Anti-Helicobacter Pylori Potential of Artemisinin and Its Derivatives
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
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| Title |
Anti-Helicobacter Pylori Potential of Artemisinin and Its Derivatives
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| Creator |
Goswami, Suchandra
Bhakuni, Rajendra S Chinniah, Annalakshmi Pal, Anirban Kar, Sudip K Das, Pratap K |
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| Subject |
Drug Development/Diagnostics & Biotechnology
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| Description |
The antimalarial drug artemisinin from Artemisia annua demonstrated remarkably strong activity against Helicobacter pylori,
the pathogen responsible for peptic ulcer diseases. In an effort to develop a novel antimicrobial chemotherapeutic agent containing
such a sesquiterpene lactone endoperoxide, a series of analogues (2 natural and 15 semisynthetic molecules), including eight
newly synthesized compounds, were investigated against clinical and standard strains of H. pylori. The antimicrobial spectrum
against 10 H. pylori strains and a few other bacterial and fungal strains indicated specificity against the ulcer causing organism.
Of five promising molecules, a newly synthesized ether derivative �-artecyclopropylmether was found to be the most potent
compound, which exhibited MIC range, MIC90, and minimum bactericidal concentration range values of 0.25 to 1.0 �g/ml, 1.0
�g/ml, and 1 to 16 �g/ml, respectively, against both resistant and sensitive strains of H. pylori. The molecule demonstrated
strong bactericidal kinetics with extensive morphological degeneration, retained functional efficacy at stomach acidic pH unlike
clarithromycin, did not elicit drug resistance unlike metronidazole, and imparted sensitivity to resistant strains. It is not cytotoxic
and exhibits in vivo potentiality to reduce the H. pylori burden in a chronic infection model. Thus, �-artecyclopropylmether
could be a lead candidate for anti-H. pylori therapeutics. Since the recurrence of gastroduodenal ulcers is believed to be
mainly due to antibiotic resistance of the commensal organism H. pylori, development of a candidate drug from this finding is
warranted
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| Publisher |
American Society for Microbiology
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| Date |
2012
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://www.eprints.iicb.res.in/1713/1/ANTIMICROBIAL_AGENTS_AND_CHEMOTHERAPY___56_(_9_)__4594%2D4607;2012[42].pdf
Goswami, Suchandra and Bhakuni, Rajendra S and Chinniah, Annalakshmi and Pal, Anirban and Kar, Sudip K and Das, Pratap K (2012) Anti-Helicobacter Pylori Potential of Artemisinin and Its Derivatives. Antimicrobial Agents and Chemotherapy, 56 (9). pp. 4594-4607. |
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| Relation |
http://dx.doi.org/10.1128/AAC.00407-12
http://www.eprints.iicb.res.in/1713/ |
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