leishmaniasis

Dapsone (Sulphadione) has activity against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae.

Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death. Paromomycin Sulfate (Aminosidine sulfate) is the sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria.

Miltefosine (HePC) is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agents produce some potency against visceral or cutaneous leishmaniasis, however a 2005 survey concluded that miltefosine is the only effective oral treatment for both forms of leishmaniasis.

LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.

DNDI-6148 has anti-experimental cutaneous leishmaniasis activity and can be used to study visceral leishmaniasis by inhibiting Leishmania protozoa cleavage and polyadenylation-specific factor (CPSF3) endonuclease.

Paromomycin (Sulfate Salt) is an aminoglycoside that is active against Gram-negative and many Gram-positive bacteria as well as some protozoa and cestodes. Paromomycin in combination with sodium stibogluconate has proven to be effective in African and Indian VL (visceral leishmaniasis) and improves survival in African VL[3]. PS (Paromomycin Sulfate) is effective for elimination of B. coli without hematological side effects[4]. The activity of phosphoglucose isomerase was slightly inhibited by 10(-3) M paromomycin sulfate while those of hexokinase, phosphofructokinase and glucose-6-phosphate dehydrogenase were not inhibited[5]. In addition, with regard to correlation of endotoxemia with renal impairment, endogenous creatinine clearance and p-aminohippurate clearance were significantly improved (P less than 0.02) in those patients whose endotoxemia disappeared on paromomycin sulfate administration. Paromomycin sulfate seems to be effective in the prevention of endotoxemia and the associated renal impairment in cirrhosis in man[6]. Significantly higher frequencies of resistance to paromomycin, kanamycin, neomycin and tobramycin were observed in S. aureus isolates from PS (paromomycin supplemented) birds. Paromomycin supplementation resulted in resistance to aminoglycosides in bacteria of PS turkeys. Co-selection for resistance to other antimicrobial agents was observed in E. coli isolates[7].

Aminoquinol diphosphate may be useful in the treatment of acute necrotising cutaneous leishmaniasis.

Calceolarioside A shows potent activity against visceral leishmaniasis. It can induce a dose-related aggregant effect on rabbit platelets, which may be partly related to a calcium-dependent mechanism. Calceolarioside A also has potent antioxidative activi

Antileishmanial agent-10 (Compound 7h) is an antiprotozoal agent effective against leishmaniasis.

GNF6702 is a selective inhibitor of the kinetoplastid proteasome, demonstrating efficacy against parasites in mouse models of leishmaniasis, Chagas disease, and human African trypanosomiasis.

N-(2-Hydroxypropyl)methacrylamide is utilized in the synthesis of copolymers for the targeted delivery of antileishmanial agents in [Visceral leishmaniasis].

PK 11195 (RP 52028) is a TSPO ligand for neuroimaging that exhibits significant protection against CoCl2-induced alterations and can be used to study leishmaniasis.

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

Lyoniside and saracoside are cytotoxic to promastigotes and intracellular amastigotes, they demonstrate strong anti-leishmanial efficacies in BALB/c mice model of leishmaniasis, suggests that these two compounds potential anti-leishmanial candidates. The

Acivicin (AT-125), a chlorinated amino acid antibiotic produced by Streptomyces porcineus, is a γ-glutamyl transpeptidase (GGT) inhibitor that crosses the blood-brain barrier, exhibits anticancer and antiparasitic activity, and is used in the study of visceral leishmaniasis.

Benzoxonium chloride, The topical treatment of anthroponotic cutaneous leishmaniasis with the tincture of thioxolone plus benzoxonium chloride (Thio-Ben) along with cryotherapy.

Aminoquinol triphosphate may be useful in the treatment of acute necrotising cutaneous leishmaniasis.

Trypanothione synthetase-IN-4, a L. infantumTryS inhibitor, exhibits a strong anti-leishmanicidal effect (EC50: 0.6 μM, SI) dependent on the concentration of the polyamine substrate and can be used to study leishmaniasis.

PT4 is a treatment agent for Cutaneous leishmaniasis (CL). PT4 decreases of mitochondrial membrane potential and increases reactive oxygen species production, therefore leads to parasite death. PT4 is effective against both species of Leishmania. The IC50 values of PT4 against L. amazonensis and L. braziliensis are 125.18 and 233.18 μM , respectively. PT4 also shows potent anti-inflammatory activity in vivo [1].

LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL).

Antimony potassium tartrate trihydrate, known for its potent emetic properties, is utilized in treating schistosomiasis and leishmaniasis.