Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines

Manda, Sudhakar; Khan, Shabana; Jain, S. K.; Mohammed, Shabber; Tekwani, Babu L.; Khan, Ikhlas A.; Vishwakarma, Ram A.; Bharate, Sandip B.

doi:10.1016/j.bmcl.2014.06.030

Cited by 46 publications

(35 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Compounds 1 – 5 were tested for their antiprotozoal activities against Leishmania donovani Promastigote, L. donovani Amastigote, L. donovani Amastigote/THP1 cells and T. b. brucei employing the methods described previously [11]. The in vitro antileishmanial and antitrypanosomal assays were done on cell cultures of L. donovani promastigotes, axenic amastigotes, THP1-amastigotes, and T. brucei trypomastigotes by Alamar Blue assays as described earlier [11].…”

Section: Methodsmentioning

confidence: 99%

“…The in vitro antileishmanial and antitrypanosomal assays were done on cell cultures of L. donovani promastigotes, axenic amastigotes, THP1-amastigotes, and T. brucei trypomastigotes by Alamar Blue assays as described earlier [11]. The assays have been adapted to 384 well micro-plate format.…”

Section: Methodsmentioning

confidence: 99%

“…The compounds were tested at three concentrations ranging from 40 to 1.6 μg/mL or 10–0.25 μg/mL. The plates were incubated at 26 °C for 72 h (37 °C for axenic amastigotes and T. brucei trypomastigotes) and growth of the parasites in cultures were determined by Alamar Blue assay [11]. The compounds were also tested against L. donovani intracellular amastigotes in THP1 cells employing a parasite-rescue and transformation assay [12].…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola

et al. 2015

Self Cite

View full text Add to dashboard Cite

Five new triterpenoid saponins, heinsiagenin A 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-β-d-glucopyranoside (1), heinsiagenin A 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→4)]-β-d-glucopyranoside (2), 2α-hydroxyheinsiagenin A 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-β-d-glucopyranoside (3), 2α-hydroxyheinsiagenin A 3-O-[β-d-glucopyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→4)]-β-d-glucopyranoside (4) and N-(2S, 3R, 4R-3-methyl-4-pentanolid-2-yl)-18-hydroxylanosta-8 (9), 22E, 24E-trien-27-amide-3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→4)]-β-d-glucopyranoside (5) were isolated from the aerial parts of Mussaenda luteola Delile (Rubiaceae). Structural elucidation was based on the analysis of spectroscopic data (1D and 2D NMR) and HR-ESI-MS. Compound 1 showed potent antitrypanosomal activity with an IC50 value of 8.80 μM. Compounds 2–4 showed highly potent antitrypanosomal activity with IC50 values ranging between (2.57–2.84 μM) and IC90 values ranging between (3.36–4.35 μM), which are 5 fold greater than the positive control DFMO (IC50 and IC90 values of 13.06 and 28.99 μM, respectively). Compounds 1 and 2 showed moderate affinity to μ-opioid receptors with Ki values of 9.936 μM and 0.872 μM, respectively compared to a Ki value of 1.958 nM for the positive control, naloxone HCl.

show abstract

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola

et al. 2015

Self Cite

View full text Add to dashboard Cite

show abstract

“…In a 384 well micro-plate, the samples with appropriate dilution were added to the cultures of protozoan cells (2 × 106 cell/mL). The plates were incubated at 26 °C for 72 h (37 o C for axenic amastigotes and T. brucei trypomastigotes) and growth of the parasites in cultures were determined by Alamar Blue assay [10,11]. The compounds were tested at concentrations ranging from 0.4-10 μg/mL.…”

Section: In Vitro Antiprotozoal Assaymentioning

confidence: 99%

“…All compounds were tested for their antiprotozoal activities against Leishmania donovani promastigote, L. donovani axenic amastigotes, intracellular L. donovani amastigotes/THP1 cells and Trypanosoma brucei [10]. The assays have been adapted to 384 well microplate format.…”

Section: In Vitro Antiprotozoal Assaymentioning

confidence: 99%

Evaluation of Secondary Metabolites from the Red Sea Tunicate Polyclinum Constellatum

Radwan¹

2017

PPIJ

View full text Add to dashboard Cite

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

Du,

Semghouli,

Mei

et al. 2024

Adv Synth Catal

View full text Add to dashboard Cite

Abstract. Tetrahydro‐β‐carbolines (THβCs) also known as tryptolines serve as important structural elements in natural products and pharmaceutical compounds, and they are also utilized in drug discovery. They display diverse bioactivities, including anticancer, antifungal, antiparasitic, anti‐ischemic, anti‐inflammatory, and other activities. Besides their pharmacological and biological significance, these structural motifs are also extensively used in the production of other bioactive compounds. This review is intended to summarize recent advancements in the chemistry of this compound class, including the synthesis and the applications as organic synthetic intermediates and bioactive molecules.

show abstract

Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines

Cited by 46 publications

References 26 publications

Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola

Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola

Evaluation of Secondary Metabolites from the Red Sea Tunicate Polyclinum Constellatum

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

Contact Info

Product

Resources

About