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Coumarins and signal transduction

Hong-Tai Chang, Chiang-Ting Chou, You-Sheng Lin, Pochuen Shieh, Daih-Huang Kuo, Chung-Ren Jan, Wei-Zhe Liang
Esculetin (6,7-dihydroxycoumarin), a derivative of coumarin compound, is found in traditional medicinal herbs. It has been shown that esculetin triggers diverse cellular signal transduction pathways leading to regulation of physiology in different models. However, whether esculetin affects Ca(2+) homeostasis in breast cancer cells has not been explored. This study examined the underlying mechanism of cytotoxicity induced by esculetin and established the relationship between Ca(2+) signaling and cytotoxicity in human breast cancer cells...
April 2016: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
Xiaoyuan Mao, Zhibin Wang, Honghao Zhou, Zhaoqian Liu, Yong Zhou
OBJECTIVE: To investigate the neuroprotective effects of osthole (OST) on glutamate-induced toxicity in hippocampal HT22 cells and to explore the correlation between the protection and phosphatidylinositol-3-kinase/protein kinase B (PI3K/Akt) signaling pathway.
 METHODS: The cell injury model of HT22 was induced by glutamate and the cell viability was detected by MTS assay. The lactate dehydrogenase (LDH) release and the caspase-3 activity were determined by commercial kits...
September 2015: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
Weiya Liu, George A Vielhauer, Jeffrey M Holzbeierlein, Huiping Zhao, Suman Ghosh, Douglas Brown, Eugene Lee, Brian S J Blagg
The 90-kDa heat-shock protein (Hsp90) assists in the proper folding of numerous mutated or overexpressed signal transduction proteins that are involved in cancer. Inhibiting Hsp90 consequently is an attractive strategy for cancer therapy as the concomitant degradation of multiple oncoproteins may lead to effective antineoplastic agents. Here we report a novel C-terminal Hsp90 inhibitor, designated KU675, that exhibits potent antiproliferative and cytotoxic activity along with client protein degradation without induction of the heat-shock response in both androgen-dependent and -independent prostate cancer cell lines...
July 2015: Molecular Pharmacology
Tereza Nehybova, Jan Smarda, Lukas Daniel, Jan Brezovsky, Petr Benes
Wedelolactone, a plant coumestan, was shown to act as anti-cancer agent for breast and prostate carcinomas in vitro and in vivo targeting multiple cellular proteins including androgen receptors, 5-lipoxygenase and topoisomerase IIα. It is cytotoxic to breast, prostate, pituitary and myeloma cancer cell lines in vitro at μM concentrations. In this study, however, a novel biological activity of nM dose of wedelolactone was demonstrated. Wedelolactone acts as agonist of estrogen receptors (ER) α and β as demonstrated by transactivation of estrogen response element (ERE) in cells transiently expressing either ERα or ERβ and by molecular docking of this coumestan into ligand binding pocket of both ERα and ERβ...
August 2015: Journal of Steroid Biochemistry and Molecular Biology
Yingying Han, Changqin Ding, Jie Zhou, Yang Tian
It is very essential to disentangle the complicated inter-relationship between pH and Cu in the signal transduction and homeostasis. To this end, reporters that can display distinct signals to pH and Cu are highly valuable. Unfortunately, there is still no report on the development of biosensors that can simultaneously respond to pH and Cu(2+), to the best of our knowledge. In this work, we developed a single fluorescent probe, AuNC@FITC@DEAC (AuNC, gold cluster; FITC, fluorescein isothiocyanate; DEAC, 7-diethylaminocoumarin-3-carboxylic acid), for biosensing of pH, Cu(2+), and pH/Cu(2+) with different ratiometric fluorescent signals...
2015: Analytical Chemistry
Haitao Liu, Yubin Wang, Ashok Sharma, Rui Mao, Na Jiang, Boying Dun, Jin-Xiong She
Coumarins are a large family of compounds derived from a wide range of plants, fungi, and bacteria, and coumarin derivatives can have extremely variable structures and consequently diverse biological properties including antitumor activity. Compounds that bear a benzimidazole moiety are known to possess antitumor activity and a variety of other biological activities. High-throughput screening of a compound library identified a coumarin-containing and a benzimidazole-containing compound [#32, 7-(diethylamino)-3-(1-methyl-1H-benzimidazol-2-yl)-2H-chromen-2-one] that has potent anticancer activity...
July 2015: Anti-cancer Drugs
Christina E Turi, Katarina E Axwik, Anderson Smith, A Maxwell P Jones, Praveen K Saxena, Susan J Murch
Galanthamine is a naturally occurring acetylcholinesterase (AchE) inhibitor that has been well established as a drug for treatment of mild to moderate Alzheimer disease, but the role of the compound in plant metabolism is not known. The current study was designed to investigate whether galanthamine could redirect morphogenesis of Artemisia tridentata Nutt. cultures by altering concentration of endogenous neurosignaling molecules acetylcholine (Ach), auxin (IAA), melatonin (Mel), and serotonin (5HT). Exposure of axenic A...
2014: Plant Signaling & Behavior
Sungmi Park, Jeong-Kook Kim, Chang Joo Oh, Seung Hee Choi, Jae-Han Jeon, In-Kyu Lee
Scoparone, which is a major constituent of Artemisia capillaries, has been identified as an anticoagulant, hypolipidemic, vasorelaxant, anti-oxidant and anti-inflammatory drug, and it is used for the traditional treatment of neonatal jaundice. Therefore, we hypothesized that scoparone could suppress the proliferation of VSMCs by interfering with STAT3 signaling. We found that the proliferation of these cells was significantly attenuated by scoparone in a dose-dependent manner. Scoparone markedly reduced the serum-stimulated accumulation of cells in the S phase and concomitantly increased the proportion of cells in the G0/G1 phase, which was consistent with the reduced expression of cyclin D1, phosphorylated Rb and survivin in the VSMCs...
March 6, 2015: Experimental & Molecular Medicine
Jeong-Tae Yeon, Sik-Won Choi, Byung Jun Ryu, Kwang-Jin Kim, Joo Yun Lee, Byung Jin Byun, Young-Jin Son, Seong Hwan Kim
Excessive activity and/or increased number of osteoclasts lead to bone resorption-related disorders. Here, we investigated the potential of praeruptorin A to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo. Praeruptorin A inhibited the RANKL-induced migration/fusion of preosteoclasts accompanied by the nuclear translocation of NFATc1, a master regulator of osteoclast differentiation. Antimigration/fusion activity of praeruptorin A was also confirmed by evaluating the mRNA expression of fusion-mediating molecules...
April 24, 2015: Journal of Natural Products
Ke-Wu Zeng, Qian Yu, Li-Xi Liao, Fang-Jiao Song, Hai-Ning Lv, Yong Jiang, Peng-Fei Tu
MC13 is a novel coumarin compound found in Murraya, an economic crop whose leaves are widely used as condiment (curry) in cuisine. The aims of the present study were to investigate the neuroprotective effects of MC13 on microglia-mediated inflammatory injury model as well as potential molecular mechanism. Cell viability and apoptosis assay demonstrated that MC13 was not toxic to neurons and significantly protected neurons from microglia-mediated inflammatory injury upon lipopolysaccharide (LPS) stimulation...
July 2015: Journal of Cellular Biochemistry
Seiya Hirano, Hue Tu Quach, Tsubasa Watanabe, Naoki Kanoh, Yoshiharu Iwabuchi, Takeo Usui, Takao Kataoka
No abstract text is available yet for this article.
June 2015: Journal of Antibiotics
Sang-Hyun Lee, Hae-Dong Jang
Scoparone, one of the bioactive components of Artemisia capillaris Thunb, has various biological properties including immunosuppressive, hepatoprotective, anti-allergic, anti-inflammatory, and antioxidant effects. This study aims at evaluating the anti-osteoporotic effect of scoparone and its underlying mechanism in vitro. Scoparone demonstrated potent cellular antioxidant capacity. It was also found that scoparone inhibited the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast differentiation and suppressed cathepsin K and tartrate-resistant acid phosphatase (TRAP) expression via c-jun N-terminal kinase (JNK)/extracellular signal-regulated kinase (ERK)/p38-mediated c-Fos-nuclear factor of activated T cells, cytoplasmic 1 (NFATc1) signaling pathway...
February 15, 2015: Experimental Cell Research
Catherine W Wright, Zhi-Fo Guo, Fu-Sen Liang
Abscisic acid (ABA) was chemically modified with a photocaging group to promote photo-induced protein dimerization. This photocontrolled chemically induced dimerization (CID) method based on caged ABA enables dose-dependent light regulation of cellular processes, including transcription, protein translocation, signal transduction, and cytoskeletal remodeling, without the need to perform extensive protein engineering. Caged ABA can be easily modified to respond to different wavelengths of light. Consequently, this strategy should be applicable to the design of light-regulated protein dimerization systems and potentially be used orthogonally with other light-controlled CID systems...
January 19, 2015: Chembiochem: a European Journal of Chemical Biology
Seema Chauhan, Uma Devi, Venkatesh R Kumar, Vikas Kumar, Firoz Anwar, Gaurav Kaithwas
The present work investigates the anti-inflammatory, analgesic and antipyretic activity of methanolic extract of mulberry leaves of variety S-1, S-13 and S-146. The S-146 extract was further evaluated for its efficacy against adjuvant arthritis in albino rats followed by inhibitory potential for COX 1, COX 2 and 5 LOX. The HPLC analysis enumerated the presence of morin, reversterol, scopoletin and 7-hydroxy coumarin as the major constituents. The anti-inflammatory, antipyretic and analgesic activity observed in the present experiment could be accredited to the dual inhibition in the AA pathway...
February 2015: Inflammopharmacology
Samuel E Schriner, Steven Kuramada, Terry E Lopez, Stephanie Truong, Andrew Pham, Mahtab Jafari
Cinnamon is a spice commonly used worldwide to flavor desserts, fruits, cereals, breads, and meats. Numerous health benefits have been attributed to its consumption, including the recent suggestion that it may decrease blood glucose levels in people with diabetes. Insulin signaling is an integral pathway regulating the lifespan of laboratory organisms, such as worms, flies, and mice. We posited that if cinnamon truly improved the clinical signs of diabetes in people that it would also act on insulin signaling in laboratory organisms and increase lifespan...
December 2014: Experimental Gerontology
Ling Liu, Qingli Mu, Weifeng Li, Wei Xing, Hailin Zhang, Ting Fan, Huan Yao, Langchong He
Isofraxidin (IF), the major bioactive component of Sarcandra glabra, has been reported to be an effective anti-inflammatory compound. In a previous study, we showed that IF acts via the MAPK pathway to produce anti-inflammatory effects, both in vivo and in vitro. However, the effect and mechanism of action of IF on inflammatory cytokines and NF-κB activation in vivo has not been investigated. We therefore aimed to evaluate how IF regulates the production of inflammatory cytokines in vivo by intraperitoneal injection of IF (1, 5 or 15mg/kg) prior to treatment with LPS (1mg/kg, i...
March 2015: Immunobiology
Chia-Jung Hsieh, Po-Lin Kuo, Ming-Feng Hou, Jen-Yu Hung, Fang-Rong Chang, Ying-Chan Hsu, Ya-Fang Huang, Eing-Mei Tsai, Ya-Ling Hsu
The bone is the most common metastatic site of breast cancer. Bone metastasis causes pain, pathologic fractures, and severely reduces the quality of life. Breast cancer causes osteolytic bone metastasis, which is dependent on osteoclast-mediated bone resorption. While current treatments rely on palliative anti-resorptive agents, there is a need to develop a drug based on potential alternative therapies. This study is the first to determine that wedelolactone (WDL), a natural coumarin isolated from plants, can inhibit breast cancer-mediated osteoclastogenesis...
February 2015: International Journal of Oncology
Ming-Ming Liu, Xiao-Yu Chen, Yao-Qing Huang, Pan Feng, Ya-Lan Guo, Gong Yang, Ying Chen
Sixteen furoxan-based nitric oxide (NO) releasing coumarin derivatives (6a-c, 8a-g, 10a, 13a,b, 15, and 17a,b) were designed, synthesized, and evaluated against the A549, HeLa, A2780, A2780/CDDP, and HUVEC cell lines. Most derivatives displayed potent antiproliferation activities. Among them, 8b exhibited the strongest antiproliferation activity on the four sensitive cell lines mentioned above and three drug resistant tumor cell lines A2780/CDDP, MDA-MB-231/Gem, and SKOV3/CDDP with IC50 values from 14 to 53 nM and from 62 to 140 nM, respectively...
November 26, 2014: Journal of Medicinal Chemistry
Aamir Rana, Rukset Attar, Muhammad Zahid Qureshi, Maria Luisa Gasparri, Violante Di Donato, Ghulam Muhammad Ali, Ammad Ahmad Farooqi
In-depth analysis of how TRAIL signals through death receptors to induce apoptosis in cancer cells using high throughput technologies has added new layers of knowledge. However, the wealth of information has also highlighted the fact that TRAIL induced apoptosis may be impaired as evidenced by experimental findings obtained from TRAIL resistant cancer cell lines. Overwhelmingly, increasing understanding of TRAIL mediated apoptosis has helped in identifying synthetic and natural compounds which can restore TRAIL induced apoptosis via functionalization of either extrinsic or intrinsic pathways...
2014: Asian Pacific Journal of Cancer Prevention: APJCP
Hosadurga Kumar Keerthy, Chakrabhavi Dhananjaya Mohan, Kodappully Sivaraman Siveen, Julian E Fuchs, Shobith Rangappa, Mahalingam S Sundaram, Feng Li, Kesturu S Girish, Gautam Sethi, Basappa, Andreas Bender, Kanchugarakoppal Subbegowda Rangappa
TNF is a pleotropic cytokine known to be involved in the progression of several pro-inflammatory disorders. Many therapeutic agents have been designed to counteract the effect of TNF in rheumatoid arthritis as well as a number of cancers. In the present study we have synthesized and evaluated the anti-cancer activity of novel biscoumarins in vitro and in vivo. Among new compounds, BIHC was found to be the most cytotoxic agent against the HepG2 cell line while exhibiting less toxicity toward normal hepatocytes...
November 14, 2014: Journal of Biological Chemistry
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