Curcumin. Antiinflammatorische Wirkung, neue Applikationsformen und klinische Studien

Zusammenfassung

Curcumin ist die am besten untersuchte antientzündliche Komponente aus dem Rhizom von Curcuma longa L. Es hat antioxidative, antiseptische und antientzündliche Wirkungen. Letztere beruht auf zahlreichen Effekten, wobei die Hemmung der Aktivierung des Transkriptionsfaktors NF-κB besondere Bedeutung hat. Die Bildung zahlreicher proinflammatorischer Proteine wird dadurch vermindert. Curcumin hemmt ebenfalls die Cyclooxygenase-2 (COX-2) und die Lipoxygenase (LOX) und steigert zudem die Bildung der induzierbaren NO-Synthase (iNOS). Problematisch ist die geringe perorale Bioverfügbarkeit von ­Curcumin. Eine interessante Möglichkeit, sie zu erhöhen, ist das Einbringen von ­Curcumin in Phytosomen. Die klinische Wirksamkeit einer solchen biooptimierten galenischen Formulierung mit Curcumin wurde in Pilotstudien bei der Behandlung der Arthrose und der Fibromyalgie bestätigt. Es fehlen aber weitere randomisierte, placebokontrollierte Studien.

Summary

Curcumin. Anti-inflammatory activity, new dosage forms and clinical studies

Part 1: Effects on disorders with musculoskeletal pain

Curcumin is a highly pleiotropic molecule with an excellent safety profile. It is the ­active component of the common spice curcuma (turmeric powder) and exerts a wide spectrum of biological activities by modulating several transcription factors and signalling pathways. However, naturally occurring curcumin cannot achieve its op­timum therapeutic outcomes in vivo due to its low solubility and poor gastrointestinal absorption and systemic bioavailability. The use of curcumin under improved formulation in patients with inflammatory disease (knee OA, fibromyalgia) appears to be a good complement to classical treatment. The clinical trials illustrate the perspective of curcumin in treating patients with inflammation-associated diseases. Despite these promising findings in pilot or retrospective studies, the results need to be confirmed and further double-blind trials are necessary.

Schlüsselwörter

Curcuma longa L - Curcumin - Bioverfügbarkeit - Signalwege - galenische Formulierungen - Arthritis - Fibromyalgie

Keywords

Curcuma longa L - curcumin - bioavailability - signalling pathways - galenic - arthritis - fibromyalgia

• Literatur

• 1 Dingermann T, Loew D. Phytopharmakologie. Stuttgart: Wissenschaftliche Verlagsges; 2003
• 2 Fintelmann V, Wegener T. Gelbwurzel − eine unterschätzte Heilpflanze. Dtsch Apoth Ztg 2001; 141: 3735-3743
• 3 >European Medicines Agency. Community Herbal Monograph on Curcuma longa L., Rhizoma. 9 November 2009 http://www.ema.europa.eu/docs/en_GB/document_library/Herbal_-_Community_herbal_monograph/2010/02/WC500070703.pdf
• 4 European Medicines Agency. Assessment Report on Curcuma longa L. Rhizoma. 12 November 2009 http://www.ema.europa.eu/docs/en_GB/document_library/Herbal_-_HMPC_assessment_report/2010/02/WC500070700.pdf
• 5 Prasad S, Tyagi AK, Aggarwal BB. Recent developments in delivery, bioavailability, absorption and metabolism of curcumin: the golden pigment from golden spice. Cancer Res Treat 2014; 46: 2-18
• 6 Gupta SC, Patchva S, Aggarwal BB. Therapeutic roles of curcumin. Lessons learned from clinical trials. AAPS J 2013; 15: 195-218
• 7 Coban D, Milenkovic D, Chanet A et al. Dietary curcumin inhibits atherosclerosis by affecting the expression of genes involved in leukocyte adhesion and transendothelial migration. Mol Nutr Food Res 2012; 56: 1270-1281
• 8 Shehzad A, Lee J, Lee YS. Curcumin in various cancers. Biofactors 2013; 39: 56-68
• 9 Aggarwal BB, Gupta SC, Sung B. Curcumin: an orally bioavailable blocker of TNF and other pro-inflammatory biomarkers. Br J Pharmacol 2013; 169: 1672-1692
• 10 Srinivasan K. Antioxidant potential of spices and their active constituents. Crit Rev Food Sci Nutr 2014; 54: 352-372
• 11 Tonnesen HH. Solubility, chemical and photochemical stability of curcumin in surfactant solutions. Studies of curcumin and curcuminoids, XXVIII. Pharmazie 2002; 57: 820-824
• 12 Kunwar A, Barik A, Pandey R, Priyadarsini KI. Transport of liposomal and albumin loaded curcumin to living cells: an absorption and fluorescence spectroscopic study. Biochim Biophys Acta 2006; 1760: 1513-1520
• 13 Zhongfa L, Chiu M, Wang J et al. Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice. Cancer Chemother Pharmacol 2012; 63: 679-689
• 14 Kurien BT, Singh A, Matsumoto H, Scofield RH. Improving the solubility and pharmacological efficacy of curcumin by heat treatment. Assay Drug Dev Technol 2007; 5: 567-576
• 15 Anand P, Nair HB, Sung B et al. Design of curcumin-loaded PLGA nanoparticles formulation with enhanced cellular uptake, and increased bioactivity in vitro and superior bioavailability in vivo. Biochem Pharmacol 2010; 79: 330-338
• 16 Prasad S, Tyagi AK, Aggarwal BB. Recent developments in delivery, bioavailability, absorption and metabolism of curcumin: the golden pigment from golden spice. Cancer Res Treat 2014; 46: 2-18
• 17 Gou M, Men K, Shi H et al. Curcumin-loaded biodegradable polymeric micelles for colon cancer therapy in vitro and in vivo. Nanoscale 2011; 3: 1558-1567
• 18 Mourtas S, Canovi M, Zona C et al. Curcumin-decorated nanoliposomes with very high affinity for amyloid-beta1-42 peptide. Biomaterials 2011; 32: 1635-1645
• 19 Kidd PM. Bioavailability and activity of phytosome complexes form botanical polyphenols: the silymarin, curcumin, green tea, and grape seed extracts. Altern Med Rev 2009; 14: 226-246
• 20 Yadav VR, Prasad S, Kannappan R et al. Cyclodextrin-complexed curcumin exhibits anti-inflammatory and antiproliferative activities superior to those of curcumin through higher cellular uptake. Biochem Pharmacol 2010; 80: 1021-1032
• 21 Henrotin Y, Priem F, Mobasheri A. Curcumin: a new paradigm and therapeutic opportunity for the treatment of osteoarthritis: curcumin for osteoarthritis management. Springerplus 2013; 2: 56-
• 22 Dr. Loges + Co. GmbH. Curcumin-loges® [Verbraucherinformation]. http://www.loges.de/fileadmin/user_upload/Packungsbeilagen/Beipackzettel_curcumin-loges.pdf
• 23 Shoba G, Joy D, Joseph T et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med 1998; 64: 353-356
• 24 Suresh D, Srinivasan K. Studies on the in vitro absorption of spice principles − curcumin, capsaicin and piperine in rat intestines. Food Chem Toxicol 2007; 45: 1437-1442
• 25 Berufsgenossenschaft Rohstoffe und chemische Industrie. Toxische Bewertungen: Piperidin. Ausgabe 11/00. ISSN 0937-4248
• 26 Oh S, Kyug TW, Choi HS. Curcumin inhibits osteoclastogenesis by decreasing receptor activator of nuclear factor-kappaB ligand (RANKL) in bone marrow stromal cells. Mol Cells 2008; 26: 486-489
• 27 Kim WK, Ke K, Sul OJ et al. Curcumin protects against ovariectomy-induced bone loss and decreases osteoclastogenesis. J Cell Biochem 2011; 112: 3159-3166
• 28 Henrotin Y, Gharbi M, Dierckxsens Y et al. Decrease of a specific biomarker of collagen degradation in osteoarthritis, Coll2-1, by treatment with highly bioavailable curcumin during an exploratory clinical trial. BMC Complement Altern Med 2014; 14: 159-
• 29 Appelboom T, Maes N, Albert A. A new curcuma extract (Flexofytol®) in osteoarthritis: results from a Belgian real-life experience. Open Rheumatol J 2014; 8: 77-81
• 30 Chandran B, Goel A. A randomized, pilot study to assess the efficacy and safety of curcumin in patients with active rheumatoid arthritis. Phytother Res 2012; 26: 1719-1725
• 31 Appelboom T, Melot C. Flexofytol, a purified curcumin extract, in fibromyalgia and gout. A retrospective study. Open J Rheumatol Autoimmune Dis 2013; 3: 104-107