issue,three lipids with various chain lengths,namely,myristic acid(MA,14C),palmitic acid(PA,16C)and stearic acid(SA,18C),were conjugated to PTX via ester bonds and the synthesized prodrugs with high lipophilicity were further formulated into liposomes,*** liposomes show high stability and drug loadings,as well as sustained drug *** chain lengths of lipids are negatively correlated with drug release and enzymatic conversion rates,which further impact the pharmacokinetics,tumor accumulation,and anti-tumor efficacy of liposomal *** rapid nor slow drug release facilitates high tumor accumulation as well as anti-tumor efficacy of *** all liposomes,PTX-PA-loaded liposomes show the longest circulation and highest tumor accumulation of PTX and exert the most potent anti-tumor capacities in vivo,owing to its moderate drug release and enzymatic conversion *** its superior safety,PTX-PA liposomes hold potential for further clinical translation.

关键词： Paclitaxel Lipids prodrugs Liposomes Drug release Chemotherapy

Emerging non-antibody‒drug conjugates (non-ADCs) therapeutics of toxins for cancer treatment

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Acta Pharmaceutica Sinica B 2024年第4期14卷 1542-1559页

作者： Xiaolan Xu Jiaming Zhang Tao Wang Jing Li Yukang Rong Yanfang Wang Chenxia Bai Qing Yan Xiaohua Ran Yingli Wang Tianhong Zhang Jin Sun Qikun Jiang Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China School of Education University of NottinghamNottingham NG72RDUK Department of Pharmacy Linyi People's HospitalShandong UniversityLinyi 276000China State Key Laboratory of Natural and Biomimetic Drugs Peking UniversityBeijing 100871China

The non-selective cytotoxicity of toxins limits the clinical relevance of the *** recent years,toxins have been widely used as warheads for antibody-drug conjugates(ADCs)due to their eff-cient killing activity against various cancer *** ADCs confer certain targeting properties to the toxins,low drug loading capacity,possible immunogenicity,and other drawbacks also limit the po-tential application of ***,non-ADC delivery strategies for toxins have been extensively *** further understand the application of toxins in anti-tumor,this paper provided an over-view of prodrugs,nanodrug delivery systems,and biomimetic drug delivery *** addition,toxins and their combination strategies with other therapies were ***,the prospect and challenge of toxins in cancertreatmentwerealso summarized.

关键词： Toxins Non-antibody-drug conjugates Delivery strategies prodrugs Nano drug delivery systems Biomimetic drugdelivery systems Combination strategies Cancer treatment

The effect of lengths of branched-chain fatty alcohols on the efficacy and safety of docetaxel-prodrug nanoassemblies

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Acta Pharmaceutica Sinica B 2024年第3期14卷 1400-1411页

作者： Shuo Wang Tian Liu Yuetong Huang Chaoying Du Danping Wang Xiyan Wang Qingzhi Lv Zhonggui He Yinglei Zhai Bingjun Sun Jin Sun Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China School of Medical Devices Shenyang Pharmaceutical UniversityShenyang 110016China School of Pharmacy Binzhou Medical UniversityBinzhou 256600China

The self-assembly prodrugs are usually consisted of drug modules,activation modules,and assembly *** the balance between efficacy and safety by selecting suitable modules remains a challenge for developing prodrug *** study designed four docetaxel(DTX)prodrugs using disulfide bonds as activation modules and different lengths of branched-chain fatty alcohols as assembly modules(C_(16),C_(18),C_(20),and C_(24)).The lengths of the assembly modules determined the self-assembly ability of prodrugs and affected the activation modules’*** extension of the carbon chains improved the prodrugs’self-assembly ability and pharmacokinetic behavior while reducing the cytotoxicity and increased cumulative *** use of C_(20) can balance efficacy and *** results provide a great reference for the rational design of prodrug nanoassemblies.

关键词： prodrugs Nanoassemblies Self-assembly Branched-chain fatty alcohols Disulfide bond Docetaxel Efficacy Safety

Practical Synthesis of Valbenazine via 1,3-Dipolar Cycloaddition

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Chinese Journal of Chemistry 2024年第8期42卷 841-845页

作者： Yalan Peng Zuming Lin Lili Zhu Shiqing Han Sha-Hua Huang Ran Hong College of Biotechnology and Pharmaceutical Engineering Nanjing Tech UniversityNanjingJiangsu211816 China School of Environmental and Chemical Engineering Shanghai Institute of TechnologyShanghai201418 China State Key Laboratory of Chemical Biology Shanghai Institute of Organic ChemistryChinese Academy of SciencesShanghai200032 China Innovation Research Institute of Traditional Chinese Medicine(IRI) Shanghai University of Traditional Chinese Medicine1200 Cailun RoadShanghai201203 China

Comprehensive Summary,Valbenazine(Ingrezza),a potent and highly selective inhibitor of vesicular monoamine transporter type 2(VMAT2)through the active metabolite hydrotetrabenazine(HTBZ),has been approved for the treatment of tardive dyskinesia and,very recently,for chorea,which is associated with Huntington's *** numerous synthetic efforts dedicated to the synthesis of HTBZ,the industrial preparation of valbenazine uses dihydroisoquinoline as a starting material and the chiral resolution of racemic HTBZ derived from ketone ***,we present a practical synthesis of HTBZ and valbenazine featuring a highly stereoselective 1,3-dipolar cycloaddition and enzymatic kinetic *** cascade process includes cycloaddition,N—O bond cleavage,and lactamization,which proved to be operationally *** allure of the enzymatic resolution developed in this work offers a rapid access toward affording tetrahydroisoquinoline(THIQ)-fused piperidine in the production of medically significant compounds,such as yohimbine and reserpine.

关键词： Cycloaddition Chemoenzymatic Kinetic resolution prodrugs VMAT2 inhibitor