QSAR prediction, synthesis, anticancer evaluation, and mechanistic investigations of novel sophoridine derivatives as topoisomerase I inhibitors.

Sophoridine, which is derived from the Leguminous plant Sophora alopecuroides L., has certain pharmacological activity as a new anticancer drug. Herein, a series of novel N-substituted sophoridine derivatives was designed, synthesized and evaluated with anticancer activity. Through QSAR prediction models, it was discovered that the introduction of a benzene ring as a main pharmacophore and reintroduced into a benzene in para position on the phenyl ring in the novel sophoridine derivatives improved the anticancer activity effectively. In vitro, 28 novel compounds were evaluated for anticancer activity against four human tumor cell lines (A549, CNE-2, HepG-2, and HEC-1-B). In particular, Compound 26 exhibited remarkable inhibitory effects, with an IC50 value of 15.6 µM against HepG-2 cells, surpassing cis-Dichlorodiamineplatinum (II). Molecular docking studies verified that the derivatives exhibit stronger binding affinity with DNA topoisomerase I compared to sophoridine. In addition, 26 demonstrated significant inhibition of DNA Topoisomerase I and could arrest cells in G0/G1 phase. This study provides valuable insights into the design and synthesis of N-substituted sophoridine derivatives with anticancer activity.

Effect of prohydrojasmon on total phenolic content, anthocyanin accumulation and antioxidant activity in komatsuna and lettuce.

Prohydrojasmon has been reported to improve the quality of crops. However, most previous studies have investigated its application on fruits. Here, we evaluated the effect of prohydrojasmon on the growth and total phenolic content, anthocyanin content, and antioxidant activity in komatsuna (Brassica rapa var. periviridis) and lettuce (Lactuca sativa L.). Prohydrojasmon did not show any serious inhibitory effect. Prohydrojasmon applied to komatsuna at a concentration of 0.5 µM significantly increased the total phenolic content and anthocyanin content, and a concentration of 1 µM increased the antioxidant activity. In lettuce, prohydrojasmon at a concentration of 400 µM significantly increased the total phenolic content and anthocyanin content, while a concentration of 0.5 µM significantly increased the antioxidant activity. These results suggest that prohydrojasmon positively affects the phenolic compound and anthocyanin accumulation and antioxidant activity in komatsuna and lettuce without adversely affecting growth.

Correlation between Antioxidant/Antimutagenic and Antiproliferative Activity of Some Phytochemicals.

BACKGROUND: Chemotherapeutic drugs have high toxicity associated with undesirable side-effects. Now, natural products are the most important anti-cancer agents because of their low toxicity and potential effectiveness. METHODS: The half maximal inhibitory concentration (IC50) of amygdalin, naringenin and ellagic acid against breast, colon, and liver cell lines was estimated. The antimutagenic, free radical-, superoxide radical-, and hydroxyl radical- scavenging activities of these phytochemicals were measured. The expression of p53, bid, bax, bcl2, and caspases 9, 3, and 7 was measured by quantitative real-time polymerase chain reaction (qRT-PCR) in breast and liver cells. In addition, the active Caspase 3 protein was estimated in liver cells. RESULTS: Ellagic acid showed the highest antioxidant and antiproliferative activities. Amygdalin and naringenin with low and moderate antioxidant profiles showed a corresponding low and moderate cytotoxicity against cancer cell lines, respectively. Naringenin and ellagic acid had a significant antimutagenic activity which was detected by the Salmonella test. Ellagic acid offered a much better antimutagenic activity than naringenin. The apoptotic pathway evoked by ellagic acid in HepG2 and MCF-7 cells was investigated. The results showed that a caspase-dependent and a caspase-independent apoptosis occurred in MCF-7 and HepG2, respectively. CONCLUSION: The antimutagenic/antioxidant properties are well correlated with the antiproliferative activity of the phytochemicals investigated. This study proved that some easy, quick and cheap assays could predict the antiproliferative activity of many nutraceuticals. Finally, this platform could help in the discovery of new anticancer agents where hundreds of compounds are investigated in the pipeline of drug discovery.

Beneficial effects and potential risks of tomato consumption for human health: An overview.

Tomato and its derived products have a very interesting nutritional value in addition to prominent antioxidant, anti-inflammatory, and anticancer activities. Tomatoes are generally quite safe to eat. However, overall consumption varies from individual to individual. Indeed, either beneficial or harmful effects of plants or their derived products are closely related to quality, including the presence of biologically active compounds. On the other hand, the synthesis and accumulation of these bioactive molecules depends on many other factors, such as environmental conditions. In this sense, this review briefly highlights the relationship between the chemistry of tomato and its derived products and their beneficial or harmful effects on human health, such as gastroesophageal reflux disease or heartburn, allergies, kidney and cardiovascular disorders, prostate cancer, irritable bowel syndrome, lycopenodermia, body aches, arthritis, and urinary problems.

Synthesis and biological evaluation of quercetin and resveratrol peptidyl derivatives as potential anticancer and antioxidant agents.

Quercetin and resveratrol are polyphenolic compounds, members of the flavonoid and the stilbene family, respectively, both medicinally important as dietary anticancer and antioxidant agents. They are present in a variety of foods-including fruits, vegetables, tea, wine, as well as other dietary supplements-and are responsible for various health benefits. Different quercetin and resveratrol esters of Leu/Met-enkephalin and tetrapeptide Leu-Ser-Lys-Leu (LSKL) were synthesized as model systems for monitoring the influence of the peptides on biological activity of resveratrol and quercetin. General formula of the main peptidyl-quercetin derivatives is 2-[3-(aa)n-4-hydroxyphenyl]-3,5,7-tri-hydroxy-4H-1-benzopyran-4-on, and the general formula of the main peptidyl-resveratrol derivatives is (E)-5-[4-(aa)n)styryl]benzene-1,3-diol. The antioxidant and anticancer activities of prepared compounds were investigated. Significant anticancer activity was obtained for the LSKL-based both quercetin and resveratrol derivatives. All prepared compounds exhibit antioxidant activity, in particular quercetin derivative containing Met-enkephalin.

Actividad cicatrizante del cremigel elaborado a base del extracto atomizado de las hojas de Solanum nitidum R.&P. "ñuñunga", Ayacucho - 2014 / Cremigel healing activity based on the atomized extract of the leaves of Solanum nitidum R. & P. "ñuñunga", Ayacucho - 2014

La búsqueda e investigación de plantas medicinales con contenidos químicos y propiedades farmacológicas que contribuyen a la cicatrización, se extraen los metabolitos responsables de dicha acción y pueden ser presentadas en formulaciones magistrales como cremas, geles, jarabes etc. La investigación es básica experimental, Solanum nitidum R. & P. "ñuñunga", fue recolectada en la comunidad de Huaraca, distrito de Vinchos, provincia de Huamanga. El objetivo de la presente investigación fue demostrar la actividad cicatrizante del cremigel elaborado a base del extracto atomizado de Solanum nitidum R. & P. "ñuñunga", su ejecución se realizó en los laboratorios de la Escuela de Formación Profesional de Farmacia y Bioquímica. Para la determinación del efecto cicatrizante se utilizó el método de Montón J. Al extracto atomizado de las hojas Solanum nitidum R. & P. "ñuñunga", se realizo la marcha fitoquimico identificando la presencia de taninos, flavonoides, saponinas, catequinas, alcaloides y quinonas; mientras que sus parámetros fisicoquímicos evaluados fueron: polvo fino color verde, sabor amargo, 7,45% de humedad, 2,24% de cenizas totales, muy solubles en agua, con un rendimiento de 9,6%. El cremigel formulado fue elaborado cumpliendo con las técnicas y procedimientos en formulación magistral dermatológica. Según Fernandez, E. De los controles se obtuvo un cremigel de color crema a marrón claro de aspecto homogéneo, poder de evanescencia y extensibilidad alta, pH entre 6,30 a 7,43, no encontrando contaminación microbiológica. El experimento se realizó con ratas wistar, a los que después de provocarles la herida de un área de 1 cm2 en el lomo del animal se aplico diariamente el cremigel formulado para ayudar a la cicatrización, luego las heridas serán fotografiadas cada dos días bajo una escala medible, estas imágenes fueron pasadas al programa de AutoCAD para su cuantificación. Las ratas fueron divididas en cinco grupos de trabajo: tres ilevaluií l.ui'ltentraciones al1%, 2% y 4% ud I,(Cilli~cl, otro grupo fue tr&táuú CÜII un estándar (Dermaclín plus®) y la última con un blanco que mostro una cicatrización normal, l. Mediante el análisis de varianza se determinó la diferencia significativa que existe entre los grupos de tratamientos (p<0.05) y con la prueba de Duncan se determinó específicamente que pruebas fueron diferentes. Se concluye que el cremigel elaborado al 1%, 2% y 4% tuvo un mejor efecto cicatrizante en comparación al estándar empleado.