Synthesis, in vitro anti-inflammatory and cytotoxic evaluation, and mechanism of action studies of 1-benzoyl-β-carboline and 1-benzoyl-3-carboxy-β-carboline derivatives

Constituents from Vigna vexillata and Their Anti-Inflammatory Activity

“…Therefore, those purified compounds isolated in sufficient quantity were evaluated for inhibition of superoxide anion generation and elastase release by human neutrophils in response to FMLP/CB (Table 2) and 1 , 3 , 19 , 22 , 23 , 25 , and 40 at 10 μM concentration exhibited the inhibition percentages higher than 50%. Among those examined constituents, daidzein ( 23 ), abscisic acid ( 25 ), and quercetin ( 40 ) displayed the most significant inhibition of superoxide anion generation and elastase release with IC 50 values ranged from 2.66 ± 0.85 to 5.51 ± 1.07 μM, compared with the reference compound LY294002 [60], which displayed IC 50 of 1.38 ± 0.22 and 1.95 ± 0.35 μM towards superoxide anion generation and elastase release, respectively. In addition, diphenyleniodonium (DPI), a NADPH oxidase inhibitor, was also used as a positive control for superoxide anion generation with IC 50 of 0.93 ± 0.52 μM.…”

The effect of CA1 dopaminergic system in harmaline-induced amnesia

“…The b-carboline alkaloids indicate modest affinity to 5-HT, dopamine and benzodiazepine receptors (Glennon et al, 2000). These alkaloids influence central neurotransmitters such as dopamine (Moura et al, 2006;Nasehi et al, 2010Nasehi et al, , 2012, via inhibition of monoamine reuptake systems (Kleven and Woolverton, 1993;Baum et al, 1996;Yang et al, 2011), and inhibition MAO-A or B (Glennon et al, 2000;Touiki et al, 2005). Some evidences displayed that harmaline change the extracellular and tissue level of dopamine (Kim et al, 1970;Glick et al, 1994Glick et al, , 1996.…”

“…The D1 receptor interacts with the Gs complex to activate adenyl cyclase, but the D2 interacts with Gi to inhibit cyclic adenosine monophosphate production (Bressan and Crippa, 2005;Ferreira et al, 2011). Some evidence reported that harmaline could influence dopaminergic transmission (Kim et al, 1970;Palmery et al, 1992), which may be done by inhibition of MAO-A or MAO-B (Herraiz and Chaparro, 2005;Touiki et al, 2005;Talhout et al, 2007;Yang et al, 2011). Since harmaline and dopamine receptors have interaction (Kim et al, 1970;Palmery et al, 1992), and considering the role of dopamine receptors (Kandel and Weeks, 1995;Wise, 2004;de Lima et al, 2011), harmaline (Meignin et al, 1999), and hippocampus (Whishaw, 1998;Burgess et al, 2002;Harvey, 2003;Faerber et al, 2007) in memory process, we attempt to determine the role of harmaline and dopamine receptors in memory acquisition and locomotor activity in the step-down passive avoidance and open field test.…”

“…In the human body, the b-carbolines may be formed from the biogenic amines tryptamine and 5-HT through condensation with aldehydes or a-keto acids (Talhout et al, 2007;Rook et al, 2010). Several investigations indicate a wide spectrum of therapeutic activities for the b-carbolines such as antinociceptive effect (Nenaah, 2010), neuroregulatory effect (Munoz et al, 2000;Splettstoesser et al, 2005;Moura et al, 2006), antibiotic properties (Martin et al, 1997;Hamsa and Kuttan, 2010;Yang et al, 2011), antidepressant-like effect (Herraiz and Chaparro, 2005), learning processes (Venault and Chapouthier, 2007), and excitation (Rommelspacher et al, 1980). The b-carboline alkaloids may act in biological tissues, such as the heart, kidney, liver and brain tissue (Ruiz-Durantez et al, 2001;Splettstoesser et al, 2005;Moura et al, 2006;Rook et al, 2010;Nasehi et al, 2012).…”

Manganese dioxide mediated one-pot synthesis of methyl 9H-pyrido[3,4-b]indole-1-carboxylate: Concise synthesis of alangiobussinine

“…Carbolines are an important class of naturally occurring compounds containing the β-carboline motif found in a number of biologically active molecules, and which have recently been shown to be active against Alzheimer’s disease [1–2], bacterial infection [3], inflammation [4–5], HIV and AIDS [6] and various forms of cancers [7–12]. The wide range of therapeutic applications of these molecules highlights the importance of carbolines as a synthetic target in medicinal chemistry.…”