Limits...
Indole alkaloids from marine sources as potential leads against infectious diseases.

França PH, Barbosa DP, da Silva DL, Ribeiro ÊA, Santana AE, Santos BV, Barbosa-Filho JM, Quintans JS, Barreto RS, Quintans-Júnior LJ, de Araújo-Júnior JX - Biomed Res Int (2014)

Bottom Line: Indole alkaloids comprise a large and complex class of natural products found in a variety of marine sources.Furthermore, the emerging resistance against these drugs makes it urgently necessary to discover and develop new, safe and, effective anti-infective agents.In this regard, the aim of this review is to highlight indole alkaloids from marine sources which have been shown to demonstrate activity against infectious diseases.

View Article: PubMed Central - PubMed

Affiliation: Institute of Chemistry and Biotechnology, Federal University of Alagoas, University City, BR 101, KM 14 Norte, Tabuleiro dos Martins, 57072-970 Maceio, AL, Brazil.

ABSTRACT
Indole alkaloids comprise a large and complex class of natural products found in a variety of marine sources. Infectious diseases remain a major threat to public health, and in the absence of long-term protective vaccines, the control of these infectious diseases is based on a small number of chemotherapeutic agents. Furthermore, the emerging resistance against these drugs makes it urgently necessary to discover and develop new, safe and, effective anti-infective agents. In this regard, the aim of this review is to highlight indole alkaloids from marine sources which have been shown to demonstrate activity against infectious diseases.

Show MeSH

Related in: MedlinePlus

Structures of fascaplysin and homofascaplysin A.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4066687&req=5

fig6: Structures of fascaplysin and homofascaplysin A.

Mentions: From the CH2Cl2 extract of the sponge Hyrtios cf. erecta, collected in Fiji, β-carbolines homofascaplysin A and fascaplysin (Figure 6) were isolated. Evaluation of the biological activity of the compounds toward P. falciparum revealed that homofascaplysin and fascaplysin are both potently active in vitro against the parasite. Homofascaplysin A also inhibited the growth of Escherichia coli (50 μg/9 mm) and Bacillus megaterium (50 μg/11 mm). Fascaplysin inhibited the growth of E. coli (50 μg/6 mm) and B. megaterium (50 μg/10 mm). Further biological activity for fascaplysin was found against Trypanosoma b. rhodesiense, displaying moderate activity with IC50 value of 0.17 μg/mL compared with melarsoprol, which showed IC50 value of 2 ng/mL. The evaluation of antiviral activity of fascaplysin revealed an increased cytopathogenic effect at noncytotoxic concentrations of 0.038 μg/mL toward fetal Rhesus monkey kidney cells (FRhK-4-cells) infected with the HAV-variant HAVcytHB1.1. Persistently infected FRhK-4-cells (HAV/7) showed cytopathogenicity at 0.038 μg/mL of fascaplysin, while untreated FRhK-4-cells remained unchanged. Homofascaplysin A and fascaplysin were shown to be potent in vitro inhibitors of chloroquine-susceptible (NF54) and chloroquine-resistant P. falciparum strains. Positive control substances were chloroquine and artemisinin. The potency against the K1 strain of homofascaplysin A was stronger than that of chloroquine. Compared with artemisinin (K1 strain) and with both positive control substances (NF54 strain), homofascaplysin was approximately 10-fold less active [81].


Indole alkaloids from marine sources as potential leads against infectious diseases.

França PH, Barbosa DP, da Silva DL, Ribeiro ÊA, Santana AE, Santos BV, Barbosa-Filho JM, Quintans JS, Barreto RS, Quintans-Júnior LJ, de Araújo-Júnior JX - Biomed Res Int (2014)

Structures of fascaplysin and homofascaplysin A.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4066687&req=5

fig6: Structures of fascaplysin and homofascaplysin A.
Mentions: From the CH2Cl2 extract of the sponge Hyrtios cf. erecta, collected in Fiji, β-carbolines homofascaplysin A and fascaplysin (Figure 6) were isolated. Evaluation of the biological activity of the compounds toward P. falciparum revealed that homofascaplysin and fascaplysin are both potently active in vitro against the parasite. Homofascaplysin A also inhibited the growth of Escherichia coli (50 μg/9 mm) and Bacillus megaterium (50 μg/11 mm). Fascaplysin inhibited the growth of E. coli (50 μg/6 mm) and B. megaterium (50 μg/10 mm). Further biological activity for fascaplysin was found against Trypanosoma b. rhodesiense, displaying moderate activity with IC50 value of 0.17 μg/mL compared with melarsoprol, which showed IC50 value of 2 ng/mL. The evaluation of antiviral activity of fascaplysin revealed an increased cytopathogenic effect at noncytotoxic concentrations of 0.038 μg/mL toward fetal Rhesus monkey kidney cells (FRhK-4-cells) infected with the HAV-variant HAVcytHB1.1. Persistently infected FRhK-4-cells (HAV/7) showed cytopathogenicity at 0.038 μg/mL of fascaplysin, while untreated FRhK-4-cells remained unchanged. Homofascaplysin A and fascaplysin were shown to be potent in vitro inhibitors of chloroquine-susceptible (NF54) and chloroquine-resistant P. falciparum strains. Positive control substances were chloroquine and artemisinin. The potency against the K1 strain of homofascaplysin A was stronger than that of chloroquine. Compared with artemisinin (K1 strain) and with both positive control substances (NF54 strain), homofascaplysin was approximately 10-fold less active [81].

Bottom Line: Indole alkaloids comprise a large and complex class of natural products found in a variety of marine sources.Furthermore, the emerging resistance against these drugs makes it urgently necessary to discover and develop new, safe and, effective anti-infective agents.In this regard, the aim of this review is to highlight indole alkaloids from marine sources which have been shown to demonstrate activity against infectious diseases.

View Article: PubMed Central - PubMed

Affiliation: Institute of Chemistry and Biotechnology, Federal University of Alagoas, University City, BR 101, KM 14 Norte, Tabuleiro dos Martins, 57072-970 Maceio, AL, Brazil.

ABSTRACT
Indole alkaloids comprise a large and complex class of natural products found in a variety of marine sources. Infectious diseases remain a major threat to public health, and in the absence of long-term protective vaccines, the control of these infectious diseases is based on a small number of chemotherapeutic agents. Furthermore, the emerging resistance against these drugs makes it urgently necessary to discover and develop new, safe and, effective anti-infective agents. In this regard, the aim of this review is to highlight indole alkaloids from marine sources which have been shown to demonstrate activity against infectious diseases.

Show MeSH
Related in: MedlinePlus