Antiproliferative Effect of Synadenium grantii Hook f. stems (Euphorbiaceae) and a Rare Phorbol Diterpene Ester

Abstract

Synadenium grantii is frequently used for the treatment of various diseases such as allergies, gastric disorders, and especially cancer. The aim of this study was to evaluate the possible antiproliferative potential of the methanol extract, fractions, and pure compounds from the stems of S grantii Phytochemical analysis was carried out by conventional chromatographic techniques, and the antiproliferative activity was analyzed using the sulforhodamine B assay and an MTT-based assay. Nonpolar fraction and its subfractions from the stems of S grantii exhibited promising cytostatic effect against several human tumor cell lines (glioma, breast, kidney, and lung), with total grown inhibition values ranging from 0.37 to 2.9 μg/mL. One of the active principles of this plant was identified as a rare phorbol diterpene ester, denoted as 3,4,12,13-tetraacetylphorbol-20-phenylacetate. This compound demonstrated antiproliferative activity against glioma, kidney, lung, and triple-negative breast cancer cell lines. These results demonstrate that S grantii stems produce active principles with relevant antiproliferative potential.

Reactivation of latent HIV-1 in vitro using an ethanolic extract from Euphorbia umbellata (Euphorbiaceae) latex

“…Some modifications at their phorbol ring can generate molecules able to induce carcinogenesis or lead to molecules that are unable to induce carcinogenesis but retain their PKC activation capacity (such as a deoxy group on ring position 4 –the 4-deoxyphorbol) [ 48 ]. The presence of this modification was identified in our JALEx during the chemical analysis and also in a previous study performed with Euphorbia umbellata latex [ 42 ]. Therefore, JALEx is not likely to induce carcinogenesis but it retains its the capacity to activate PKC proteins and consequently reactivate HIV/SIV latency.…”

“…A phorbol ester-rich fraction was obtained by chromatographing crude JALEx in a silica gel open column using mixtures of chloroform-ether as eluent (Ph1 and Ph 2— Fig 1 ). The class of phorbol ester has been represented by the 12-O-tigloyl-4-deoxyphorbol-13-isobutirate [ 40 ], 12-deoxyphorbol-13-(2-methylpropionate), phorbol 12,13,20-triacetate [ 41 ], 4-deoxyphorbol-12,13-ditiglate and 3,4,12,13-tetraacetylphorbol-20-phenylacetate [ 42 ] distributed in several plant tissues ( S1 Fig ).…”

Enriched Terpenes Fractions of the Latex of Euphorbia umbellata Promote Apoptosis in Leukemic Cells

“…It is already established in literature the influence of terpenes on cytotoxic activity, especially diterpenes, which are present in Dcm and Eth. [15] Intermediate polarity fractions were more cytotoxic to tumoral cells, including leukemia cell lines; [12,22,23] this may be a result of the chemical affinity of terpenes (di-and triterpenes) with such solvents. [15] Therefore, some mechanisms were evaluated for these two fractions against HL-60 lineage cells trying to increase the Figure 3).…”

Potencial antineoplásico e inmunológico del lechero africano (Synadenium grantii hook) en pacientes con factores de riesgo a Covid 19

“…De experimentación previa, se ha sugerido que el látex del S. Grantii potencialmente puede presentar un efecto anti-ulcerogénico; así como, el extracto de cloroformo que contiene las hojas de esta planta demostró citotoxicidad y actividad anti-parasitaria (Campos et al, 2016). En un estudio reciente realizado con la corteza del tallo de S. Grantii, los ensayos in-vitro e in-vivo demostraron capacidad anti-oxidante significativa y anti-inflamatoria que se asociaron a la presencia de compuestos fenólicos y terpenos (Campos et al, 2016). El látex vegetal resulta ser, entonces, una mezcla compleja de compuestos orgánicos e inorgánicos, materiales cerosos y enzimas hidrolíticas.…”

“…Nuevos estudios y publicaciones han reportado casos exitosos in-vitro e in-vivo con aplicaciones, principalmente, del látex natural como anti-inflamatorio, anti-viral y anti-bacteriano (Mattar, 2013), controlador de esclerosis simple y múltiple y de infecciones agudas, subagudas, crónicas y degenerativas, regenerador de células y tejidos necrosados, inhibidor de efectos de dependencia por estupefacientes, desinfectante y biocida (Calvero A., 2018), e incluso, como potenciador de la actividad sexual y regulador del sistema hormonal además de su conocido efecto anti-tumoral y anti-proliferativo en todo tipo de cáncer incluyendo el cáncer cerebral (Campos et al, 2016). Como consecuencia de la situación pandémica que se atraviesa en la actualidad por efecto del SARSCoV-2 y de su expresión en el ser humano como COVID-19, su aplicación como potenciador del sistema inmune se ha colocado en primer plano pues una reciente publicación (Kutikov A, Weinmberg DS, 2020) coloca al látex del Synadenium grantii como un potente estimulante inmunológico a ataques virales y aún en pacientes de riesgo (oncológicos, diabéticos, obesos, etc.…”