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Total 109 results found since Jan 2013.

Molecules, Vol. 23, Pages 2755: HSP70 Acetylation Prevents Combined mTORC1/2 Inhibitor and Curcumin Treatment-Induced Apoptosis
Kyu Kwon We previously reported that PP242 (dual inhibitor of mTORC1/2) plus curcumin induced apoptotic cell death through lysosomal membrane permeabilization (LMP)-mediated autophagy. However, the relationship between ER stress and apoptotic cell death by combined PP242 and curcumin treatment remains unknown. In the present study, we found that combined PP242 and curcumin treatment induced cytosolic Ca2+ release and ER stress. Interestingly, pretreatment with the chemical chaperones (TUDCA and 4-PBA) and knockdown of CHOP and ATF4 by siRNA did not abolish combined treatment-induced apoptosis in renal carcinoma cells....
Source: Molecules - October 24, 2018 Category: Chemistry Authors: Seung Un Seo Kyoung-jin Min Seon Min Woo Ji Hae Seo Taeg Kyu Kwon Tags: Article Source Type: research

Molecules, Vol. 23, Pages 2327: Resveratrol Suppresses Matrix Metalloproteinase-2 Activation Induced by Lipopolysaccharide in Mouse Osteoblasts via Interactions with AMP-Activated Protein Kinase and Suppressor of Cytokine Signaling 1
Lihong Qiu Porphyromonas endodontalis (P. endodontalis) lipopolysaccharide (LPS) is associated with the progression of bone resorption in periodontal and periapical diseases. Matrix metalloproteinase-2 (MMP-2) expression and activity are elevated in apical periodontitis and have been suggested to participate in bone resorption. Therefore, inhibiting MMP-2 activation may be considered a therapeutic strategy for treating apical periodontitis. Resveratrol is a natural non-flavonoid polyphenol that has been reported to have antioxidant, anti-cancer, and anti-inflammatory properties. However, the capacity of resveratrol ...
Source: Molecules - September 12, 2018 Category: Chemistry Authors: Yaqiong Yu Xiaolin Li Jing Mi Liu Qu Di Yang Jiajie Guo Lihong Qiu Tags: Article Source Type: research

Molecules, Vol. 23, Pages 2264: Involvement of Up-Regulation of DR5 Expression and Down-Regulation of c-FLIP in Niclosamide-Mediated TRAIL Sensitization in Human Renal Carcinoma Caki Cells
eg Kyu Kwon Niclosamide is used to treat intestinal parasite infections, as being an anthelmintic drug. Recently, several papers suggest the niclosamide inhibits multiple signaling pathways, which are highly activated and mutated in cancer. Here, niclosamide was evaluated for identifying strategies to overcome tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) resistance. Although niclosamide (100–200 nM) alone did not bring about cell death, combinations of niclosamide and TRAIL led to apoptotic cell death in carcinoma cells, but not in normal cells. Niclosamide markedly increased DR5 protei...
Source: Molecules - September 5, 2018 Category: Chemistry Authors: Jeong Mi Yun Seon Min Woo Seung Un Seo Kyoung-Jin Min Dong Eun Kim Taeg Kyu Kwon Tags: Article Source Type: research

Molecules, Vol. 23, Pages 2028: Evaluation of Amino-Functional Polyester Dendrimers Based on Bis-MPA as Nonviral Vectors for siRNA Delivery
Malkoch Herein, we present the first evaluation of cationic dendrimers based on 2,2-bis(methylol)propionic acid (bis-MPA) as nonviral vectors for transfection of short interfering RNA (siRNA) in cell cultures. The study encompassed dendrimers of generation one to four (G1–G4), modified to bear 6–48 amino end-groups, where the G2–G4 proved to be capable of siRNA complexation and protection against RNase-mediated degradation. The dendrimers were nontoxic to astrocytes, glioma (C6), and glioblastoma (U87), while G3 and G4 exhibited concentration dependent toxicity towards primary ...
Source: Molecules - August 14, 2018 Category: Chemistry Authors: Patrik Stenstr öm Dario Manzanares Yuning Zhang Valentin Ce ña Michael Malkoch Tags: Article Source Type: research

Molecules, Vol. 23, Pages 1614: Garcinol Enhances TRAIL-Induced Apoptotic Cell Death through Up-Regulation of DR5 and Down-Regulation of c-FLIP Expression
k Taeg Kyu Kwon Garcinol is a polyisoprenylated benzophenone derived from the Garcinia indica fruit that possess potential therapeutic effects such as inhibition of inflammation and tumor expansion. Here, we investigated whether garcinol induces TRAIL sensitization in renal carcinoma cells. Single treatment with garcinol or TRAIL did not effect on apoptosis. However, combined treatment with garcinol plus TRAIL significantly induced apoptosis in renal carcinoma (Caki, ACHN and A498), lung carcinoma (A549), and hepatoma (SK-Hep1) cells. In contrast, garcinol plus TRAIL did not alter cell viability in normal cells. Garc...
Source: Molecules - July 2, 2018 Category: Chemistry Authors: Seok Kim Seung Un Seo Kyoung-Jin Min Seon Min Woo Ju-Ock Nam Peter Kubatka Shin Kim Jong-Wook Park Taeg Kyu Kwon Tags: Article Source Type: research

Molecules, Vol. 23, Pages 1586: The Mechanism for siRNA Transmembrane Assisted by PMAL
nnan Lu The capacity of silencing genes makes small interfering RNA (siRNA) appealing for curing fatal diseases. However, the naked siRNA is vulnerable to and degraded by endogenous enzymes and is too large and too negatively charged to cross cellular membranes. An effective siRNA carrier, PMAL (poly(maleic anhydride-alt-1-decene) substituted with 3-(dimethylamino) propylamine), has been demonstrated to be able to assist siRNA transmembrane by both experiments and molecular simulation. In the present work, the mechanism of siRNA transmembrane assisted by PMAL was studied using steered molecular dynamics simulations bas...
Source: Molecules - June 29, 2018 Category: Chemistry Authors: Yanfei Lu Jipeng Li Nan Su Diannan Lu Tags: Article Source Type: research

Molecules, Vol. 23, Pages 1085: Liposomes as Gene Delivery Vectors for Human Placental Cells
In this study, we evaluated the potential of liposomes as carriers for small interfering RNAs to placental cells. Three neutral formulations carrying rhodamine-labelled siRNAs were evaluated on an in vitro model, i.e., human primary villous cytotrophoblasts. siRNA internalization rate from lipoplexes were compared to the one in the presence of the lipofectamine reagent and assessed by confocal microscopy. Results showed cellular internalization of nucleic acid with all three formulations, based on two cationic lipids, either DMAPAP or CSL-3. Moreover, incubation with DMAPAP+AA provided a rate of labelled cells as high as w...
Source: Molecules - May 4, 2018 Category: Chemistry Authors: Lucie Valero Khair Alhareth Jenifer Espinoza Romero Warren Viricel Jeanne Leblond Audrey Chissey H élène Dhotel Caroline Roques Danielle Campiol Arruda Virginie Escriou Nathalie Mignet Thierry Fournier Karine Andrieux Tags: Communication Source Type: research

Molecules, Vol. 23, Pages 777: Polymer-Mediated Delivery of siRNAs to Hepatocellular Carcinoma: Variables Affecting Specificity and Effectiveness
Lucia Scarabel Marica Garziera Concetta Russo Spena Lucia De Stefano Barbara Salis Giuseppe Toffoli Flavio Rizzolio Gabriele Grassi Barbara Dapas Despite the advances in anticancer therapies, their effectiveness for many human tumors is still far from being optimal. Significant improvements in treatment efficacy can come from the enhancement of drug specificity. This goal may be achieved by combining the use of therapeutic molecules with tumor specific effects and delivery carriers with tumor targeting ability. In this regard, nucleic acid-based drug (NABD) and particularly small interfering RNAs (siR...
Source: Molecules - March 28, 2018 Category: Chemistry Authors: Rossella Farra Francesco Musiani Francesca Perrone Maja Čemažar Ur ška Kamenšek Federica Tonon Michela Abrami Ale š Ručigaj Mario Grassi Gabriele Pozzato Deborah Bonazza Fabrizio Zanconati Giancarlo Forte Maguie El Boustani Lucia Scarabel Marica Gar Tags: Review Source Type: research

Molecules, Vol. 23, Pages 478: Phycocyanin Protects Against UVB-induced Apoptosis Through the PKC α/βII-Nrf-2/HO-1 Dependent Pathway in Human Primary Skin Cells
ok Chae Phycocyanin (Pc) is one of the active pigment constituents of Spirulina microalgae. It has been used for its potent antioxidant and anti-inflammatory properties. However, the protective effects of Pc against ultraviolet-B (UVB)-induced primary skin cells damage are still undefined. In the present study, we investigated whether Pc prevented UVB-induced apoptotic cell death in human dermal fibroblasts (HDF) and human epidermal keratinocytes (HEK). Pc induced the transcription of heme oxygenase-1 (HO-1). Furthermore, Pc treatments resulted in a marked increase in nuclear factor erythroid-derived 2 (NF-E2)-like 2 (...
Source: Molecules - February 22, 2018 Category: Chemistry Authors: Ki Mo Kim Joo Young Lee A-Rang Im Sungwook Chae Tags: Article Source Type: research

Molecules, Vol. 22, Pages 1754: Emodin Inhibition of Influenza A Virus Replication and Influenza Viral Pneumonia via the Nrf2, TLR4, p38/JNK and NF-kappaB Pathways
In conclusion, emodin can inhibit IAV replication and influenza viral pneumonia, at least in part, by activating Nrf2 signaling and inhibiting IAV-induced activations of the TLR4, p38/JNK MAPK and NF-κB pathways.
Source: Molecules - October 18, 2017 Category: Chemistry Authors: Jian-Ping Dai Qian-Wen Wang Yun Su Li-Ming Gu Ying Zhao Xiao-Xua Chen Cheng Chen Wei-Zhong Li Ge-Fei Wang Kang-Sheng Li Tags: Article Source Type: research

Molecules, Vol. 22, Pages 1724: Enhancing the Therapeutic Delivery of Oligonucleotides by Chemical Modification and Nanoparticle Encapsulation
nguang Zhou Oligonucleotide (ON) drugs, including small interfering RNA (siRNA), microRNA (miRNA) and antisense oligonucleotides, are promising therapeutic agents. However, their low membrane permeability and sensitivity to nucleases present challenges to in vivo delivery. Chemical modifications of the ON offer a potential solution to improve the stability and efficacy of ON drugs. Combined with nanoparticle encapsulation, delivery at the site of action and gene silencing activity of chemically modified ON drugs can be further enhanced. In the present review, several types of ON drugs, selection of chemical modificatio...
Source: Molecules - October 13, 2017 Category: Chemistry Authors: Yating Sun Yarong Zhao Xiuting Zhao Robert J. Lee Lesheng Teng Chenguang Zhou Tags: Review Source Type: research

Molecules, Vol. 22, Pages 1285: Fisetin Induces Apoptosis Through p53-Mediated Up-Regulation of DR5 Expression in Human Renal Carcinoma Caki Cells
Kwon Fisetin is a natural compound found in fruits and vegetables such as strawberries, apples, cucumbers, and onions. Since fisetin can elicit anti-cancer effects, including anti-proliferation and anti-migration, we investigated whether fisetin induced apoptosis in human renal carcinoma (Caki) cells. Fisetin markedly induced sub-G1 population and cleavage of poly (ADP-ribose) polymerase (PARP), which is a marker of apoptosis, and increased caspase activation. We found that pan-caspase inhibitor (z-VAD-fmk) inhibited fisetin-induced apoptosis. In addition, fisetin induced death receptor 5 (DR5) expression at the trans...
Source: Molecules - August 2, 2017 Category: Chemistry Authors: Kyoung-jin Min Ju-Ock Nam Taeg Kwon Tags: Article Source Type: research

Molecules, Vol. 22, Pages 969: Docosahexaenoic Acid Induces Expression of Heme Oxygenase-1 and NAD(P)H:quinone Oxidoreductase through Activation of Nrf2 in Human Mammary Epithelial Cells
In conclusion, DHA activates Nrf2, possibly through modification of critical Keap1 cysteine 288 residue and PKCδ-mediated phosphorylation of Nrf2, leading to upregulation of HO-1 and NQO1 expression.
Source: Molecules - June 10, 2017 Category: Chemistry Authors: Hye-Yoon Bang Sin-Aye Park Soma Saeidi Hye-Kyung Na Young-Joon Surh Tags: Article Source Type: research

Molecules, Vol. 22, Pages 892: The Cytotoxicity of the Ajoene Analogue BisPMB in WHCO1 Oesophageal Cancer Cells Is Mediated by CHOP/GADD153
Garlic is a food and medicinal plant that has been used in folk medicine since ancient times for its beneficial health effects, which include protection against cancer. Crushed garlic cloves contain an array of small sulfur-rich compounds such as ajoene. Ajoene is able to interfere with biological processes and is cytotoxic to cancer cells in the low micromolar range. BisPMB is a synthetic ajoene analogue that has been shown in our laboratory to have superior cytotoxicity to ajoene. In the current study we have performed a DNA microarray analysis of bisPMB-treated WHCO1 oesophageal cancer cells to identify pathways and pro...
Source: Molecules - May 28, 2017 Category: Chemistry Authors: Vuyolwethu Siyo Georgia Sch äfer Roger Hunter Andriy Grafov Iryna Grafova Martin Nieger Arieh A. Katz M. Iqbal Parker Catherine H. Kaschula Tags: Article Source Type: research

Molecules, Vol. 22, Pages 782: Mesoporous Silica Nanoparticles as Carriers for Intracellular Delivery of Nucleic Acids and Subsequent Therapeutic Applications
Nucleic acids, including DNA, microRNA (miRNA), small interfering RNA (siRNA), and antisense oligonucleotide (ASO), are powerful gene regulators, which have been demonstrated as promising drug candidates for therapeutic treatments. Nevertheless, poor cellular membrane permeability and serum stability have greatly hindered the applications of nucleic acids in biomedicine. To address these issues, associate carriers that can encapsulate and protect nucleic acids are urgently required. Mesoporous silica nanoparticles (MSNs or MSNPs), which are nanomaterials with excellent biocompatibility, large surface area for functionaliza...
Source: Molecules - May 11, 2017 Category: Chemistry Authors: Wenzhang Cha Rengen Fan Yufeng Miao Yong Zhou Chenglin Qin Xiangxiang Shan Xinqiang Wan Jinbo Li Tags: Review Source Type: research