Julieth Correa-Royero

Synthesis and biological evaluation of dehydroabietic acid derivatives

A series of C18-oxygenated derivatives of dehydroabietic acid were synthesized from commercial abietic acid and evaluated for their cytotoxic, antimycotic, and antiviral activities.

Synthesis and biological evaluation of abietic acid derivatives.

A series of C18-oxygenated derivatives of abietic acid were synthesized and evaluated for their cytotoxic, antimycotic, and antiviral activities. In general, the introduction of an aldehyde group at C18 did improve the resultant bioactivity, while the presence of an acid or alcohol led to less active compounds.

In vitro antifungal activity and cytotoxic effect of essential oils and extracts of medicinal and aromatic plants against Candida krusei and Aspergillus fumigatus

As plantas sao geralmente utilizadas na medicina tradicional como agentes antimicrobianos e seus oleos essenciais e extratos foram conhecidos por possuir atividade antifungica. O objetivo deste estudo foi avaliar in vitro a atividade de 32 oleos essenciais e 29 extratos contra Candida krusei e Aspergillus fumigatus, bem como o efeito citotoxico em celulas Vero. A curva do tempo-morte e a interacao entre antifungicos e Chenopodium ambrosioidese do extrato de Myrcia cucullata mostraram atividade antifungica contra C. krusei (geometric means of the minimal inhibitory concentration [GM-MIC] 7,82 e 31,25 µg/mL, respectivamente). Lippia citriodora foi ativa contra C. krusei e A. fumigatus (GM-CIM = 99,21 µg/mL e 62,5 µg/mL, respectivamente). Os testes de tempo-morte feitos com oleo de C. ambrosioides mostraram atividade fungicida em 4x MIC. A interacao do oleo C. ambrosioides com itraconazol e anfotericina B foi testada pela tecnica de xadrez. Nenhuma interacao foi detectada pela combinacao do oleo C. ambrosioides com anfotericina B e itraconazol (intervalo fractional inhibitory index [FICI] = 1,03-1,06 e 1,03-1,00, respectivamente). Os ensaios de citotoxicidade para todas as amostras foram realizadas com MTT. Apenas os oleos Hedyosmun sp. e L. dulcis foram citotoxicos.

Anti-Candida albicans activity, cytotoxicity and interaction with antifungal drugs of essential oils and extracts from aromatic and medicinal plants

Objetivo. Determinar la actividad anti-Candida albicans, la citotoxicidad y la interaccion con antifungicos de aceites y extractos de plantas recolectadas en Colombia. Materiales y metodos. La actividad antifungica fue evaluada siguiendo el protocolo Antifungal Susceptibility Testing Subcommittee of the European Committee on Antimicrobial Susceptibility Testing (AFST-EUCAST). Con las muestras mas activas se evaluo la inhibicion de la formacion de tubogerminal y la gemacion, la farmacodinamia mediante curvas de tiempo muerte y la interaccion con itraconazol y anfotericina B. Se determino la citotoxicidad mediante la tecnica MTT.

Anti-dermatophyte, anti-Fusarium and cytotoxic activity of essential oils and plant extracts of Piper genus

Interest in medicinal and aromatic plants as a source of antimicrobial drugs has emerged, mainly due to increased resistance of infectious agents. In this study, the antifungal and cytotoxic activity of thirteen essential oils and nine extracts of plants of the genus Piper, from Colombia, were evaluated. The Piper hispidum Sw oil showed activity against the multi-resistant fungus Fusarium oxysporum. Six samples showed strong activity against dermatophytes, being Piper bogotense the most active, followed by P. hispidum. The oils from Piper hispidum, Piper coruscans, Piper marginatum and Piper cf. divaricatum, and the extract from Piper sanctifelicis, were not cytotoxic, unlike Piper bredemeyeri, Piper eriopodon and Piper bogotense oils, which exhibited significant cytotoxicity. The main components of the most active samples showed the presence of trans-β-caryophyllene. In addition, caryophyllene oxide, β-pinene and α-pinene were present in most antifungal oils at different concentrations. These results confirm the anti-mycotic potential of essential oils of the Piper genus against the most pathogenic fungi, as well as against important dermatological fungi.

Synthesis and biological evaluation of pyridinebetaine A and B

The synthesis of the marine natural products pyridinebetaine A and B is reported. The biological evaluation of pyridinebetaine A and B and several analogues as cytotoxic, antifungal and antiviral agents is also described. Unfortunately, none of the compounds tested showed relevant antifungal or cytotoxic activity. Only pyridinebetaine B reduced the Herpes simplex virus type 1 virus replication, though only weakly.

Synthesis and cytotoxic evaluation of novel 2-aryl-4-(4-hydroxy-3-methoxyphenyl)-3-methyl-6,7-methylendioxy-1,2,3,4-tetrahydroquinolines, podophyllotoxin-like molecules

Diverse 2-aryl-4-(4-hydroxy-3-methoxyphenyl)-3-methyl-6,7-methylendioxy-1,2,3,4-tetrahydroquinolines (DM series) were synthesized using three-component reaction of 3,4-methylendioxyaniline, benzaldehydes and isoeugenol. Purified and characterized tetrahydroquinoline molecules were tested in vitro for potential antitumor and cytotoxic activities. It was observed a strong relationship between selective cytotoxic activity on U937 and HeLa cells and the substitutions presented in aryl ring of position C-2 of the synthesized tetrahydroquinoline derivatives. Tested molecules, called DM108, DM116 and DM118, resulted in active compounds having a greater SI compared with colchicine and doxorubicin, reference compounds.