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 Noscapine

Noscapine hydrochloride is an orally bioavailable hydrochloride salt of the opioid agonist noscapine, a phthalideisoquinoline alkaloid derived from the opium poppy Papaver somniferum, with mild analgesic, antitussive, and potential antineoplastic activities. Noscapine binds to tubulin and alters its conformation, resulting in a disruption of the dynamics of microtubule assembly (by increasing the time that microtubules spend idle in a paused state) and, subsequently, the inhibition of mitosis and tumor cell death. Unlike other tubulin inhibitors such as the taxanes and vinca alkaloids, noscapine does not affect microtubule polymerization. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

According to wikipedia.com, Noscapine (also known as Narcotine, Nectodon, Nospen, and Anarcotine) is a benzylisoquinoline alkaloid from plants of the Papaveraceae family, without significant painkilling properties. This agent is primarily used for its antitussive (cough-suppressing) effects. It has also been shown to have anticancer activity.

Noscapine's antitussive effects appear to be primarily mediated by its sigma receptor agonist activity. Evidence for this mechanism is suggested by experimental evidence in rats. Pretreatment with rimcazole, a sigma specific antagonist, causes a dose-dependent reduction in antitussive activity of noscapine.

Noscapine is currently under investigation for use in the treatment of several cancers and hypoxic ischemia in stroke patients. In cancer treatment, noscapine appears to interfere with microtubule function, and thus the division of cancer cells in a way similar to the taxanes. Early studies in treatment of prostate cancer are very promising. In stroke patients, noscapine blocks the bradykinine b-2 receptors. A 2003 study in Iran showed a dramatic decrease in mortality in patients treated with noscapine. Studies are currently underway to assess the effectiveness of this drug in cancer and stroke treatment. Noscapine is non-addictive, widely available, has a low side-effect incidence, and is easily administered orally, thus it has great potential for use, especially in developing countries.

 Current developer:   Cougar Biotechnology, Inc

  1: Liu M, Luo XJ, Liao F, Lei XF, Dong WG. Noscapine induces mitochondria-mediated apoptosis in gastric cancer cells in vitro and in vivo. Cancer Chemother Pharmacol. 2010 May 21. [Epub ahead of print] PubMed PMID: 20490799.

2: Karna P, Zughaier S, Pannu V, Simmons R, Narayan S, Aneja R. Induction of reactive oxygen species (ROS)-mediated autophagy by a novel microtubule-modulating agent. J Biol Chem. 2010 Apr 19. [Epub ahead of print] PubMed PMID: 20404319.

3: Sung B, Ahn KS, Aggarwal BB. Noscapine, a benzylisoquinoline alkaloid, sensitizes leukemic cells to chemotherapeutic agents and cytokines by modulating the NF-kappaB signaling pathway. Cancer Res. 2010 Apr 15;70(8):3259-68. Epub 2010 Mar 30. PubMed PMID: 20354190; PubMed Central PMCID: PMC2855771.

4: Barken I, Geller J, Rogosnitzky M. Prophylactic noscapine therapy inhibits human prostate cancer progression and metastasis in a mouse model. Anticancer Res. 2010 Feb;30(2):399-401. PubMed PMID: 20332445.

5: Aneja R, Miyagi T, Karna P, Ezell T, Shukla D, Vij Gupta M, Yates C, Chinni SR, Zhau H, Chung LW, Joshi HC. A novel microtubule-modulating agent induces mitochondrially driven caspase-dependent apoptosis via mitotic checkpoint activation in human prostate cancer cells. Eur J Cancer. 2010 Mar 17. [Epub ahead of print] PubMed PMID: 20303260.

6: Karna P, Sharp SM, Yates C, Prakash S, Aneja R. EM011 activates a survivin-dependent apoptotic program in human non-small cell lung cancer cells. Mol Cancer. 2009 Oct 30;8:93. PubMed PMID: 19878573; PubMed Central PMCID: PMC2776016.

7: Bughani U, Li S, Joshi HC. Recent patents reveal microtubules as persistent promising target for novel drug development for cancers. Recent Pat Antiinfect Drug Discov. 2009 Nov;4(3):164-82. Review. PubMed PMID: 19673697.

8: Priyadarshani A. Relevance of an opioid, noscapine in reducing cystogeneses in rat experimental model of polycystic ovary syndrome. J Endocrinol Invest. 2009 Nov;32(10):837-43. Epub 2009 Jul 17. PubMed PMID: 19609106.

9: Jaiswal AS, Aneja R, Connors SK, Joshi HC, Multani AS, Pathak S, Narayan S. 9-bromonoscapine-induced mitotic arrest of cigarette smoke condensate-transformed breast epithelial cells. J Cell Biochem. 2009 Apr 15;106(6):1146-56. PubMed PMID: 19229861; PubMed Central PMCID: PMC2728348.

10: Barken I, Geller J, Rogosnitzky M. Noscapine inhibits human prostate cancer progression and metastasis in a mouse model. Anticancer Res. 2008 Nov-Dec;28(6A):3701-4. PubMed PMID: 19189652.

11: Mahmoudian M, Rahimi-Moghaddam P. The anti-cancer activity of noscapine: a review. Recent Pat Anticancer Drug Discov. 2009 Jan;4(1):92-7. Review. PubMed PMID: 19149691.

12: Newcomb EW, Lukyanov Y, Alonso-Basanta M, Esencay M, Smirnova I, Schnee T, Shao Y, Devitt ML, Zagzag D, McBride W, Formenti SC. Antiangiogenic effects of noscapine enhance radioresponse for GL261 tumors. Int J Radiat Oncol Biol Phys. 2008 Aug 1;71(5):1477-84. Erratum in: Int J Radiat Oncol Biol Phys. 2009 Jun 1;74(2):655-6. PubMed PMID: 18640497; PubMed Central PMCID: PMC2572218.

13: Newcomb EW, Lukyanov Y, Smirnova I, Schnee T, Zagzag D. Noscapine induces apoptosis in human glioma cells by an apoptosis-inducing factor-dependent pathway. Anticancer Drugs. 2008 Jul;19(6):553-63. PubMed PMID: 18525314.

14: Jackson T, Chougule MB, Ichite N, Patlolla RR, Singh M. Antitumor activity of noscapine in human non-small cell lung cancer xenograft model. Cancer Chemother Pharmacol. 2008 Dec;63(1):117-26. Epub 2008 Mar 13. PubMed PMID: 18338172.

15: Heidari N, Goliaei B, Moghaddam PR, Rahbar-Roshandel N, Mahmoudian M. Apoptotic pathway induced by noscapine in human myelogenous leukemic cells. Anticancer Drugs. 2007 Nov;18(10):1139-47. PubMed PMID: 17893514.

16: Aneja R, Ghaleb AM, Zhou J, Yang VW, Joshi HC. p53 and p21 determine the sensitivity of noscapine-induced apoptosis in colon cancer cells. Cancer Res. 2007 Apr 15;67(8):3862-70. PubMed PMID: 17440101.

17: Aneja R, Vangapandu SN, Joshi HC. Synthesis and biological evaluation of a cyclic ether fluorinated noscapine analog. Bioorg Med Chem. 2006 Dec 15;14(24):8352-8. Epub 2006 Sep 27. PubMed PMID: 17008104.

18: Aneja R, Zhou J, Zhou B, Chandra R, Joshi HC. Treatment of hormone-refractory breast cancer: apoptosis and regression of human tumors implanted in mice. Mol Cancer Ther. 2006 Sep;5(9):2366-77. PubMed PMID: 16985071.

19: Verma AK, Bansal S, Singh J, Tiwari RK, Kasi Sankar V, Tandon V, Chandra R. Synthesis and in vitro cytotoxicity of haloderivatives of noscapine. Bioorg Med Chem. 2006 Oct 1;14(19):6733-6. Epub 2006 Jun 19. PubMed PMID: 16784870.

20: Aneja R, Vangapandu SN, Lopus M, Viswesarappa VG, Dhiman N, Verma A, Chandra R, Panda D, Joshi HC. Synthesis of microtubule-interfering halogenated noscapine analogs that perturb mitosis in cancer cells followed by cell death. Biochem Pharmacol. 2006 Aug 14;72(4):415-26. Epub 2006 May 10. PubMed PMID: 16780803.

21: Altinoz MA, Bilir A, Del Maestro RF, Tuna S, Ozcan E, Gedikoglu G. Noscapine and diltiazem augment taxol and radiation-induced S-phase arrest and clonogenic death of C6 glioma in vitro. Surg Neurol. 2006 May;65(5):478-84; discussion 485. PubMed PMID: 16630910.

22: Newcomb EW, Lukyanov Y, Schnee T, Ali MA, Lan L, Zagzag D. Noscapine inhibits hypoxia-mediated HIF-1alpha expression andangiogenesis in vitro: a novel function for an old drug. Int J Oncol. 2006 May;28(5):1121-30. PubMed PMID: 16596228.

23: Aneja R, Lopus M, Zhou J, Vangapandu SN, Ghaleb A, Yao J, Nettles JH, Zhou B, Gupta M, Panda D, Chandra R, Joshi HC. Rational design of the microtubule-targeting anti-breast cancer drug EM015. Cancer Res. 2006 Apr 1;66(7):3782-91. PubMed PMID: 16585205.

24: Aneja R, Vangapandu SN, Lopus M, Chandra R, Panda D, Joshi HC. Development of a novel nitro-derivative of noscapine for the potential treatment of drug-resistant ovarian cancer and T-cell lymphoma. Mol Pharmacol. 2006 Jun;69(6):1801-9. Epub 2006 Mar 3. Erratum in: Mol Pharmacol. 2007 Aug;72(2):486. PubMed PMID: 16517755.

25: Aneja R, Zhou J, Vangapandu SN, Zhou B, Chandra R, Joshi HC. Drug-resistant T-lymphoid tumors undergo apoptosis selectively in response to an antimicrotubule agent, EM011. Blood. 2006 Mar 15;107(6):2486-92. Epub 2005 Nov 10. PubMed PMID: 16282340; PubMed Central PMCID: PMC1895738.

26: Zhou J, Giannakakou P. Targeting microtubules for cancer chemotherapy. Curr Med Chem Anticancer Agents. 2005 Jan;5(1):65-71. Review. PubMed PMID: 15720262.

27: Landen JW, Hau V, Wang M, Davis T, Ciliax B, Wainer BH, Van Meir EG, Glass JD, Joshi HC, Archer DR. Noscapine crosses the blood-brain barrier and inhibits glioblastoma growth. Clin Cancer Res. 2004 Aug 1;10(15):5187-201. PubMed PMID: 15297423.

28: Zhou J, Gupta K, Aggarwal S, Aneja R, Chandra R, Panda D, Joshi HC. Brominated derivatives of noscapine are potent microtubule-interfering agents that perturb mitosis and inhibit cell proliferation. Mol Pharmacol. 2003 Apr;63(4):799-807. PubMed PMID: 12644580.

29: Zhou J, Gupta K, Yao J, Ye K, Panda D, Giannakakou P, Joshi HC. Paclitaxel-resistant human ovarian cancer cells undergo c-Jun NH2-terminal kinase-mediated apoptosis in response to noscapine. J Biol Chem. 2002 Oct 18;277(42):39777-85. Epub 2002 Aug 14. PubMed PMID: 12183452.

30: Landen JW, Lang R, McMahon SJ, Rusan NM, Yvon AM, Adams AW, Sorcinelli MD, Campbell R, Bonaccorsi P, Ansel JC, Archer DR, Wadsworth P, Armstrong CA, Joshi HC. Noscapine alters microtubule dynamics in living cells and inhibits the progression of melanoma. Cancer Res. 2002 Jul 15;62(14):4109-14. PubMed PMID: 12124349.

31: Yao X, Teruya-Feldstein J, Raffeld M, Sorbara L, Jaffe ES. Peripheral T-cell lymphoma with aberrant expression of CD79a and CD20: a diagnostic pitfall. Mod Pathol. 2001 Feb;14(2):105-10. PubMed PMID: 11235901.

32: Ke Y, Ye K, Grossniklaus HE, Archer DR, Joshi HC, Kapp JA. Noscapine inhibits tumor growth with little toxicity to normal tissues or inhibition of immune responses. Cancer Immunol Immunother. 2000 Jul;49(4-5):217-25. PubMed PMID: 10941904.

33: Ye K, Ke Y, Keshava N, Shanks J, Kapp JA, Tekmal RR, Petros J, Joshi HC. Opium alkaloid noscapine is an antitumor agent that arrests metaphase and induces apoptosis in dividing cells. Proc Natl Acad Sci U S A. 1998 Feb 17;95(4):1601-6. PubMed PMID: 9465062; PubMed Central PMCID: PMC19111.

34: Porter R, Parry EM, Parry JM. Morphological transformation of an established Syrian hamster dermal cell with the anti-tussive agent noscapine. Mutagenesis. 1992 May;7(3):205-9. PubMed PMID: 1602976.

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