Preparation, characterization, and antiproliferative activities of biotin-decorated docetaxel-loaded bovine serum albumin nanoparticles

ABSTRACT The aim of the present study was to characterize biotin-decorated docetaxel-loaded bovine serum albumin nanoparticles (DTX-BIO-BSA-NPs) and evaluate their antiproliferative activity in vitro. The particle size of prepared DTX-BIO-BSA-NPs was found to be always lower than 200 nm, with sizes of 166.9, 160.3, 159.0, 176.1 and 184.8 nm and the zeta potential was -29.51, -28.54, -36.54, -36.08 and -27.56 mV after redissolution with water for 0, 1, 2, 4 and 8 hours, respectively. The polydispersity index (PDI) was stable in the range of 0.170 - 0.178. In the in vitro drug-release study, the DTX-BIO-BSA-NPs targeted a human breast cancer cell line MCF-7 effectively. The x-ray diffraction spectrum and DSC curve of DTX-BIO-BSA-NPs suggested that docetaxel was in an amorphous or disordered crystalline phase in DTX-BIO-BSA-NPs. In vitro cytotoxicity results showed that DTX-BIO-BSA-NPs inhibits proliferation of MCF-7, SGC7901, LS-174T and A549 cells in a concentration-dependent manner after exposure to DTX-BIO-BSA-NPs for 48 hours. Taken together, these results indicate that DTX-BIO-BSA-NPs may have potential as an alternative delivery system for parenteral administration of docetaxel.

Synthesis of hydroxycinnamic acid derivatives as mitochondria-targeted antioxidants and cytotoxic agents

In order to develop agents with superior chemopreventive and chemotherapeutic properties against hepatocellular carcinomas, mitochondria-targeted hydroxycinnamic acids (MitoHCAs) were synthesized by conjugation with a triphenylphosphonium cation. These synthetic compounds were evaluated for their antioxidant activities in hepatic mitochondria, including against OHand ROOinduced lipid peroxidation. HOproduction was decreased significantly by increasing glutathione peroxidase and catalase activities. In addition, cell proliferation data from three cell lines (HepG2, L02 and WI38) indicated that the MitoHCAs were selective for cancer cells. Interestingly, the MitoHCAs both with or without Catriggered mitochondrial dysfunction by inducing mitochondrial swelling, collapsing the mitochondrial membrane potential and causing cytochromerelease. In particular, an inhibitor of the mitochondrial permeability transition pore (mPTP), cyclosporin A, attenuated mitochondrial damage and cell apoptosis, indicating that mPTP may be involved in the antiproliferative activity of MitoHCAs. Further studies focused on structural optimization of these compounds are onging.

Nutritional Compositions and Antiproliferative Activities of Different Solvent Fractions from Ethanol Extract of Cyphomandra betacea (Tamarillo) Fruit

Background: This study aims to examine various solvent extracts of Cyphomandra betacea (tamarillo) also known as the tree tomato, for their bioactive constituents and antioxidant activity. The study also aims to examine its effect on cancer cell death using two types of cancer cell lines (liver and breast cancer cell). Methods: The first part of the study evaluates the nutritional composition of tamarillo. Then, phytochemical profiling using GC-MS analysis in ethanolic tamarillo extract was conducted. Different fractions of n-butanol, ethyl acetate and aqueous fractions were obtained from the ethanolic extract of tamarillo. Then, the fractions were subjected to the quantification of total phenol (TPC) and flavonoid contents (TFC), free radical scavenging activity (SA) and also antioxidant activity (AOX) assayed by beta-carotene bleaching (BCB) assay. Finally, the capability of the ethanolic extract of tamarillo and different fractions were evaluated for their anticancer properties. Results: Findings from this study revealed that the nutritional composition (ash, protein, carbohydrate and total dietary fiber), and mineral levels (calcium, magnesium, potassium and iron) of tamarillo were moderate. The crude ethanol extract of tamarillo contained the highest phenolic and total flavonoid content. FT-IR analysis revealed the presence of alkanes, carboxylic acid, phenol, alkanes, carboxylic acids, aromatics and nitro compounds. Twelve bioactive constituents in tamarillo have been identified through GC-MS analysis. Cytotoxic activity suggests the potential of ethanolic extracts of tamarillo having a chemopreventive effect on breast and liver cancer cells. Conclusion: This study reveals that tamarillo has substantial antioxidant activity as well as anticancer properties.

Antiproliferative and antimicrobial activities of endophytic fungus isolated from erycibe elliptilimba.

Background: Erycibe elliptilimba Merr.&Chun. is a Thai herb in the family Convolvulaceae that has long been used in traditional medicine to treat various diseases including infections and malignancies. Its methanolic extract has antiproliferative activities against various human cancer cell lines with potential ED50 values. Objective: The antiproliferative activities exhibited from this plant should be investigated to ensure that the effects were from the plant itself. Therefore, the endophytic fungus from this special plant was isolated and evaluated for their antiproliferative and antimicrobial activities. Methods: The isolation of fungal endophytes from the stems of Erycibe elliptilimba Merr.&Chun. was identified by macroscopic and microscopic morphology. Fungal extraction was demonstrated using thin layer chromatography of the crude broth extract. Four human breast cancer cell lines, two human lung cancer cell lines, and one human colon cancer cell line were used to evaluate the antiproliferative activity of the crude broth extract on the cell growth and determine of antibacterial activities. Results: The results revealed that only one species, Trichoderma ovalisporum, was isolated and its cultured broth extract did not provide an antiproliferative effect against any human cancer cell line nor antimicrobial activities. Conclusion: Based on this study, the antiproliferative activities against several human cancer cell lines of Erycibe elliptilimba, Merr&Chun extract, in recent reports may depend upon the active compounds in the plant itself.

Antiprolifrative activities of three Thai medicinal plants on human cancer cells.

In Thailand, the stems and leaves of Pouzolzia pentandra Benn., stems of Erycibe elliptilimba Merr.& Chun., and Gelonium multiflorum A. Juss. have long been used as traditional medicines for cancer therapy. The ethanol, water, methanol:water and ethyl acetate extracts of these three plants were tested in vitro against four different human breast cancer cell lines and two human lung cancer cell lines using MTT screening method. The methanol extract of Erycibe elliptilimba Merr. & Chun. showed the most potent antiproliferative activities against these specific human cancer cells. The results, therefore, suggested to some extent the benefit of the traditional use of Erycibe elliptilimba Merr.& Chun. in the treatment of malignancies.