Roche’s breast cancer drug patent partly annulled by Indian government
Patents granted to pharmaceutical giant Roche Holding for the breast cancer drug Herceptin (trastuzumab) have been partially voided by the Indian government.
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This unassuming weed is currently the source for of the anticancer drug ingenol © Floral Images/Alamy
US scientists have developed the first efficient and scalable route for the total synthesis of ingenol – a plant-derived diterpenoid used to treat precancerous skin legions. The work offers cheaper and faster production of the drug than the current, inefficient plant extraction route, and could pave the way for the chemical synthesis of many other complex natural compounds.
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The two patents on the tyrosine kinase inhibitor were challenged by German generics company Fresenius Kabi Oncology. The decisions follow a string of similar rulings in which Indian authorities have revoked or refused to grant drug patents, in an effort to drive generic competition.
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6-Shogaol, an active constituent of ginger, inhibits breast cancer cell invasion by reducing matrix metalloproteinase-9 expression via blockade of nuclear factor-κB activation.
Br J Pharmacol. 2010 Dec ;161(8):1763-77. PMID: 20718733
H Ling, H Yang, S-H Tan, W-K Chui, E-H Chew
Department of Pharmacy, National University of Singapore, Singapore, Singapore.
BACKGROUND AND PURPOSE: Shogaols are reported to possess anti-inflammatory and anticancer activities. However, the antimetastatic potential of shogaols remains unexplored. This study was performed to assess the effects of shogaols against breast cancer cell invasion and to investigate the underlying mechanisms.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3010581/
Shogaol, also known as (6)-shogaol, is a pungent constituent of ginger similar in chemical structure to gingerol. Likezingerone, it is produced when ginger is dried or cooked.
Shogaols are artifacts formed during storage or through excess heat, probably created by a dehydration reaction of the gingerols. The ratio of shogaols to gingerols sometimes is taken as an indication of product quality.
The name ‘shogaol’ is derived from the Japanese name for ginger (生姜、shōga).
Shogaol is rated 160,000 SHU on Scoville scale. When compared to other pungent compounds, shogaol is moderately more pungent than piperine, but less than capsaicin.
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6-Shogaol is isolated from the dried or cooked rhizomes or roots of the plant Zingiber officinale (ginger). It is a perennial reed-like plant with annual leafy stems, about a meter (3 to 4 feet) tall. 6-Shogaol is a dehydrated 6-gingerol molecule that has lost a molecule of water during the drying or cooking process.
Ginger produces clusters of white and pink flower buds that bloom into yellow flowers. Because of its aesthetic appeal and the adaptation of the plant to warm climates, ginger is often used as landscaping around subtropical homes. Traditionally, the root is gathered when the stalk withers; it is immediately dried, scalded, or washed and scraped, to kill it and prevent sprouting.
6-Shogaol is isolated from dried or cooked ginger root using ethanol and other organic solvents followed by chromatographic purification. Aphios isolates 6-shogaol utilizing near-critical and supercritical fluids using CXF and CXP enabling technology platforms as alternatives to ethanol and conventional organic solvents techniques.
Ginger (Zingiber officinale Roscoe, Zingiberaceae) is a medicinal plant that has been widely used in Chinese, Ayurvedic and other global herbal medicinal practices since ancient times for a wide array of ailments including arthritis, rheumatism, sprains, muscular aches, pains, sore throats, cramps, constipation, indigestion, vomiting, hypertension, dementia, fever, infectious diseases and helminthiasis (Ali et al., 2008).
Ginger has been approved for use by Germany’s Commission E, the agency responsible for regulating the use of herbal products in that country (Blumenthal, 1998). Ginger has recently been studied scientifically for its effect on nausea and vomiting associated with motion sickness, surgery, pregnancy and cancer chemotherapy.
There may be several mechanisms of action in play relative to the antiemetic properties of ginger. It has been reported that the antiemetic qualities may be derived from ginger’s anti-serotonin 3 effects on the gastrointestinal and central nervous system (Chaiyakunapruk et al., 2006). In a study of guinea pig ileum, it was found that certain ingredients of ginger (6-, 8- and 10-gingerols) inhibit the anti-serotonin 3 receptor function (Huang et al., 1991 and Yamahara et al., 1989). In addition, these active ingredients have been shown to affect gastric motility and potentially have an antispasmodic effect on the gastrointestinal system (Hashimoto et al., 2002 and Suekawa et al., 1984).
Pan et al. (2008) investigated the inhibitory effects of 6-shogaol and a related compound, 6-gingerol, on the induction of nitric oxide synthase (NOS) and cyclooxygenase-2 (COX-2) in murine RAW 264.7 cells activated with LPS. Their results show that 6-shogaol downregulates inflammatory iNOS and COX-2 gene expression in macrophages by inhibiting the activation of NF-κB by interfering with the activation PI3K/Akt/I κB kinases IKK and MAPK.
Ali B, Blunden G, Tanira M and Nemmar A. (2008). Some phytochemical, pharmacological and toxicological properties of ginger (Zingiber officinale Roscoe): A review of recent research. Food and Chemical Toxicology. 46(2): 409-420.
Blumenthal M, Busse W, Goldberg A, Gruenwald J, Hall T, Klein S, Riggins C and Rister R. (1998). The Complete German Commission E monographs. Therapeutic Guide to Herbal Medicines, Austin TX, American Botanical Council.
Chaiyakunapruk N, Kitikannakorn N, Nathisuwan S, Leeprakobboon K and Leelasettagool C. (2006). The efficacy of ginger for the prevention of postoperative nausea and vomiting: a meta-analysis. Am. J. Obstet. Gynecol. 194, 95–99.
Chen C, Kuo M, Wu C and Ho C. (1986). Pungent Compounds of Ginger (Zingiber officinale Roscoe) Extracted by Liquid Carbon Dioxide. Journal of Agriculture and Food Chemistry 34(3): 477-480.
Hashimoto K, Satoh K, Murata P, Makino B, Sakakibara I, Kase Y, Ishige A, Higuchi M and Sasaki H. (2002). Component of Zingiber officinale that improves the enhancement of small intestinal transport. Planta Medica. 68:936-9.
Huang Q, Iwamoto M, Aoki S, Tanaka N, Tajima K, Yamahara J, Takaishi Y, Yoshida M, Tomimatsu T and Tamai Y. (1991). Anti-5-hydroxytryptamine 3 effect of galanolactone, diterpenoid isolated from ginger. Chem. Pharm. Bull. (Tokyo) 39, 397–399.
Pan M, Hsieh M, Hsu P, Ho S, Lai C, Wu H, Sang S and Ho C. (2008). 6-Shogaol suppressed lipopolysaccharide-induced up-expression of iNOS and COX-2 in murine macrophages. Mol Nutr Food Res. 52(12):1467-77.
Suekawa M, Ishige A, Yuasa K, Sudo K, Aburada M and Hosoya E. (1984). Pharmacological studies on ginger: I. Pharmacological action of pungent constituents, (6)-gingerol and (6)-shogaol. J Pharmacobiodyn. 7:836-48.
Yamahara J, Rong H, Iwamoto M, Kobayashi G, Matsuda H and Fujimura H. (1989). Active components of ginger exhibiting anti-serotonergic action. Phytother. Res. 3, 70–71.
Introduction
Plants had been used for medicinal purposes long before recorded history. Ancient Chinese and Egyptian papyrus writings describe medicinal uses for plants as early as 3,000 BC. Indigenous cultures (such as African and Native American) used herbs in their healing rituals, while others developed traditional medical systems (such as Ayurveda and Traditional Chinese Medicine) in which herbal therapies were used;…………………………..
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