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Nimbolide

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https://www.readbyqxmd.com/read/28899496/neem-azadirachta-indica-an-indian-traditional-panacea-with-modern-molecular-basis
#1
REVIEW
Subash Chandra Gupta, Sahdeo Prasad, Amit K Tyagi, Ajaikumar B Kunnumakkara, Bharat B Aggarwal
BACKGROUND: For centuries, agents derived from natural sources (mother nature), especially plants have been the primary source of medicine. Neem, also referred to as Azadirachta indica is one such plant that has been so named because it provides freedom from all diseases, and used for thousands of years in Indian and African continents. Different parts of the plant including flowers, leaves, seeds and bark have been used to treat both acute and chronic human diseases; and used as insecticide; antimicrobial, larvicidal, antimalarial, antibacterial, antiviral, and spermicidal...
October 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28888965/-click-reaction-based-synthesis-of-nimbolide-derivatives-and-study-of-their-insect-antifeedant-activity-against-spodoptera-litura-larvae
#2
Bandi Siva, Amujuri Devi, Arramsetti Venkanna, Borra Poornima, Genji Sukumar, Solipeta Divya Reddy, Movva Vijaya, Ramesh Ummanni, Katragadda Suresh Babu
A series of Nimbolide-triazole conjugates were synthesized through copper(I)- catalyzed azide-alkyne "click" chemistry approach and these derivatives (2-4, 2a-2l) were characterized using modern spectroscopic techniques. Antifeedant activities of these derivatives were studied on Tobacco Caterpillar, Spodoptera litura (F.) using no-choice leaf disk bioassay. Interestingly, the synthesized derivatives were more effective in reducing feedancy by insect species when compared to the parent nimbolide. Among the tested compounds, 2a, 2c, and 2d showed potent antifeedancy with ED50 values of 0...
September 6, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28655693/in-vitro-comparative-cytotoxic-effect-of-nimbolide-a-limonoid-from-azadirachta-indica-neem-tree-on-cancer-cell-lines-and-normal-cell-lines-through-mtt-assay
#3
Muhammad Kashif, Yawon Hwang, Gyeongmi Hong, Gonhyung Kim
The present study was conducted to find the cytotoxicity in vitro of nimbolide, limonoids derivative of flowers and leaves from Azadirachta indica (neem tree) on the selected cell lines of cancer (Du-145, PC-3, A-549) and normal fibroblast cell lines (NIH3T3, CCD-18Co) using MTT assay. The cells were seeded in 96 multi-well tissue plate using different concentrations of nimbolide for 24hrs and 48hrs. The percentage of viability of cell lines was calculated by optical density obtained by micro plate reader and cytotoxic effect in term of IC50 value was determined by using linear regression analysis...
May 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28554129/nimbolide-suppresses-non-small-cell-lung-cancer-cell-invasion-and-migration-via-manipulation-of-dusp4-expression-and-erk1-2-signaling
#4
Hua Lin, Shiyang Qiu, Lihua Xie, Chun Liu, Shenghua Sun
Nimbolide plays an important role in treating human diseases. In these years, the anticancer property of nimbolide has been paid more and more attention. However, the role of nimbolide in non-small cell lung cancer (NSCLC) remains unclear. In this study, we found that nimbolide treatment suppressed the invasion and migration of NSCLC cells, in a dose-dependent manner. Moreover, nimbolide treatment dose-dependently inhibited ERK1/2 activation, decreased Snail and MMP-3 expression, and increased E-cadherin expression...
August 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28515436/nimbolide-upregulates-reck-by-targeting-mir-21-and-hif-1%C3%AE-in-cell-lines-and-in-a-hamster-oral-carcinogenesis-model
#5
Jaganathan Kowshik, Rajakishore Mishra, Josephraj Sophia, Satabdi Rautray, Kumaraswamy Anbarasu, G Deepak Reddy, Madhulika Dixit, Sundarasamy Mahalingam, Siddavaram Nagini
Reversion-inducing cysteine-rich protein with Kazal motifs (RECK), a potent inhibitor of matrix metalloproteinases (MMPs) is a common negative target of oncogenic signals and a potential therapeutic target for novel drug development. Here, we show that sequential RECKlessness stimulates angiogenesis and Notch signalling in the 7,12-dimethylbenz[a]anthracene (DMBA)-induced hamster buccal pouch (HBP) carcinogenesis model, a paradigm for oral oncogenesis and chemointervention. We also report the chemotherapeutic effect of nimbolide, a limonoid from the neem tree (Azadirachta indica) based on the upregulation of RECK as well as modulation of the expression of key molecules involved in invasion and angiogenesis...
May 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28488233/p2x7-participates-in-intracerebral-hemorrhage-induced-secondary-brain-injury-in-rats-via-mapks-signaling-pathways
#6
Zunjia Wen, Binbin Mei, Haiying Li, Yang Dou, Xiaodi Tian, Meifen Shen, Gang Chen
This study aimed to study the role of P2X7 in intracerebral hemorrhage (ICH)-induced secondary brain injury (SBI) and the underlying mechanisms. An autologous blood injection was used to induce ICH model in Sprague-Dawley rats, and cultured primary rat cortical neurons were exposed to oxyhemoglobin to mimic ICH in vitro. siRNA interference and over-expression of P2X7, agonists and antagonists of P2X7, p38 MAPK and ERK were exploited. The protein levels were assessed using Western blotting and immunofluorescence staining...
August 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28383207/nimbolide-induces-apoptosis-in-human-nasopharyngeal-cancer-cells
#7
Su-Yu Chien, Ching-Hui Hsu, Chia-Chieh Lin, Yi-Ching Chuang, Yu-Sheng Lo, Yi-Ting Hsi, Ming-Ju Hsieh, Mu-Kuan Chen
Nasopharyngeal carcinoma (NPC), a tumor arising from epithelial cells that cover the surface and line the nasopharynx, is a rare malignancy worldwide but is prevalent in certain geographical areas, such as Southern Asia (Taiwan, Hong Kong, Singapore, Malaysia, and Southern China) and North Africa. Despite advances in diagnostic techniques and improvements in treatment modalities, the prognosis of NPC remains poor. Therefore, an effective chemotherapy regimen that enhances tumor sensitivity to chemotherapeutics is urgently required...
April 6, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28025797/inhibition-of-cell-survival-and-proliferation-by-nimbolide-in-human-androgen-independent-prostate-cancer-pc-3-cells-involvement-of-the-pi3k-akt-pathway
#8
Paulraj Raja Singh, Elayapillai Sugantha Priya, Solaimuthu Balakrishnan, Ramachandran Arunkumar, Govindaraj Sharmila, Manikkam Rajalakshmi, Jagadeesan Arunakaran
Prostate cancer is most common malignancy among men in the world. PI3K-Akt signaling appears to be critical to prostate cancer cell proliferation and survival. Our earlier study reveals that nimbolide (2 µM) prevents cell survival via IGF signaling pathway through PI3K/Akt and induces apoptosis in PC-3 cell line. Akt mediates the phosphorylation and activation of mTOR that plays a critical role in the regulation of protein translation and synthesis, angiogenesis, and cell cycle progression. The present study was aimed to investigate the effect of nimbolide on tPI3K, tAkt, pAkt, tmTOR, GSK3β, pGSK3β, PCNA, c-Myc, Cyclin D1, and Survivin protein levels by western blot analysis...
March 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27889231/nimbolide-inhibits-androgen-independent-prostate-cancer-cells-survival-and-proliferation-by-modulating-multiple-pro-survival-signaling-pathways
#9
P Raja Singh, E Sugantha Priya, S Balakrishnan, R Arunkumar, G Sharmila, M Rajalakshmi, J Arunakaran
BACKGROUND: Prostate cancer is the most prominent cancer in men, experiencing a relapse in disease often express high serum TNF-α levels. It has been correlated with increased cell survival and proliferation of prostate cancer cells. Previous studies reported that nimbolide, a terpenoid derived from the leaves and flowers of neem tree inhibits cancer growth through selective modulation of cell signaling pathways linked to inflammation, survival, proliferation, angiogenesis and metastasis...
December 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27553840/intracellular-biofilm-inhibitory-and-membrane-damaging-activities-of-nimbolide-isolated-from-azadirachta-indica-a-juss-meliaceae-against-meticillin-resistant-staphylococcus-aureus
#10
Prodipta Sarkar, Saurabh Acharyya, Anirban Banerjee, Amarendra Patra, Karthika Thankamani, Hemanta Koley, Prasanta K Bag
Staphylococcus aureus is a leading aetiologic agent of nosocomial- and community-acquired infectious diseases worldwide. The public health concern regarding staphylococcal infections is inflated by the increasing occurrence of multidrug-resistant strains, e.g. multidrug- and meticillin-resistant S.aureus (MDR MRSA). This study was designed to evaluate the intracellular killing, membrane-damaging and biofilm-inhibitory activities of nimbolide isolated from Azadirachta indica against MDR MRSA. In vitro antibacterial activity of nimbolide was determined by performing MIC, minimal bactericidal concentration (MBC) and time-kill kinetic studies...
October 2016: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27496966/nimbolide-sensitizes-human-colon-cancer-cells-to-trail-through-reactive-oxygen-species-and-erk-dependent-up-regulation-of-death-receptors-p53-and-bax
#11
Subash C Gupta, Simone Reuter, Kanokkarn Phromnoi, Byoungduck Park, Padmanabhan S Hema, Mangalam Nair, Bharat B Aggarwal
No abstract text is available yet for this article.
August 5, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27270592/nimbolide-inhibits-nuclear-factor-%C3%B0-b-pathway-in-intestinal-epithelial-cells-and-macrophages-and-alleviates-experimental-colitis-in-mice
#12
Ji Yeon Seo, Changhyun Lee, Sung Wook Hwang, Jaeyoung Chun, Jong Pil Im, Joo Sung Kim
Nimbolide is a limonoid extracted from neem tree (Azadirachta indica) that has antiinflammatory properties. The effect of nimbolide on the nuclear factor-kappa B (NF-κB) pathway in intestinal epithelial cells (IECs), macrophages and in murine colitis models was investigated. The IEC COLO 205, the murine macrophage cell line RAW 264.7, and peritoneal macrophages from interleukin-10-deficient (IL-10(-/-) ) mice were preconditioned with nimbolide and then stimulated with tumor necrosis factor-α (TNF-α) or lipopolysaccharide...
October 2016: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/27268643/combination-of-nimbolide-and-tnf-%C3%AE-increases-human-colon-adenocarcinoma-cell-death-through-jnk-mediated-dr5-up-regulation
#13
Chantana Chantana, Chavi Yenjai, Prasert Reubroycharoen, Pornthip Waiwut
Tumor necrosis factor (TNF-α), an inflammatory cytokine that plays an important role in the control of cell proliferation, differentiation, and apoptosis, has previously been used in anti-cancer therapy. However, the therapeutic applications of TNF-α are largely limited due to its general toxicity and anti-apoptotic influence. To overcome this problem, the present study focused on the effect of active constituents isolated from a medicinal plant on TNF-α-induced apoptosis in human colon adenocarcinoma (HT-29) cells...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/27134816/natural-agents-used-in-chemoprevention-of-aerodigestive-and-gi-cancers
#14
Jay Morris, Yuan Fang, Keya De Mukhopdhyay, Michael J Wargovich
Aerodigestive cancers are on an increasing level in both occurrence and mortality. A major cause in many of these cancers is disruption of the inflammatory pathway, leading to increased cell proliferation, and epigenetic silencing of normal regulatory genes. Here we review the research on several natural products: silibinin, silymarin, quercetin, neem & nimbolide, gingerol, epigallatecatechin-3- gallate, curcumin, genistein and resveratrol conducted on aerodigestive cancers. These types of cancers are primarily those from oral cavity, esophagus/windpipe, stomach, small and large intestine, colon/rectum and bile/pancreas tissues...
February 2016: Current Pharmacology Reports
https://www.readbyqxmd.com/read/27027349/anticancer-properties-of-nimbolide-and-pharmacokinetic-considerations-to-accelerate-its-development
#15
REVIEW
Lingzhi Wang, Do Dang Khoa Phan, Jingwen Zhang, Pei-Shi Ong, Win Lwin Thuya, Ross Soo, Andrea Li-Ann Wong, Wei Peng Yong, Soo Chin Lee, Paul Chi-Lui Ho, Gautam Sethi, Boon Cher Goh
Nimbolide is one of the main components in the leaf extract of Azadirachta indica (A. indica). Accumulating evidence from various in vitro and in vivo studies indicates that nimbolide possesses potent anticancer activity against several types of cancer and also shows potential chemopreventive activity in animal models. The main mechanisms of action of nimbolide include anti-proliferation, induction of apoptosis, inhibition of metastasis and angiogenesis, and modulation of carcinogen-metabolizing enzymes. Although multiple pharmacodynamic (PD) studies have been carried out, nimbolide is still at the infant stage in the drug development pipeline due to the lack of systematic pharmacokinetic (PK) studies and long-term toxicological studies...
July 12, 2016: Oncotarget
https://www.readbyqxmd.com/read/26902162/nimbolide-a-neem-limonoid-inhibits-phosphatidyl-inositol-3-kinase-to-activate-glycogen-synthase-kinase-3%C3%AE-in-a-hamster-model-of-oral-oncogenesis
#16
Josephraj Sophia, Kranthi Kiran Kishore T, Jaganathan Kowshik, Rajakishore Mishra, Siddavaram Nagini
Glycogen synthase kinase-3β (GSK-3β), a serine/threonine kinase is frequently inactivated by the oncogenic signalling kinases PI3K/Akt and MAPK/ERK in diverse malignancies. The present study was designed to investigate GSK-3β signalling circuits in the 7,12-dimethylbenz[a]anthracene (DMBA)-induced hamster buccal pouch (HBP) carcinogenesis model and the therapeutic potential of the neem limonoid nimbolide. Inactivation of GSK-3β by phosphorylation at serine 9 and activation of PI3K/Akt, MAPK/ERK and β-catenin was associated with increased cell proliferation and apoptosis evasion during stepwise evolution of HBP carcinomas...
February 23, 2016: Scientific Reports
https://www.readbyqxmd.com/read/26804739/nimbolide-inhibits-pancreatic-cancer-growth-and-metastasis-through-ros-mediated-apoptosis-and-inhibition-of-epithelial-to-mesenchymal-transition
#17
Ramadevi Subramani, Elizabeth Gonzalez, Arunkumar Arumugam, Sushmita Nandy, Viviana Gonzalez, Joshua Medel, Fernando Camacho, Andrew Ortega, Sandrine Bonkoungou, Mahesh Narayan, Alok kumar Dwivedi, Rajkumar Lakshmanaswamy
The mortality and morbidity rates of pancreatic cancer are high because of its extremely invasive and metastatic nature. Its lack of symptoms, late diagnosis and chemo-resistance and the ineffective treatment modalities warrant the development of new chemo-therapeutic agents for pancreatic cancer. Agents from medicinal plants have demonstrated therapeutic benefits in various human cancers. Nimbolide, an active molecule isolated from Azadirachta indica, has been reported to exhibit several medicinal properties...
January 25, 2016: Scientific Reports
https://www.readbyqxmd.com/read/26649526/nimbolide-induced-oxidative-stress-abrogates-stat3-signaling-cascade-and-inhibits-tumor-growth-in-transgenic-adenocarcinoma-of-mouse-prostate-model
#18
Jingwen Zhang, Kwang Seok Ahn, Chulwon Kim, Muthu K Shanmugam, Kodappully Sivaraman Siveen, Frank Arfuso, Ramar Perumal Samym, Amudha Deivasigamanim, Lina Hsiu Kim Lim, Lingzhi Wang, Boon Cher Goh, Alan Prem Kumar, Kam Man Hui, Gautam Sethi
AIMS: Prostate cancer (PCa) is one of the most commonly diagnosed cancers worldwide. Currently available therapies for metastatic PCa are only marginally effective, hence novel treatment modalities are urgently required. Considerable evidence(s) suggest that deregulated activation of oncogenic transcription factor, signal transducer and activator of transcription 3 (STAT3) plays a pivotal role in the development and progression of PCa. Thus, agents that can abrogate STAT3 activation could form the basis of novel therapy for PCa patients...
April 10, 2016: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/26536350/potential-compounds-for-oral-cancer-treatment-resveratrol-nimbolide-lovastatin-bortezomib-vorinostat-berberine-pterostilbene-deguelin-andrographolide-and-colchicine
#19
Saurabh Bundela, Anjana Sharma, Prakash S Bisen
Oral cancer is one of the main causes of cancer-related deaths in South-Asian countries. There are very limited treatment options available for oral cancer. Research endeavors focused on discovery and development of novel therapies for oral cancer, is necessary to control the ever rising oral cancer related mortalities. We mined the large pool of compounds from the publicly available compound databases, to identify potential therapeutic compounds for oral cancer. Over 84 million compounds were screened for the possible anti-cancer activity by custom build SVM classifier...
2015: PloS One
https://www.readbyqxmd.com/read/26426012/nimbolide-induces-ros-regulated-apoptosis-and-inhibits-cell-migration-in-osteosarcoma
#20
Ju-Fang Liu, Chun-Han Hou, Feng-Ling Lin, Ya-Ting Tsao, Sheng-Mou Hou
Osteosarcoma (OS) is a primary malignant tumor of bone and is most prevalent in children and adolescents. OS is frequently associated with pulmonary metastasis, which is the main cause of OS-related mortality. OS has a poor prognosis and is often unresponsive to conventional chemotherapy. In this study, we determined that Nimbolide, a novel anti-cancer therapy, acts by modulating multiple mechanisms in osteosarcoma cells. Nimbolide induces apoptosis by increasing endoplasmic reticulum (ER) stress, mitochondrial dysfunction, accumulation of reactive oxygen species (ROS), and finally, caspase activation...
2015: International Journal of Molecular Sciences
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