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  4. Ethambutol

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.

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Ethambutol Chemical Structure

Ethambutol Chemical Structure

CAS No. : 74-55-5

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Based on 1 publication(s) in Google Scholar

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Description

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases. Target: Antibacterial Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].

In Vivo

Induction of Hyperuricaemic Disease[4][5]
Background
Elevated uric acid levels can lead to crystal deposition and may cause gout, urolithiasis, and urate nephropathy. Ethambutol can cause increased uric acid levels by reducing renal uric acid clearance, ultimately leading to hyperuricemia[4][5].
Specific Mmodeling Methods
Rat[4]: male • Wistar rats • SPF • 200-220 g
Administrtion: 250 mg/kg • intragastric administration • once daily for 23 days
Note
Modeling Indicators
Pathological changes: Pathological damage and inflammatory reaction in the thymus and spleen; thymus atrophy, cortical medullary fusion; splenic sinus congestion, with iron yellow deposition.
Physiological changes: serum uric acid level ↑; sparse cells, increased number of tissue cells, and decreased number of lymphocytes.
Molecular changes: URAT1 level ↑, OAT1 level ↓ in kidney homogenate.
Correlated Product(s)
Opposite Product(s) Xanthine Oxidase Inhibitors