Anti-leishmanial activity

Amona muricata L. -graviola Tranquilizer No information Caboclos [59] Acetogenins [86,87] neurotoxic benzylisoquinoline derivatives [88] essential oil [89,90] alkaloids [91,92] flavonoids and terpenoids [93] striatal neurodegeneration [252] atypical parkinsonism [253] anti leishmanial activity [254] antidepressive activity [91]... 

These sialoglycans induce high humoral responses in the host and these antibodies have important application in the field of thettqty as well thqr have anti-leishmanial activity as reported by its capacity to induce complement lysis of parasite. Thus, sialoglycans appear to be important target molecules. 

Structuie-acdvity relationship studies with mitonafide have revealed that the compound inhibits both nuclear and mitochondrial topoisomerase of Leishmania with preferential taiget-ing of the mitochondrial enzyme over the nuclear enzyme. Anilinoacridines have recently been found to possess andparasidc activity towards Leishmania, Trypanosoma and Plasmodium species. These compounds have been shown to induce protein associated DNA lesions in L. chagasi promastigotes. Linearization of kinteoplast DNA minicirdes have also been repotted in parasites treated with anilinoacridines at similar concentrations. Members of the 9-anilinoacridine topoisomerase II inhibitors have also been shown to inhibit growth of L. major promast otes and amastigotes. 9-aminoacridines, that are reported topoisomerase II inhibitors and structurally related to the antileishmanial compound quinacrine and chlorpro-mazine, have shown anti leishmanial activity at concentrations in the range of 10-20 pM. ... 

Flere we present the anti-leishmanial activity of a set of S3nnmetrical bis-p3rridinium compounds with cyclic or acyclic structures. Both t)rpes of compoimds can be named according to the lUPAC nomenclature for phanes, a method based on assembling names that describe component parts of a complex structure. 

Table 2. Anti-leishmanial activity and toxicity in THP-1 cells of symmetrical bis-pyridinium compounds. ...

Gomez-Perez V, Manzano JI, Garcia-Hem dez R, Castanys S, Gamarro F, Campos Rosa JM. Design, s)mthesis and anti-leishmanial activity of novel S)nnmetrical bispyr-idinium cyclophanes. European Journal of Medicinal Chemistry 2015 89, 362-369. Doi 10.1016/j.ejmech.2014.10.040. 

Major Applications Fluorescent brighteners, fungicides, cosmetics, antitrypanosomal, " anti-leishmanial activities, " antifungal," antibacterial," Antiinflammatory, 12 antiHIV, detection of microorganisms, - treatment of impaired neurotransmission disorders, Alzheimer s disease, vascular and lymphatic edema cancer, early diagnosis of stroke, " dental material, " drug-coated coronary stent system ... 

Betulin (lup-20(29)-ene-3,28-diol) is an abundant naturally occurring triterpene, and it is found predominantly in bushes and trees forming the principal extractive (up to 30% of dry weight) of the bark of birch trees. Betulin and its derivatives such as betulinic acid have many interesting pharmacological properties, such as cytotoxic activity against many tumour cell lines and anti-HIV activity with a new mechanism of action. Several synthetic betulin derivatives that have been chemically modified at the positions C-3 and C-28 of the lupane skeleton were produced, and the anti-leishmanial inhibition activity of compounds was evaluated at 50 pM against Leishmania donovani and Leishmania tropica. Betulonic acid had the best anti-leishmanial activity with... 

Carballeira, N.M., Montano, N., Reguera, R.M., and Balania-Fouce, R. (2010) The first total synthesis of the ( )-17-methyl-tr s-4,5-mefhyleneoctadecanoic acid and related analogs with anti-leishmanial activity. Tetrahedron Lett., 51, 6153-6155. 

Organotin compounds have a wide range of other biological activities such as anti-oxidant, antiinflammatory and vasodepressant" amoebicidal, and anti-leishmanial, which have been described in a... 

To date no drugs preferentially target leishmanial components of the pyrimidine biosynthetic pathway. This is likely due to similarities in enzymatic activities shared between Leishmania and humans. For example, acivicin and PALA inhibit both human and leishmanial pyrimidine biosynthesis. Similarly, classical inhibitors such as methotrexate, which target leishmanial DHFR-TS, an essential component of thymidylate synthesis, are poor anti-leishmanial drugs because they also inhibit the human enzyme. ... 

Alkali mentholates were also involved in the first stereoselective synthesis of bismurrayaquinone A, an axially chiral biscarbazole alkaloid (Scheme 5.42). Naphthylisoquinoline alkaloids show interesting bioactivities, including strong anti-malarial and anti-leishmanial properties. Some of their dimers also exhibit high anti-HIV activities. The lactone concept allowed an efficient synthetic access to this class of alkaloids, such as korupensamines A and B (Scheme... 

Among new examples of linear peptides, dragonamide E and the series of almiramides A-C display potent anti-leishmanial adivity. All of these compounds were isolated from Lyngbya majuscula collected on the Caribbean coast of Panama (Bocas del Toro), and most of them are active with IC50 values ranging from 1.9 to 6.5 pM (Balunas et al, 2010 Sanchez et al, 2010). 

Quassinoids have attracted much attention due to the wide spectrum of biological activities that they display, viz., antimalarial, antifeedant, anti-inflanunatory, antiulcer, antipyretic, antifertility, antileukemic, cytotoxic activities, and induction of murine stem cell differentiation which have been widely reported [54-59]. We have demonstrated that quassin is a potent immunomodulatory tool that efficiently controls the estabhshment of leishmanial parasite within the host macrophages [60]. Our contention was that quassin could be used as a potential inununomodulator to generate the required immunity not only for the treatment of leishmaniasis but also for the treatment of other chronic infectious diseases. Subsequently, we had shown that both quassin and neoquassin can be used along with artesunate (a derivative of artemisinin) as combinatorial therapy against malaria [61]. 

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