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Total 1090 results found since Jan 2013.

Molecules, Vol. 24, Pages 1829: RA-XII Suppresses the Development and Growth of Liver Cancer by Inhibition of Lipogenesis via SCAP-dependent SREBP Supression
Mao Tan Lipogenesis plays a critical role in the growth and metastasis of tumors, which is becoming an attractive target for anti-tumor drugs. RA-XII, one of the cyclopeptide glycosides isolated from Rubia yunnanensis, exerts anti-tumor effects on liver cancer. However, the underlying mechanisms are not clear. In the present study, the effects of RA-XII on lipogenesis were evaluated and the underlying mechanisms were investigated. The results indicated that RA-XII strongly inhibited tumor growth and lipogenesis (triglycerides and lipid droplets) in HepG2 cells, and the expression of key factors involved in lipog...
Source: Molecules - May 11, 2019 Category: Chemistry Authors: Guo Wang Wang Song Wang Mao Tan Tags: Article Source Type: research

Molecules, Vol. 24, Pages 2079: Novel pH Selective, Highly Lytic Peptides Based on a Chimeric Influenza Hemagglutinin Peptide/Cell Penetrating Peptide Motif
as J. Tucker Delivery of macromolecular cargos such as siRNA to the cytosol after endocytosis remains a critical challenge. Numerous approaches including viruses, lipid nanoparticles, polymeric constructs, and various peptide-based approaches have yet to yield a general solution to this delivery issue. In this manuscript, we describe our efforts to design novel endosomolytic peptides that could be used to facilitate the release of cargos from a late endosomal compartment. These amphiphilic peptides, based on a chimeric influenza hemagglutinin peptide/cell-penetrating peptide (CPP) template, utilize a pH-triggering mech...
Source: Molecules - May 30, 2019 Category: Chemistry Authors: Bethany Algayer Ann O ’Brien Aaron Momose Dennis J. Murphy William Procopio David M. Tellers Thomas J. Tucker Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3287: Site Selective Antibody-Oligonucleotide Conjugation via Microbial Transglutaminase
even F. Dowdy Nucleic Acid Therapeutics (NATs), including siRNAs and AntiSense Oligonucleotides (ASOs), have great potential to drug the undruggable genome. Targeting siRNAs and ASOs to specific cell types of interest has driven dramatic improvement in efficacy and reduction in toxicity. Indeed, conjugation of tris-GalNAc to siRNAs and ASOs has shown clinical efficacy in targeting diseases driven by liver hepatocytes. However, targeting non-hepatic diseases with oligonucleotide therapeutics has remained problematic for several reasons, including targeting specific cell types and endosomal escape. Monoclonal antibody (m...
Source: Molecules - September 9, 2019 Category: Chemistry Authors: Ian J. Huggins Carlos A. Medina Aaron D. Springer Arjen van den Berg Satish Jadhav Xianshu Cui Steven F. Dowdy Tags: Article Source Type: research

Molecules, Vol. 25, Pages 645: Discovery of Novel Inhibitors Targeting Multi-UDP-hexose Pyrophosphorylases as Anticancer Agents
In this study, we focused on, among the altered metabolic processes in cancerous cells, altered glycosylation due to its documented roles in cancer tumorigenesis, metastasis and drug resistance. We hypothesize that the enzymes required for the biosynthesis of UDP-hexoses, glycosyl donors for glycan synthesis, could serve as therapeutic targets for cancers. Through structure-based virtual screening and kinetic assay, we identified a drug-like chemical fragment, GAL-012, that inhibit a small family of UDP-hexose pyrophosphorylases-galactose pyro-phosphorylase (GALT), UDP-glucose pyrophosphorylase (UGP2) and UDP-N-acetylgluco...
Source: Molecules - February 2, 2020 Category: Chemistry Authors: Yueqin Yang Hariprasad Vankayalapati Manshu Tang Yingbo Zheng Yingri Li Cong Ma Kent Lai Tags: Article Source Type: research

Molecules, Vol. 25, Pages 694: Design, Synthesis and Characterization of a Novel Type of Thermo-Responsible Phospholipid Microcapsule –Alginate Composite Hydrogel for Drug Delivery
Molecules, Vol. 25, Pages 694: Design, Synthesis and Characterization of a Novel Type of Thermo-Responsible Phospholipid Microcapsule–Alginate Composite Hydrogel for Drug Delivery Molecules doi: 10.3390/molecules25030694 Authors: Liang Ding Xinxia Cui Rui Jiang Keya Zhou Yalei Wen Chenfeng Wang Zhilian Yue Shigang Shen Xuefeng Pan Liposomes are extensively used in drug delivery, while alginates are widely used in tissue engineering. However, liposomes are usually thermally unstable and drug-leaking when in liquids, while the drug carriers made of alginates show low loading capacities when used for...
Source: Molecules - February 5, 2020 Category: Chemistry Authors: Liang Ding Xinxia Cui Rui Jiang Keya Zhou Yalei Wen Chenfeng Wang Zhilian Yue Shigang Shen Xuefeng Pan Tags: Article Source Type: research

Molecules, Vol. 25, Pages 1320: Evodiamine Mitigates Cellular Growth and Promotes Apoptosis by Targeting the c-Met Pathway in Prostate Cancer Cells
Blough Ahn Evodiamine (EVO) is an indoloquinazoline alkaloid that exerts its various anti-oncogenic actions by blocking phosphatidylinositol-3-kinase/protein kinase B (PI3K/Akt), mitogen-activated protein kinase (MAPK), c-Met, and nuclear factor kappa B (NF-B) signaling pathways, thus leading to apoptosis of tumor cells. We investigated the ability of EVO to affect hepatocyte growth factor (HGF)-induced c-Met/Src/STAT3 activation cascades in castration-resistant prostate cancer (CRPC). First, we noted that EVO showed cytotoxicity and anti-proliferation activities in PC-3 and DU145 cells. Next, we found that EVO m...
Source: Molecules - March 12, 2020 Category: Chemistry Authors: Hwang Um Chinnathambi Alharbi Narula Namjoshi Blough Ahn Tags: Article Source Type: research

Molecules, Vol. 25, Pages 1414: Unknown Areas of Activity of Human Ribonuclease Dicer: A Putative Deoxyribonuclease Activity
rniak The Dicer ribonuclease plays a crucial role in the biogenesis of small regulatory RNAs (srRNAs) by processing long double-stranded RNAs and single-stranded hairpin RNA precursors into small interfering RNAs (siRNAs) and microRNAs (miRNAs), respectively. Dicer-generated srRNAs can control gene expression by targeting complementary transcripts and repressing their translation or inducing their cleavage. Human Dicer (hDicer) is a multidomain enzyme comprising a putative helicase domain, a DUF283 domain, platform, a PAZ domain, a connector helix, two RNase III domains (RNase IIIa and RNase IIIb) and a dsRNA-binding d...
Source: Molecules - March 19, 2020 Category: Chemistry Authors: Marta Wojnicka Agnieszka Szczepanska Anna Kurzynska-Kokorniak Tags: Article Source Type: research

Molecules, Vol. 25, Pages 3344: Synthesis of Nucleobase-Modified RNA Oligonucleotides by Post-Synthetic Approach
szczynska The chemical synthesis of modified oligoribonucleotides represents a powerful approach to study the structure, stability, and biological activity of RNAs. Selected RNA modifications have been proven to enhance the drug-like properties of RNA oligomers providing the oligonucleotide-based therapeutic agents in the antisense and siRNA technologies. The important sites of RNA modification/functionalization are the nucleobase residues. Standard phosphoramidite RNA chemistry allows the site-specific incorporation of a large number of functional groups to the nucleobase structure if the building blocks are synthetic...
Source: Molecules - July 22, 2020 Category: Chemistry Authors: Karolina Bartosik Katarzyna Debiec Anna Czarnecka Elzbieta Sochacka Grazyna Leszczynska Tags: Review Source Type: research

Molecules, Vol. 25, Pages 4136: The Potential Role of Cathepsin K in Non-Small Cell Lung Cancer
Conclusion: Cathepsin K may potentially represent a viable drug target for NSCLC treatment.
Source: Molecules - September 9, 2020 Category: Chemistry Authors: Hui Yang Jasmine Heyer Hui Zhao Shengxian Liang Rui Guo Li Zhong Tags: Article Source Type: research

Molecules, Vol. 25, Pages 4591: Magnolol Enhances the Therapeutic Effects of TRAIL through DR5 Upregulation and Downregulation of c-FLIP and Mcl-1 Proteins in Cancer Cells
Kwon Magnolol is a biologically active compound, isolated from the Chinese herb Magnolia, that regulates antiproliferative, anticancer, antiangiogenic and antimetastatic activities. We found that magnolol sensitizes TRAIL-induced apoptotic cell death via upregulation of DR5 and downregulation of cellular FLICE-inhibitory protein (c-FLIP) and Mcl-1 in cancer cells, but not in normal cells. Mechanistically, magnolol increased ATF4-dependent DR5 expression at the transcription level, and knockdown of ATF4 markedly inhibited magnolol-induced DR5 upregulation. Silencing DR5 with siRNA prevented combined treatment with magn...
Source: Molecules - October 8, 2020 Category: Chemistry Authors: Seon Min Woo Kyoung-jin Min Taeg Kyu Kwon Tags: Article Source Type: research

Molecules, Vol. 26, Pages 901: Silencing ZEB2 Induces Apoptosis and Reduces Viability in Glioblastoma Cell Lines
Conclusions: In line with previous investigations, our results indicated a critical oncogenic role for ZEB2 overexpression in brain glioma tumors. These properties make ZEB2 an essential molecule for further studies in the treatment of glioma cancer.
Source: Molecules - February 9, 2021 Category: Chemistry Authors: Sahar Safaee Masoumeh Fardi Nima Hemmat Neda Khosravi Afshin Derakhshani Nicola Silvestris Behzad Baradaran Tags: Article Source Type: research

Molecules, Vol. 26, Pages 1328: Identification of a Sesquiterpene Lactone from Arctium lappa Leaves with Antioxidant Activity in Primary Human Muscle Cells
In this study, we investigated the antioxidant properties of Arctium lappa leaves in a model of primary human muscle cells exposed to H2O2 oxidative stress. We identified using bioassay-guided purification, onopordopicrin, a sesquiterpene lactone as the main molecule responsible for the antioxidant activity of A. lappa leaf extract. According to our findings, onopordopicrin inhibited the H2O2-mediated loss of muscle cell viability, by limiting the production of free radicals and abolishing DNA cellular damages. Moreover, we showed that onopordopicrin promoted the expression of the nuclear factor-erythroid-2-related factor ...
Source: Molecules - March 2, 2021 Category: Chemistry Authors: Nour El Khatib Sylvie Morel G érald Hugon Sylvie Rapior Gilles Carnac Nathalie Saint Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2018: An Activatable T1-Weighted MR Contrast Agent: A Noninvasive Tool for Tracking the Vicinal Thiol Motif of Thioredoxin in Live Cells
iya Kwan Soo Hong We have synthesized new magnetic resonance imaging (MRI) T1 contrast agents (CA1 and CA2) that permit the activatable recognition of the cellular vicinal thiol motifs of the protein thioredoxin. The contrast agents showed MR relaxivities typical of gadolinium complexes with a single water molecule coordinated to a Gd3+ center (i.e., ~4.54 mM−1s−1) for both CA1 and CA2 at 60 MHz. The contrast agent CA1 showed a ~140% relaxivity enhancement in the presence of thioredoxin, a finding attributed to a reduction in the flexibility of the molecule after binding to thioredoxin. Support for this rationale...
Source: Molecules - April 1, 2021 Category: Chemistry Authors: Jongeun Kang Eunha Hwang Hyunseung Lee Mi Young Cho Sanu Karan Hak Nam Kim Jong Seung Kim Jonathan L. Sessler Sankarprasad Bhuniya Kwan Soo Hong Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2092: Simultaneous Quantitative Analysis of Ginsenosides Isolated from the Fruit of Panax ginseng C.A. Meyer and Regulation of HO-1 Expression through EGFR Signaling Has Anti-Inflammatory and Osteogenic Induction Effects in HPDL Cells
In conclusion, this study evaluated the contents of ginsenosides-Re, -Ra8, and -Rf isolated from P. ginseng fruit extract. Therefore, these results provide important basic data for future P. ginseng fruit component studies and suggest that ginsenosides Re, Ra8, and Rf have potential as future treatment options for periodontitis.
Source: Molecules - April 6, 2021 Category: Chemistry Authors: Eun-Nam Kim Oryon Kaygusuz Hyun-Su Lee Gil-Saeng Jeong Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2119: A Versatile Solid-Phase Approach to the Synthesis of Oligonucleotide Conjugates with Biodegradable Hydrazone Linker
aminova One of the ways to efficiently deliver various drugs, including therapeutic nucleic acids, into the cells is conjugating them with different transport ligands via labile or stable bonds. A convenient solid-phase approach for the synthesis of 5′-conjugates of oligonucleotides with biodegradable pH-sensitive hydrazone covalent bonds is proposed in this article. The approach relies on introducing a hydrazide of the ligand under aqueous/organic media to a fully protected support-bound oligonucleotide containing aldehyde function at the 5′-end. We demonstrated the proof-of-principle of this approach by synthesiz...
Source: Molecules - April 7, 2021 Category: Chemistry Authors: Mariya I. Meschaninova Nina S. Entelis Elena L. Chernolovskaya Alya G. Venyaminova Tags: Article Source Type: research