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https://www.readbyqxmd.com/read/29117113/design-synthesis-and-anticancer-evaluation-of-fangchinoline-derivatives
#1
Yazhou Liu, Bin Xia, Junjie Lan, Shengcao Hu, Lan Huang, Chao Chen, Xueyi Zeng, Huayong Lou, Changhu Lin, Weidong Pan
Twenty fangchinoline derivatives were synthesized from the natural product fangchinoline, and their anticancer activities on human breast cancer MDA-MB-231 cell line, human prostate cancer PC3 cell line, human melanoma WM9 cell line and human leukaemia HEL and K562 cell lines were evaluated. The biological result showed that those derivatives exhibited potent activities on inhibiting cancer cell growth, and the structure-activity relationships were investigated. Among them, compound 4g, which was protected by benzoyl group in 7-phenolic position and nitrified in 14-position, showed impressive inhibition on all 5 cancer cell lines, especially WM9 cell line, with an IC50 value of 1...
November 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29065840/design-synthesis-and-evaluation-of-2-pyridinyl-methylene-1-tetralone-chalcones-for-anticancer-and-antimicrobial-activity
#2
Maya Z Gibson, Minh A Nguyen, Sarah K Zingales
BACKGROUND: Chalcones, natural products produced by plants as a natural defense mechanisms against various pathogens, are molecules with structures that include two aromatic rings joined by an α, β unsaturated carbonyl system. Previous research has demonstrated that chalcones exhibit a wide variety of biological activities, including anticancer, antifungal, and antibiotic properties. OBJECTIVE: Our goal is to synthesize novel heterocyclic-containing chalcones and have their biological activities evaluated...
October 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29064398/coumestrol-epigenetically-suppresses-cancer-cell-proliferation-coumestrol-is-a-natural-haspin-kinase-inhibitor
#3
Jong-Eun Kim, Sung-Young Lee, Mi Jang, Hyo-Kyung Choi, Jong Hun Kim, Hanyong Chen, Tae-Gyu Lim, Zigang Dong, Ki Won Lee
Targeting epigenetic changes in gene expression in cancer cells may offer new strategies for the development of selective cancer therapies. In the present study, we investigated coumestrol, a natural compound exhibiting broad anti-cancer effects against skin melanoma, lung cancer and colon cancer cell growth. Haspin kinase was identified as a direct target protein of coumestrol using kinase profiling analysis. Histone H3 is a direct substrate of haspin kinase. We observed haspin kinase overexpression as well as greater phosphorylation of histone H3 at threonine 3 (Thr-3) in the cancer cells compared to normal cells...
October 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29039788/impact-of-natural-compounds-on-dna-methylation-levels-of-the-tumor-suppressor-gene-rassf1a-in-cancer
#4
REVIEW
Reinhard H Dammann, Antje M Richter, Adriana P Jiménez, Michelle Woods, Miriam Küster, Chamindri Witharana
Epigenetic inactivation of tumor suppressor genes (TSG) is a fundamental event in the pathogenesis of human cancer. This silencing is accomplished by aberrant chromatin modifications including DNA hypermethylation of the gene promoter. One of the most frequently hypermethylated TSG in human cancer is the Ras Association Domain Family 1A (RASSF1A) gene. Aberrant methylation of RASSF1A has been reported in melanoma, sarcoma and carcinoma of different tissues. RASSF1A hypermethylation has been correlated with tumor progression and poor prognosis...
October 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29039537/juglone-potentiates-trail%C3%A2-induced-apoptosis-in-human-melanoma-cells-via-activating-the-ros%C3%A2-p38%C3%A2-p53-pathway
#5
Xiao Liu, Yan Chen, Yaohua Zhang, Juan Du, Yubao Lv, Shuming Mo, Yingchao Liu, Feng Ding, Jinfeng Wu, Ji Li
Tumor necrosis factor‑related apoptosis‑inducing ligand (TRAIL)‑based cancer therapy offers promise as TRAIL can kill cancer cells without apparent toxicity towards normal cells. However, intrinsic or acquired resistance to TRAIL inseveral types of cancer cell has become a major challenge in TRAIL‑based cancer therapy. Juglone is a natural compound isolated from walnut trees. In the present study, it was demonstrated that juglone sensitized melanoma cells to TRAIL‑induced cytotoxicity by MTT and crystal violet assays...
December 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29032930/3-hydroxy-3-4-dimethoxyflavone-blocks-tubulin-polymerization-and-is-a-potent-apoptotic-inducer-in-human-sk-mel-1-melanoma-cells
#6
Francisco Estévez-Sarmiento, Mercedes Said, Ignacio Brouard, Francisco León, Celina García, José Quintana, Francisco Estévez
Flavonoids are naturally occurring polyphenolic compounds and are among the most promising anticancer agents. A series of flavonols and their 3-methyl ether derivatives were synthesized and assessed for cytotoxicity. It was found that 3'-hydroxy-3,4'-dimethoxyflavone (flavonoid 7a) displayed strong cytotoxicity against human SK-MEL-1 melanoma cells and blocked tubulin polymerization, but had no significant cytotoxic effects against quiescent or proliferating human peripheral blood mononuclear cells. Our analyses showed that flavonoid 7a induces G2-M cell cycle arrest and apoptosis in melanoma cells which is associated with cytochrome c release and activation of both extrinsic and intrinsic apoptotic pathways of cell death...
November 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29028954/1-benzyl-indole-3-carbinol-is-a-highly-potent-new-small-molecule-inhibitor-of-wnt-%C3%AE-catenin-signaling-in-melanoma-cells-that-coordinately-inhibits-cell-proliferation-and-disrupts-expression-of-microphthalmia-associated-transcription-factor-isoform-m
#7
Aishwarya Kundu, Michelle G Khouri, Sheila Aryana, Gary L Firestone
1-Benzyl-indole-3-carbinol (1-benzyl-I3C), a synthetic analogue of the crucifer derived natural phytochemical I3C, displayed significantly wider sensitivity and anti-proliferative potency in melanoma cells than the natural compound. Unlike I3C, which targets mainly oncogenic BRAF-expressing cells, 1-benzyl I3C effectively inhibited proliferation of melanoma cells with a more extensive range of mutational profiles, including those expressing wild type BRAF. In both cultured melanoma cell lines and in vivo in melanoma cell-derived tumor xenografts, 1-benzyl-I3C disrupted canonical Wnt/β-catenin signaling that resulted in the down regulation of β-catenin protein levels with a concomitant increase in levels of the β-catenin destruction complex components GSK3β and Axin...
September 23, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/29027311/natural-compound-licochalcone-b-induced-extrinsic-and-intrinsic-apoptosis-in-human-skin-melanoma-a375-and-squamous-cell-carcinoma-a431-cells
#8
Tae-Ho Kang, Goo Yoon, In-A Kang, Ha-Na Oh, Jung-Il Chae, Jung-Hyun Shim
Licochalcone B (Lico B), which is normally isolated from the roots of Glycyrrhiza inflata (Chinese Licorice), generally classified into organic compounds including retrochalcones. Potential pharmacological properties of Lico B include anti-inflammatory, anti-bacterial, anti-oxidant, and anti-cancer activities. However, its biological effects on melanoma and squamous cell carcinoma (SCC) are unknown. Based on these known facts, this study investigated the role of Lico B in apoptosis, through the extrinsic and intrinsic pathways and additional regulation of specificity protein 1 in human skin cancer cell lines...
October 13, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28956863/ionic-liquid-catalyzed-green-protocol-for-multi-component-synthesis-of-dihydropyrano-2-3-c-pyrazoles-as-potential-anticancer-scaffolds
#9
Urja D Nimbalkar, Julio A Seijas, Maria Pilar Vazquez-Tato, Manoj G Damale, Jaiprakash N Sangshetti, Anna Pratima G Nikalje
A series of 6-amino-4-substituted-3-methyl-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitriles 5a-j were synthesized via one-pot, four-component condensation reactions of aryl aldehydes 1a-j, propanedinitrile (2), hydrazine hydrate (3) and ethyl acetoacetate (4) under solvent-free conditions. We report herein the use of the Brønsted acid ionic liquid (BAIL) triethylammonium hydrogen sulphate [Et₃NH][HSO₄] as catalyst for this multi-component synthesis. Compared with the available reaction methodology, this new method has consistent advantages, including excellent yields, a short reaction time, mild reaction conditions and catalyst reusability...
September 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28936555/resveratrol-suppresses-melanoma-by-inhibiting-nf-%C3%AE%C2%BAb-mir-221-and-inducing-tfg-expression
#10
Fangfang Wu, Liying Cui
Resveratrol (Res) is a natural compound with anti-cancer effects. The goal of this study is to evaluate the suppression of Res in melanoma and investigate its relationship with miRNAs during this process. The in vitro and in vivo anti-cancer abilities of Res were evaluated using cellular assays and animal model. Two melanoma cell lines (A375 and MV3) were used for both in vitro assay and in vivo experiments. qRT-PCR and Western blot were used to detect the changes in gene expressions and protein levels. Dual-luciferase reporter assay and bioinformatic tools were used to further confirm the protein binding and activation of targeted genes...
September 21, 2017: Archives of Dermatological Research
https://www.readbyqxmd.com/read/28868958/selective-in-vitro-anti-melanoma-activity-of-ursolic-and-oleanolic-acids
#11
Camelia Oprean, Alexandra Ivan, Florina Bojin, Mirabela Cristea, Codruta Soica, Lavinia Drăghia, Angela Caunii, Virgil Paunescu, Calin Tatu
Products of natural origin have become important agents in the treatment of cancer, and the active principles of natural sources could be used in combination with chemotherapeutic agents to increase their effects and to minimize their toxicity. Oleanolic (OA) and ursolic (UA) acids are intensely studied for their promising anticancer potential. The aim of this study was focused on the in vitro toxicological effects induced by UA and OA human mesenchymal stem cells and on melanoma, one of the most frequent cancers whose incidence is increasing every year...
September 29, 2017: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/28775302/deoxyarbutin-displays-antitumour-activity-against-melanoma-in-vitro-and-in-vivo-through-a-p38-mediated-mitochondria-associated-apoptotic-pathway
#12
Limei Ma, Yao Xu, Zeliang Wei, Guang Xin, Zhihua Xing, Hai Niu, Wen Huang
Deoxyarbutin (DeoxyArbutin, dA), a natural compound widely used in skin lighting, displayed selectively cytotoxicity in vitro. In the study, we found that dA significantly inhibited viability/proliferation of B16F10 melanoma cells, induced tumour cell arrest and apoptosis. Furthermore, dA triggered its pro-apoptosis through damaging the mitochondrial function (membrane potential loss, ATP depletion and ROS overload generation etc.) and activating caspase-9, PARP, caspase-3 and the phosphorylation of p38. Treatment with p38 agonist confirmed the involvement of p38 pathway triggered by dA in B16F10 cells...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729227/computational-and-experimental-prediction-of-molecules-involved-in-the-anti-melanoma-action-of-berberine
#13
Bin Liu, Xiu-Qiong Fu, Ting Li, Tao Su, Hui Guo, Pei-Li Zhu, Anfernee Kai-Wing Tse, Shi-Ming Liu, Zhi-Ling Yu
ETHNOPHARMACOLOGIC RELEVANCE: Berberine (BBR) is a naturally occurring alkaloid compound that can be found in Chinese medicinal herbs such as Rhizoma Coptidis and Phellodendri Cortex. These BBR containing herbs are commonly used by Chinese medicine doctors to treat cancers including melanoma. In this study, we explored proteins potentially involved in the anti-melanoma effects of BBR using computational and experimental approaches. MATERIALS AND METHODS: Target proteins of BBR were predicted using the reverse pharmacophore screening, molecular docking and molecular dynamics...
July 18, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28714807/structural-analysis-spectroscopic-characterization-and-molecular-docking-studies-of-the-cyclic-heptapeptide
#14
Sefa Celik, Serda Kecel-Gunduz, Sevim Akyuz, Aysen E Ozel
The theoretically possible stable conformer of the cyclic heptapeptide, that has significant anti-metastatic activity, was examined by conformational analysis followed by DFT calculations. Experimental infrared and Raman spectroscopy, together with theoretical DFT (6-31G (d,p) basis set)-based quantum chemical calculations, have been used to understand the structural and spectral characteristics of cyclo(Gly-Arg-Gly-Asp-Ser-Pro-Ala) {cyclo(GRGDSPA)}. A complete analysis of the vibrational spectrum has been reported on the basis of potential energy distribution (PED%) data of the vibrational modes...
August 3, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28641528/drug-design-synthesis-and-in-vitro-evaluation-of-substituted-benzofurans-as-hsp90-inhibitors
#15
Sundeep Kadasi, Thadeu E M M Costa, Neha Arukala, Mallika Toshakani, Chaitanya Duggineti, Sreekanth Thota, Sayan Dutta Gupta, Shiva Raj, Carmen Penido, Maria G Henriques, Nulgumnalli Manjunathaiah Raghavendra
BACKGROUND: Heat shock protein 90 is a molecular chaperone required for the stability and function of several client proteins that promote cancer cell growth and/or survival. Discovery of Hsp90 inhibitors has emerged as an attractive target of research in cancer therapeutics. Natural products like geldanamycin and radicicol are established Hsp90 inhibitors, but face limitations with toxicity and inactivity, by in vivo studies respectively. However, they lay the logical starting point for the design of novel synthetic or semi-synthetic congeners as Hsp90 inhibitors...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28638458/anti-metastatic-effect-of-semi-purified-nuphar-lutea-leaf-extracts
#16
Janet Ozer, Daniel Fishman, Brit Eilam, Avi Golan-Goldhirsh, Jacob Gopas
Nuphar lutea L. SM., leaf and rhizome extracts (NUP), contain nupharidines as active components. Nupharidines belong to the sesquiterpene lactones class of a naturally occurring plant terpenoids. This family of compounds has gained considerable interest for treating infection, inflammation and cancer. NF-κB is a central, downstream regulator of inflammation, cell proliferation and apoptosis. In our previous work we demonstrated strong inhibition of NF-κB activity and induction of apoptosis by NUP. In addition, NUP exhibited anti-inflammatory properties and partial protection from LPS-induced septic shock by modulating ERK pathway and cytokine secretion in macrophages...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28570563/a-natural-product-like-jak2-stat3-inhibitor-induces-apoptosis-of-malignant-melanoma-cells
#17
Ke-Jia Wu, Jie-Min Huang, Hai-Jing Zhong, Zhen-Zhen Dong, Kasipandi Vellaisamy, Jin-Jian Lu, Xiu-Ping Chen, Pauline Chiu, Daniel W J Kwong, Quan-Bin Han, Dik-Lung Ma, Chung-Hang Leung
The JAK2/STAT3 signaling pathway plays a critical role in tumorigenesis, and has been suggested as a potential molecular target for anti-melanoma therapeutics. However, few JAK2 inhibitors were being tested for melanoma therapy. In this study, eight amentoflavone analogues were evaluated for their activity against human malignant melanoma cells. The most potent analogue, compound 1, inhibited the phosphorylation of JAK2 and STAT3 in human melanoma cells, but had no discernible effect on total JAK2 and STAT3 levels...
2017: PloS One
https://www.readbyqxmd.com/read/28485554/identification-of-aca-28-a-1-acetoxychavicol-acetate-analogue-compound-as-a-novel-modulator-of-erk-mapk-signaling-which-preferentially-kills-human-melanoma-cells
#18
Ryosuke Satoh, Kanako Hagihara, Kazuki Matsuura, Yoshiaki Manse, Ayako Kita, Tatsuki Kunoh, Takashi Masuko, Mariko Moriyama, Hiroyuki Moriyama, Genzoh Tanabe, Osamu Muraoka, Reiko Sugiura
The extracellular signal-regulated kinase (ERK) signaling pathway is essential for cell proliferation and is frequently deregulated in human tumors such as melanoma. Melanoma remains incurable despite the use of conventional chemotherapy; consequently, development of new therapeutic agents for melanoma is highly desirable. Here, we carried out a chemical genetic screen using a fission yeast phenotypic assay and showed that ACA-28, a synthetic derivative of 1'-acetoxychavicol acetate (ACA), which is a natural ginger compound, effectively inhibited the growth of melanoma cancer cells wherein ERK MAPK signaling is hyperactivated due to mutations in the upstream activating regulators...
May 9, 2017: Genes to Cells: Devoted to Molecular & Cellular Mechanisms
https://www.readbyqxmd.com/read/28481901/%C3%AE-lapachone-suppresses-the-lung-metastasis-of-melanoma-via-the-mapk-signaling-pathway
#19
Ji-Ye Kee, Yo-Han Han, Dae-Seung Kim, Jeong-Geon Mun, Seong-Hwan Park, Hong-Seob So, Sung-Joo Park, Raekil Park, Jae-Young Um, Seung-Heon Hong
β-Lapachone is a natural quinone compound from Lapacho trees, which has various pharmacological effects such as anti-bacterial, anti-fungal, anti-viral, and anti-inflammatory activities. However, the effect of β-lapachone on metastasis of melanoma cells is unclear. In this study, β-lapachone reduced cell viability of metastatic melanoma cancer cell lines B16F10 and B16BL6 through induction of apoptosis via the mitogen-activated protein kinase (MAPK) pathway. Additionally, flow cytometry results showed that β-lapachone increased DNA content in the G0/G1 phase of the cell cycle...
2017: PloS One
https://www.readbyqxmd.com/read/28456625/effects-of-matsutake-mushroom-scent-compounds-on-tyrosinase-and-murine-b16-f10-melanoma-cells
#20
Hiroki Satooka, Philip Cerda, Hae-Jung Kim, William F Wood, Isao Kubo
Tyrosinase-catalyzed l-tyrosine oxidation is a key step in melanogenesis, and intense melanin formation is often a problem in chemotherapies or food preservation. Here we report that methyl cinnamate one of the constituents characterized from mycelium and sporocarp of American matsutake mushroom Tricholoma magnivelare inhibits both enzymatic and cellular melanin formation. Methyl cinnamate inhibits mushroom tyrosinase-catalyzed l-tyrosine oxidation while the oxidation of l-3,4-dihydroxyphenylalanine (l-DOPA) was not inhibited...
June 10, 2017: Biochemical and Biophysical Research Communications
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