A real‑time cell‑monitoring analysis (RTCA) system was previously developed based on the change in impedance when cells attach and spread in a culture dish coated with a gold microelectrode array. However, the potential applications of this system have not yet been fully demonstrated. The purpose of this study was to test the utility of the RTCA system to determine the cytotoxicity of four anticancer agents in carcinoma cells. The results were compared with those of the conventional WST‑8 assay at the endpoint to determine the potential of the RTCA system as a new real‑time assay method to evaluate cytotoxicity. iCELLigence was used as the RTCA system in this study. Suspensions of oral squamous cell carcinoma (OSCC) cell lines were seeded (2x104 cells/well) onto the E‑plate (the culture plate of the iCELLigence system). After 24 h of culture, anticancer agents were added to each well, and changes in electrical impedance (cell index, CI) were recorded for another 72 h of culture. Cell proliferation was detected in real‑time by the RTCA device in an automated, high throughput manner. Then, the IC50 profiles of the four anticancer agents were calculated based on the real‑time cell index values. The results indicated that the RTCA system was useful in evaluating cytotoxic reactions immediately after the addition of the anticancer agents as it was able to record the data in real‑time. Furthermore, the IC50 levels measured by the real‑time assay were lower than those measured by the endpoint assay. Thus, RTCA systems can be used to evaluate chemotherapeutic agents in cancer cells as well as their side effects in normal cells.

Small interfering RNA (siRNA) has received much attention and for possible therapeutic applications to treat incurable chronic and genetic diseases, including cancer. However, the development of safe and efficient carriers for siRNA delivery still remains formidable hurdles for in vivo. The purpose of this study is to prepare siRNA-PLGA hybrid micelles to deliver the siRNA into the ovarian cancer cells and to evaluate of gene silencing effects in mice model. Here we focused on glypican-3 (Gpc3) gene silencing, which involved in tumor progression and inflammatory reaction, as a siRNA target in a murine ovarian cancer cells, HM-1. As a result, linear polyethyleneimine (LPEI)-coated siRNA-PLGA hybrid micelles were shown to effectively inhibit GPC3 expression in vitro in HM-1 cells, compared with siRNA in solution, because of their superior intracellular uptake and enhanced gene silencing effects. In addition, intraperitoneal administration of the cationic LPEI-coated siRNA-PLGA hybrid micelles decreased the number of tumor nodes in the mesentery, compared with the siRNA sole solution, in a HM-1 peritoneal dissemination model. These results suggested that siRNA-PLGA hybrid micelles could be an effective siRNA delivery tool in a murine ovarian cancer model, especially in case it targets molecules, such as Gpc3.

Various peptides and their derivatives have been reported to exhibit antimicrobial activities. Although these activities have been examined against microorganisms, novel methods have recently emerged for conjugation of the biomaterials to improve their activities. Here, we prepared CKR12-PLGA, in which CKR12 (a mutated fragment of human cathelicidin peptide, LL-37) was conjugated with poly (lactic-co-glycolic) acid (PLGA), and compared the antimicrobial and antifungal activities of the conjugated peptide with those of FK13 (a small fragment of LL-37) and CKR12 alone. The prepared CKR12-PLGA was characterized by dynamic light scattering and measurement of the zeta potential, critical micellar concentration, and antimicrobial activities of the fragments and conjugate. Although CKR12 showed higher antibacterial activities than FK13 against Staphylococcus aureus and Escherichia coli, the antifungal activity of CKR12 was lower than that of FK13. CKR12-PLGA showed higher antibacterial activities against S. aureus and E. coli and higher antifungal activity against Candida albicans compared to those of FK13. Additionally, CKR12-PLGA showed no hemolytic activity in erythrocytes, and scanning and transmission electron microscopy suggested that CKR12-PLGA killed and disrupted the surface structure of microbial cells. Conjugation of antimicrobial peptide fragment analogues was a successful approach for obtaining increased microbial activity with minimized cytotoxicity.

Small interfering RNAs (siRNAs) are susceptible to nucleases and degrade quickly in vivo. Moreover, siRNAs demonstrate poor cellular uptake and cannot cross the cell membrane because of its polyanionic characteristics. To overcome these challenges, an intelligent gene delivery system that protects siRNAs from nucleases and facilitates siRNA cellular uptake is required. We previously reported the potential of siRNA-poly(d,l-lactic-co-glycolic acid; PLGA) micelles as an effective siRNA delivery tool in a murine peritoneal dissemination model by local injection. However, there was no effective formulation for siRNA delivery to target cells via intravenous injection. This study aimed to prepare siRNA–PLGA/Fabʹ–PLGA mixed micelles for siRNA delivery to target floating cells and evaluate its formulation in vitro. As the target siRNA protein in CEMx174, CyclinB1 levels were significantly reduced when siRNA–PLGA/Fabʹ–PLGA mixed micelles were added to cells compared with siRNA–PLGA micelles. siRNA–PLGA/Fabʹ–PLGA mixed micelles have high cell permeability and high target cell accumulation by endocytosis because flow cytometry detected labeling micelles in target cells. This study supports siRNA–PLGA/Fabʹ–PLGA mixed micelles as an effective siRNA delivery tool. This formulation can be administered systemically in dosage form against target cells, including cancer metastasis or blood cancer.

Fruits and vegetables have been recognized as natural sources of various bioactive compounds. Peppers, one such natural source, are consumed worldwide as spice crops. They additionally have an important role in traditional medicine, as a result of their antioxidant bioactivity via radical scavenging. However, there are no reports regarding the bioactivity of the bell pepper (Capsicum annuum L. var. grossum), a commonly used edible vegetable. The present study aimed to evaluate the anti‑inflammatory effect of water extract from bell pepper leaves on mouse spleen cells, and explore the potential mechanism underlying this effect. The extract was prepared through homogenization of bell pepper leaves in deionized water. The sterilized supernatant was added to a mouse spleen cell culture stimulated by concanavalin A. Following 72 h of culture, the levels of inflammatory cytokines in the culture supernatant were measured using a sandwich enzyme‑linked immunosorbent assay system, and levels of inflammatory proteins were assessed using western blotting. The bell pepper leaf extract significantly inhibited inflammatory cytokine production, inhibited cell proliferation without producing cytotoxicity, and suppressed the expression of inflammatory proteins. These results suggest that components of the bell pepper leaf extract possess anti‑inflammatory activity. The study of the anti‑inflammatory mechanism of bell pepper leaf extract has provided useful information on its potential for therapeutic application.

Exosomes are nano-sized extracellular vesicles that are known to carry various messages to distant cells. It was recently reported that cancer-derived exosomes are orientated to metastatic organs. However, there are no reports on drug carrier development using autologous serum-derived exosomes in vivo. The purpose of this study was to deliver therapeutic siRNAs for melanoma lung metastases using autologous serum-derived exosomes. Primary tumors were induced by subcutaneously injecting melanoma cells into the hindlimbs of female C57BL/6 mice. Primary tumors were surgically removed on day 14. On day 21 after tumor removal, lung metastases were evaluated. Exosomes were isolated from serum collected from mice on days 0, 3, 7, 10, and 14 after primary tumor inoculation. After isolating serum exosomes, siRNA-loaded exosomes were prepared. siRNA-loaded exosomes were intravenously injected into the B16/BL6 spontaneous lung metastasis model mice on days 0, 3, 7, and 10 after tumor removal. siRNA-loaded exosomes prepared with autologous serum-derived exosomes significantly decreased the number of metastatic lung colonies. Autologous serum-derived exosomes, which have high organ accumulation, could potentially be used as efficient carriers of therapeutic siRNAs for melanoma patients with lung metastases.