Biological activities of curcuminoids, other biomolecules from turmeric and their derivatives – A review
TL;DR: The aim of this review is to summarize the chemistry, analog, metal complex, formulations of curcuminoids and their biological activities.
About: This article is published in Journal of Traditional and Complementary Medicine.The article was published on 2017-04-01 and is currently open access. It has received 526 citations till now.
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TL;DR: The strategies to improve ROS generation through optimizing photoinduced electron transfer and energy transfer processes of PSs are highlighted and the approaches that combine PDT with other therapeutics and the targeted delivery in cancer cells or tumor tissue are introduced.
Abstract: As an emerging clinical modality for cancer treatment, photodynamic therapy (PDT) takes advantage of the cytotoxic activity of reactive oxygen species (ROS) that are generated by light irradiating photosensitizers (PSs) in the presence of oxygen (O2 ). However, further advancements including tumor selectivity and ROS generation efficiency are still required. Substantial efforts are devoted to design and synthesize smart PSs with optimized properties for achieving a desirable therapeutic efficacy. This review summarizes the recent progress in developing intelligent PSs for efficient PDT, ranging from single molecules to delicate nanomaterials. The strategies to improve ROS generation through optimizing photoinduced electron transfer and energy transfer processes of PSs are highlighted. Moreover, the approaches that combine PDT with other therapeutics (e.g., chemotherapy, photothermal therapy, and radiotherapy) and the targeted delivery in cancer cells or tumor tissue are introduced. The main challenges for the clinical application of PSs are also discussed.
523 citations
TL;DR: Application of optimal sample preparation, chromatographic separation, and detection methodologies will significantly improve the assessment of different formulations and biological activities of curcuminoids.
Abstract: Turmeric is a curry spice that originated from India, which has attracted great interest in recent decades because it contains bioactive curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin). Curcumin (1,7-bis-(4-hydroxy-3-methoxyphenyl)-hepta-1,6-diene-3,5-dione), a lipophilic polyphenol may work as an anticancer, antibiotic, anti-inflammatory, and anti-aging agent as suggested by several in vitro, in vivo studies and clinical trials. However, poor aqueous solubility, bioavailability, and pharmacokinetic profiles limit curcumin’s therapeutic usage. To address these issues, several curcumin formulations have been developed. However, suboptimal sample preparation and analysis methodologies often hamper the accurate evaluation of bioactivities and their clinical efficacy. This review summarizes recent research on biological, pharmaceutical, and analytical aspects of the curcumin. Various formulation techniques and corresponding clinical trials and in vivo outcomes are discussed. A detailed comparison of different sample preparation (ultrasonic, pressurized liquid extraction, microwave, reflux) and analytical (FT-IR, FT-NIR, FT-Raman, UV, NMR, HPTLC, HPLC, and LC-MS/MS) methodologies used for the extraction and quantification of curcuminoids in different matrices, is presented. Application of optimal sample preparation, chromatographic separation, and detection methodologies will significantly improve the assessment of different formulations and biological activities of curcuminoids.
324 citations
Cites background from "Biological activities of curcuminoi..."
...Turmeric (Curcuma longa) is a plant related to the ginger family (Zingiberaceae), which originated from India and is currently grown in several other parts of the world, including Southeast Asia, China, and Latin America [6,7]....
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TL;DR: This review summarizes the most recent developments in exosome bioactivities and discusses the biochemical nature of exosomes and their biogenesis, and summarizes the use ofExosomes as delivery vehicles for drugs and natural compounds to the targeted site.
212 citations
TL;DR: This review systematically analyze the preclinical studies of curcumin in CVDs such as cardiac hypertrophy, heart failure, drug-induced cardiotoxicity, myocardial infarction, atherosclerosis, abdominal aortic aneurysm, stroke and diabetic cardiovascular complications.
182 citations
TL;DR: The formulations designed to enhance bioavailability, metabolism of curcumin, relationships between solubility and particle size relative to bioavailability and human pharmacokinetic studies involving formulatedCurcumin products are discussed.
Abstract: Curcumin exerts a wide range of beneficial physiological and pharmacological activities, including antioxidant, anti-amyloid, anti-inflammatory, anti-microbial, anti-neoplastic, immune-modulating, metabolism regulating, anti-depressant, neuroprotective and tissue protective effects. However, its poor solubility and poor absorption in the free form in the gastrointestinal tract and its rapid biotransformation to inactive metabolites greatly limit its utility as a health-promoting agent and dietary supplement. Recent advances in micro- and nano-formulations of curcumin with greatly enhanced absorption resulting in desirable blood levels of the active forms of curcumin now make it possible to address a wide range of potential applications, including pain management, and as tissue protective. Using these forms of highly bioavailable curcumin now enable a broad spectrum of appropriate studies to be conducted. This review discusses the formulations designed to enhance bioavailability, metabolism of curcumin, relationships between solubility and particle size relative to bioavailability, human pharmacokinetic studies involving formulated curcumin products, the widely used but inappropriate practice of hydrolyzing plasma samples for quantification of blood curcumin, current applications of curcumin and its metabolites and promising directions for health maintenance and applications.
171 citations
References
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TL;DR: From the data presented, the utility of natural products as sources of novel structures, but not necessarily the final drug entity, is still alive and well, and in the area of cancer, the percentage of small molecule, new chemical entities that are nonsynthetic has remained at 62% averaged over the whole time frame.
Abstract: This review is an updated and expanded version of a paper that was published in this journal in 1997. The time frame has been extended in both directions to include the 22 years from 1981 to 2002, and a new secondary subdivision related to the natural product source but applied to formally synthetic compounds has been introduced, using the concept of a “natural product mimic” or “NM” to join the original primary divisions. From the data presented, the utility of natural products as sources of novel structures, but not necessarily the final drug entity, is still alive and well. Thus, in the area of cancer, the percentage of small molecule, new chemical entities that are nonsynthetic has remained at 62% averaged over the whole time frame. In other areas, the influence of natural product structures is quite marked, particularly in the antihypertensive area, where of the 74 formally synthetic drugs, 48 can be traced to natural product structures/mimics. Similarly, with the 10 antimigraine drugs, seven are bas...
2,985 citations
"Biological activities of curcuminoi..." refers background in this paper
...[VO(Fc-tpy)(CUR)](ClO4) (1), [VO(Fc-tpy)(BDHC)](ClO4) (2), [VO(Fctpy)(BDMC)](ClO4) (3) and [VO(Ph-tpy)(CUR)](ClO4) (4), of 40-ferrocenyl-2,20:60,200-terpyridine(Fc-tpy) and 40-phenyl2,20:60,200-terpyridiine (Ph-tpy) and monoanionic curcumin (CUR), bisdehydrocycurcumin (bDHC) and bis-demethoxy curcumin (BDMC) were designed, prepared and characterized and their photo-induced DNA cleavage activity and phototoxicity studied by visible light....
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Journal Article•
TL;DR: Investigation of the efficiency of encapsulation of curcumin in poly (lactic-coglycolic acid) (PLGA) nanospheres using solid/oil/water emulsion solvent evaporation method indicates that nanoparticle-based formulation ofCurcumin has high potential as an adjuvant therapy for clinical application in prostate cancer.
Abstract: Background: Among the potent anticancer agents, curcumin has been found to be very efficacious against many different types of cancer cells. However, the major disadvantage associated with the use of curcumin is its low systemic bioavailability when administered orally due to its poor aqueous solubility. Our present work investigated the efficiency of encapsulation of curcumin in poly (lactic-co- glycolic acid) (PLGA) nanospheres using solid/oil/water emulsion solvent evaporation method. Materials and Methods: The nanospheres were formulated and then characterized for percent yield, encapsulation efficiency, surface morphology, particle size, drug distribution studies, drug polymer interaction studies and in vitro drug release profiles. Results: Our studies showed the successful formation of smooth and spherical curcumin-loaded PLGA nanospheres, with an encapsulation efficiency of 90.88±0.14% . The particle size distribution showed a range of 35 nm to 100 nm, with the mean particle size being 45 nm. Evaluation of these curcumin-loaded nanospheres was carried out in prostate cancer cell lines. Results showed robust intracellular uptake of the nanospheres in the cells. Cell viability studies revealed that the curcumin-loaded nanospheres were able to exert a more pronounced effect on the cancer cells as compared to free curcumin. Conclusion: Our studies achieved successful formulation of curcumin loaded PLGA nanospheres, thus indicating that nanoparticle-based formulation of curcumin has high potential as an adjuvant therapy for clinical application in prostate cancer. Curcumin has been used in traditional medicine for many centuries in countries such as India and China (1). It is chemically a yellow polyphenol, diferuloylmethane extracted from the rhizomes of turmeric (Curcuma longa). It posseses low intrinsic toxicity alongwith a wide range of pharmacological activities that include antitumor, anti- amyloid, antioxidant and anti-inflammatory properties. Previous investigations on curcumin have established that free curcumin induces cell cycle arrest and/or apoptosis and blocks nuclear factor kappa B (NF-κB) activation in various human cancer cell lines (2-11). Curcumin has been associated with regression of pre-malignant lesions of the bladder, soft palate, gastrointestinal tract, cervix and the skin, with treatment responses in established malignancy (12-16). The only factor that limits the use of free curcumin for cancer therapy is its poor solubility in water, which in turn limits its systemic bioavailability when administered orally. Polymeric nanoparticle-based drug delivery is being increasingly investigated as this delivery route is known to overcome many obstacles associated with the delivery of free drugs. PLGA was chosen for its biodegradable and biocompatible properties and its approval by the U.S. Food and Drug Administration. In our present work, we formulated a delivery system where curcumin was encapsulated in PLGA nanospheres by solid-in-oil-in-water (s/o/w) solvent evaporation technique. The curcumin loaded nanospheres were then characterized for their percent yield and encapsulation efficiency, particle size, surface morphology. Curcumin distribution within the nanospheres and the existence of any drug-polymer interaction were investigated. Furthermore, the curcumin- PLGA nanospheres were evaluated for their in vitro release profiles, cellular uptake and effect on cell viability in prostate cancer cell lines (LNCaP, PC3 and DU145).
414 citations
TL;DR: In this paper, an attempt has been made to test individual curcuminoids such as Curcumin, bisdemethoxycurcumin and demethoxyCurcumin for their antioxidant activities by in vitro model systems, such as the phosphomolybdenum and linoleic acid peroxidation methods.
390 citations
TL;DR: Compare analysis suggests the compound to be a possible RNA/DNA antimetabolite, but also implies that the compound's cytotoxicity may arise from a presently unknown mechanism.
356 citations
"Biological activities of curcuminoi..." refers methods in this paper
...A series of novel CUR analogs were synthesized by Adams et al (2004)142 for anticancer and anti-angiogenesis activities....
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TL;DR: Short-term supplementation with curcuminoid-piperine combination significantly improves oxidative and inflammatory status in patients with MetS and could be regarded as natural, safe and effective CRP-lowering agents.
306 citations
"Biological activities of curcuminoi..." refers methods in this paper
...Panahi et al15 (continued on next page) Table 3 (continued ) Disease/Activity Formulations Model used and study design Effect of curcuminoids treatment References Anti-diabetic activity Mono-carbonyl analogs of CUR Human 11b-HSD1 and adult rat testicular 11b-HSD1 These analogs were highly selective…...
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