Literature DB >> 35852367

Leishmania donovani Dipeptidylcarboxypeptidase Inhibitor as a Potential Oral Treatment for Visceral Leishmaniasis.

Karthik Ramalingam1, Sonali Gangwar1,2, Deep Chandra Balodi1,2, Apeksha Anand1,2, Shailendra Yadav1,2, Subhasish Biswas3, Anil Kumar Karunakaran Sasikala3, Kailash Chand Gupta4, Sanjay Batra3,2, Neena Goyal1,2.   

Abstract

Chemotherapy is the key intervention to control visceral leishmaniasis (VL), a neglected tropical disease. Current regimens include not only a few drugs but also present several drawbacks, including moderate to severe toxicity, cost, long-term administration, patient compliance, and growing drug resistance. Thus, the need for better treatment options against VL is a priority. In an endeavor to find an orally active and affordable antileishmanial agent, we evaluated the therapeutic potential of compounds belonging to the (2Z,2'Z)-3,3'-(ethane-1,2-diylbis(azanediyl))bis(1-(4-halophenyl)-6-hydroxyhex-2-en-1-ones) series, identified as inhibitor(s) of Leishmania donovani dipeptidylcarboxypeptidase, a novel drug target. Among them, compound 3c exhibited best in vivo antileishmanial efficacy via both intraperitoneal and oral routes. Therefore, the present study led to the identification of compound 3c as the lead candidate for treating VL.

Entities:  

Keywords:  Leishmania donovani; dipeptidylcarboxypeptidase; in vivo efficacy; inhibitor; visceral leishmaniasis

Mesh:

Substances:

Year:  2022        PMID: 35852367      PMCID: PMC9380552          DOI: 10.1128/aac.02361-21

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.938


  23 in total

Review 1.  Leishmaniasis chemotherapy--challenges and opportunities.

Authors:  S L Croft; P Olliaro
Journal:  Clin Microbiol Infect       Date:  2011-10       Impact factor: 8.067

2.  A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.

Authors:  M M Bradford
Journal:  Anal Biochem       Date:  1976-05-07       Impact factor: 3.365

3.  Cloning and characterization of angiotensin converting enzyme related dipeptidylcarboxypeptidase from Leishmania donovani.

Authors:  Neena Goyal; Robert Duncan; Angamuthu Selvapandiyan; Alain Debrabant; Mirza S Baig; Hira L Nakhasi
Journal:  Mol Biochem Parasitol       Date:  2005-10-12       Impact factor: 1.759

4.  The hamster as a model of human visceral leishmaniasis: progressive disease and impaired generation of nitric oxide in the face of a prominent Th1-like cytokine response.

Authors:  P C Melby; B Chandrasekar; W Zhao; J E Coe
Journal:  J Immunol       Date:  2001-02-01       Impact factor: 5.422

5.  Cleavage of structural proteins during the assembly of the head of bacteriophage T4.

Authors:  U K Laemmli
Journal:  Nature       Date:  1970-08-15       Impact factor: 49.962

6.  A comparison of three methods of estimating EC50 in studies of drug resistance of malaria parasites.

Authors:  W Huber; J C Koella
Journal:  Acta Trop       Date:  1993-12       Impact factor: 3.112

7.  Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays.

Authors:  T Mosmann
Journal:  J Immunol Methods       Date:  1983-12-16       Impact factor: 2.303

Review 8.  Recent advances in leishmaniasis treatment.

Authors:  Tatiana S Tiuman; Adriana O Santos; Tânia Ueda-Nakamura; Benedito P Dias Filho; Celso V Nakamura
Journal:  Int J Infect Dis       Date:  2011-05-24       Impact factor: 3.623

9.  Exploration of antileishmanial activity in heterocycles; results of their in vivo & in vitro bioevaluations.

Authors:  S Bhatnagar; P Y Guru; J C Katiyar; R Srivastava; A Mukherjee; M S Akhtar; M Seth; A P Bhaduri
Journal:  Indian J Med Res       Date:  1989-11       Impact factor: 2.375

10.  Leishmaniasis worldwide and global estimates of its incidence.

Authors:  Jorge Alvar; Iván D Vélez; Caryn Bern; Mercé Herrero; Philippe Desjeux; Jorge Cano; Jean Jannin; Margriet den Boer
Journal:  PLoS One       Date:  2012-05-31       Impact factor: 3.240

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