ArticleLiterature Review

Biological activities of curcuminoids, other biomolecules from turmeric and their derivatives – A review

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  • Molecules Biolabs Private Limited
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Abstract

In recent years, several drugs have been developed deriving from traditional products and current drug research is actively investigating the possible therapeutic roles of many Ayruvedic and Traditional Indian medicinal therapies. Among those being investigated is Turmeric. Its most important active ingredient is curcuminoids. Curcuminoids are phenolic compounds commonly used as a spice, pigment and additive also utilized as a therapeutic agent used in several foods. Comprehensive research over the last century has revealed several important functions of curcuminoids. Various preclinical cell culture and animals studies suggest that curcuminoids have extensive biological activity as an antioxidant, neuroprotective, antitumor, anti-inflammatory, anti-acidogenic, radioprotective and arthritis. Different clinical trials also suggest a potential therapeutic role for curcuminoids in numerous chronic diseases such as colon cancer, lung cancer, breast cancer, inflammatory bowel diseases. The aim of this review is to summarize the chemistry, analog, metal complex, formulations of curcuminoids and their biological activities.

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... Curcumin, a bioactive compound derived from plants of the Curcuma genus in the Zingiberaceae family, has been extensively utilized as a natural active ingredient in herbal cosmetics, including as a photoprotective agent [57][58][59]. Recent studies demonstrate that curcumin protects skin cells from UV radiation and prevents sunburn through its potent Cosmetics 2025, 12, 10 3 of 24 antioxidant and anti-inflammatory properties [60][61][62]. Moreover, curcumin enhances cellular antioxidant defenses by activating the Nrf2 pathway, which plays a pivotal role in mitigating oxidative stress [63,64]. ...
... Several studies have demonstrated that curcumin improves SPF values, as outlined in Table 4. Its ability to enhance the skin's defense against ultraviolet (UV) radiation is attributed to its antioxidant and UV-absorbing properties [60][61][62]. By neutralizing free radicals and reducing oxidative stress caused by UV exposure, curcumin enhances the photoprotective capacity of sunscreen formulations [48,49]. ...
... Curcumin enhances the effectiveness of sunscreen formulations by complementing other SPF-active ingredients, as evidenced by its multifunctional properties [152]. Acting as a skin protector, curcumin's antioxidant and anti-inflammatory activities provide substantial benefits [60][61][62]. Specifically, its anti-inflammatory effects include the ability to reduce redness and tissue damage caused by inflammation following sunlight exposure [133,134]. Curcumin achieves this by inhibiting the production of pro-inflammatory cytokines, such as IL-β, IL-6, and TNF-α, while reducing arachidonic acid release through the suppression of phospholipase A2 and phospholipase C g1 activity [37,156]. ...
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Exposure to ultraviolet (UV) radiation from the sun significantly damages the skin, leading to premature aging, hyperpigmentation, and oxidative stress that disrupts skin homeostasis. UV radiation increases the production of reactive oxygen species (ROS), accelerating skin deterioration. Although sunscreens remain the primary method for UV protection, chemical-based formulations are often associated with side effects, such as allergic reactions and acne. To address these concerns, the inclusion of natural ingredients in sunscreen formulations has gained attention. Curcumin, an active compound found in turmeric (Curcuma longa) and Java turmeric (Curcuma xanthorrhiza), is well-known for its antioxidant and anti-inflammatory properties. This review explores the potential of curcumin as a natural ingredient for enhancing the Sun Protection Factor (SPF) of sunscreen products. A systematic literature review was conducted, analyzing 200 articles sourced from Google Scholar and PubMed using keywords such as “Curcumin”, “Curcuma”, “Antioxidant”, “Anti-Inflammatory”, and “Sun Protection Factor”. Studies unrelated to UV protection were excluded. The findings, presented in tabular form, indicate that curcumin and Curcuma exhibit significant potential to enhance SPF values due to their antioxidant, anti-inflammatory, and UV-absorbing properties. Additionally, curcumin may aid in skin repair following UV-induced damage. However, the specific concentration of curcumin in various Curcuma species remains unknown, and further research is necessary to determine its optimal use. Consideration of additional excipients in sunscreen formulations is also required to maximize efficacy. In conclusion, curcumin demonstrates considerable promise as a sustainable and effective natural ingredient for protecting the skin from UV radiation, offering a safer alternative to conventional chemical-based sunscreens.
... Curcumin possesses antioxidant and antiinflammatory properties, which are attributed to the actions of enzymes like catalase, superoxide dismutase, and glutathione peroxidase. Notably, its antioxidant activity surpasses that of vitamin E by tenfold, owing to the presence of the 1,3-diketone system and the phenyl ring with the methoxy group, which impedes the generation of free radicals [31]. The phenolic composition of curcumin primarily accounts for its antioxidant efficacy, facilitating the elimination of hydroxyl and superoxide radicals. ...
... Curcumin, a compound found in turmeric, has garnered significant interest in the context of muscle injuries induced by sports due to its potential anti-inflammatory and antioxidant properties [30,31]. These characteristics make it a promising candidate for alleviating muscle damage and pain that often result from intense physical activities. ...
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Background: Sports practice, particularly eccentric exercises, induces significant muscular changes, including muscle fiber injuries, strength loss, pain, and increased permeability of the muscle membrane. The duration of muscle recovery depends on factors such as exercise intensity and the specific muscle groups engaged. The inflammatory response plays a crucial role in muscle regeneration, involving various cell types. Curcumin, especially when its stability is enhanced through encapsulation, exhibits potent antioxidant and anti-inflammatory properties. Supplementing with curcumin can reduce muscle damage and inflammation caused by eccentric exercise, making it a potential remedy for athletes. Objective: The objective of this systematic review is to assess the scientific evidence supporting the efficacy of curcumin in reducing muscle damage caused by sports. Methods: A structured search in SCOPUS, Medline, and Web of Science databases was conducted in March 2023, including all available articles. The strategy involved selecting English articles without time constraints, using the search terms "curcumin" AND "Exercise-Induced Muscle Damage" (ALL(curcumin AND "Exercise-Induced Muscle Damage")). Titles and abstracts were screened to assess eligibility. Studies were chosen based on PICOS criteria, and quality was evaluated using the reliable PEDro scale. The eligibility criteria included adults without any diagnosed diseases who regularly exercise (at least three times per week) and follow a consistent pattern of curcumin intake before, during, or after exercise. Results: The comprehensive search identified 11 relevant studies investigating the effects of curcumin supplementation in sport-simulated interventions. These studies suggest that curcumin intake may help reduce muscle symptoms associated with eccentric exercises, thereby improving pain perception. Effective use of curcumin depends on factors such as dosage, bioavailability, and timing, with post-exercise ingestion appearing to be more beneficial. Conclusions: Curcumin demonstrates a significant potential to relieve muscle-related symptoms, especially delayed-onset muscle soreness (DOMS) that arises from eccentric exercises, thus potentially improving the well-being of those who are trained. It also appears to have the capability to lower biomarkers associated with inflammation and boost antioxidant levels. Nevertheless, for future studies, the bioavailability of curcumin must be considered, as it is a key factor in its efficacy.
... Diabetes mellitus often leads to diabetic cardiomyopathy, which is dysfunction in the left ventricle of the heart during diastole or systole (Amalraj et al., 2017). Factors such as apoptosis, inflammation, hypertrophy, and oxidative damage contribute to negative effects on the heart in individuals with Type 2 diabetes. ...
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A group of metabolic disorders, known as diabetes mellitus, has reached pandemic levels worldwide. Managing patients with this complex illness, who require continuous medication and lifestyle  Corresponding Author's Email: sainiakki16041991@gmail.com. Aakriti Saini, Diksha Gulati, Deepshi Arora et al. 276 adjustments, poses a significant challenge. It is widely known that diabetes mellitus can be prevented, and reducing the number of new cases could help lessen its burden on the world. Current research supports the effectiveness of herbal supplements in preventing and controlling diabetes mellitus. One increasingly studied medicinal plant is curcumin, found in the rhizome of the turmeric plant, Curcuma longa. Turmeric, a natural product with extensive medicinal properties, has been predominantly linked to the therapeutic effects of curcuminoids on various diseases, including cancer, diabetes, and neurodegenerative, hepatic, and renal damage. Curcumin has been shown to improve the metabolic profile and related issues of diabetes mellitus, functioning as a hypoglycemic drug or as an adjuvant. It is important to investigate any potential interactions between curcumin and conventional antidiabetic medications for the treatment of diabetes mellitus.
... These observations confirmed the beneficial and the wide array of the pharmacological effects of turmeric extract due essentially to the presence of curcuminoids (a mixture of curcumin, demethoxycurcumin, and bisdemethoxycurcumin) which were reported to have several biological effects including anti-inflammatory, anticancer, anti-Alzheimer, antimicrobial effects, etc [28]. Curcumin alone can exert a more potent than curcuminoids (mixture) but some studies time, while C Loaded represents the concentration of the TE retained in the microcapsules. ...
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The present work investigated the possibility of encapsulating turmeric extract (TE) by complex coacervation using gelatin and carrageenan as the encapsulating wall to act as a delivery system in the production of TE-enriched kefir. Curcuminoids were the major compounds in TE, as shown by TLC and HPLC analysis. The free extract exhibited interesting biological effects, including antioxidant, anti-inflammatory, and antidiabetic effects, making it an interesting bioactive ingredient for functional foods. The extract was successfully incorporated into gelatin/carrageenan coacervates as indicated by a high encapsulation yield of 82.11 and an encapsulation efficiency of 92.2% for the ratio wall/core2:1.FTIR analysis showed that electrostatic interactions are the principal driving forces involved in the encapsulation process. The micro-particles presented a round shape with different sizes by Scanning Electron Microscopy (SEM) observation. The antibacterial effect of the encapsulated TE was lower compared to the free extract due to its entrapment by the biopolymers. Simulated digestion of TE-loaded microcapsules showed a burst release during the gastrointestinal phase (32.97% after the first 30 min and reach 39.56% after 2 h) and a gradual release during the intestinal digestion (48.01% at the end of the phase). The encapsulation of TE improved its stability during kefir storage compared to free extract. Thus, the encapsulation of TE gelatin/carrageenan microcapsules improved the stability of curcuminoids and can be serve as a carrier in food systems.
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Curcumin, a naturally occurring compound found in the rhizome of Curcuma plants, particularly in turmeric (Curcuma longa L.), exhibits a broad range of biological activities, including anti-inflammatory, antioxidant, and anticancer properties. Curcumin has demonstrated effectiveness in inhibiting tumor growth, arousing interest for its potential in treating various cancers, such as breast, lung, prostate, and brain cancers. However, the clinical application of curcumin is limited due to its low chemical stability, poor water solubility, and low bioavailability. In response to these challenges, structural modifications of curcumin have been explored to improve its pharmacological properties, including enhanced anticancer selectivity index and bioavailability. This review highlights promising chemical modifications of curcumin that could lead to the development of more effective anticancer therapies. By functionalizing the parent curcumin molecule, researchers aim to create more stable and bioavailable compounds with enhanced therapeutic potential, making curcumin derivatives promising candidates for medical applications.
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Background Turmeric (Curcuma longa L.) is a widely recognized spice and medicinal plant that has gained significant attention for its potential health benefits. This review aims to provide a comprehensive overview of the beneficial applications of turmeric in improving health and egg production in layers. Objective The objective of this review is to assess the current scientific literature on the effects of turmeric supplementation in layer diets and evaluate its impact on layer health and egg production. Methods A systematic search was conducted in Google Scholar database to identify relevant studies published in peer‐reviewed journals. Studies investigating the effects of turmeric or its bioactive compound curcumin on layer health and egg production were included. Data on various parameters, including immune function, reproductive performance, egg quality and production parameters, were extracted and analysed. Results Turmeric contains a bioactive compound called curcumin, which possesses antioxidant, anti‐inflammatory, antimicrobial and immunomodulatory effects. These properties have been extensively studied and have shown promising results in enhancing layer health and performance. Turmeric supplementation has been reported to improve the overall immune response in layers, reducing the incidence and severity of infectious diseases. It has also been shown to have positive effects on gut health by modulating the gut microbiota composition, improving nutrient absorption and reducing digestive disorders. Furthermore, studies have demonstrated that turmeric supplementation in layer diets can improve egg weight, shell quality, yolk colour and egg production rates. The mechanisms underlying these effects involve the antioxidant properties of turmeric, which protect the reproductive organs, enhance ovarian function and improve reproductive performance. Conclusion The findings underscore the potential of turmeric as a natural, cost‐effective and sustainable intervention for improving layer well‐being, egg quality and productivity. However, further research is needed to fully understand the mechanisms of action, optimize dosage regimens and evaluate the long‐term effects of turmeric supplementation in layer diets.
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Turmeric (Curcuma longa L.), the plant from which curcumin is derived, is renowned for its wide range of therapeutic and agricultural benefits. Curcumin, the key bioactive compound, is highly valued for its potent anti-provocative, antioxidant, and antimicrobial properties, which contribute to its effectiveness in treating various human diseases and improving plant resilience to environmental stresses. The therapeutics potential of curcumin is notable owing its abilities to combat microbes act as an oxidant and reduce inflammation. Its effectiveness in treating a range of human disease such as tumor, cardiac problems, and brain degenerative ailments stems from its ability to modulate various cellular process and signaling pathways. Despite its low bioavailability, innovations in delivery system such as nanoparticles and liposomal formulations, have enhanced its therapeutic efficacy by improving solubility and systemic absorption. In agriculture, curcumin's antimicrobial properties provide a natural alternative to chemical pesticides, offering protection against pathogens and enhancing plant resilience to specific environmental stresses such as drought, salinity, and oxidative stress. Nanotechnology applications have furthered these benefits by facilitating the efficient uptake and distribution of curcumin within plant tissues, promoting growth and stress tolerance. This review also highlights curcumin's nutritional benefits, including its impact on gut health and metabolic syndrome. Synergistic interactions with dietary nutrients can amplify its health benefits, making it a valuable dietary supplement. However, ongoing research is needed to fully understand curcumin's mechanisms of action and long-term safety. Overall, curcumin holds promise as a versatile agent in both medical and agricultural fields, supporting sustainable practices and advancing health outcomes. Future research should focus on optimizing curcumin formulations and translating preclinical findings into clinical successes. Graphical abstract Extended author information available on the last page of the article Journal of Umm Al-Qura University for Applied Sciences
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Curcumin, a curcuminoid from Curcuma longa, presents antioxidant and anti-inflammatory actions and, among pathological changes of cerebral ischemic injury, inflammation is an important one. The objectives were to study the neuroprotective action of curcumin, in a model of global ischemia. Male Wistar rats (sham-operated, ischemic untreated and ischemic treated with curcumin, 25 or 50 mg/kg, p.o.) were anesthesized and their carotid arteries occluded, for 30 min. The SO group had the same procedure, except for carotid occlusion. In the 1st protocol, animals were treated 1 h before ischemia and 24 h later; and in the 2nd protocol, treatments began 1 h before ischemia, continuing for 7 days. Twenty four hours after the last administration, animals were euthanized and measurements for striatal monoamines were performed, at the 1st and 7th days after ischemia, as well as histological and immunohistochemical assays in hippocampi. We showed in both protocols, depletions of DA and its metabolites (DOPAC and HVA), in the ischemic group, but these effects were reversed by curcumin. Additionally, a decrease seen in 5-HT contents, 1 day after ischemia, was also reversed by curcumin. This reversion was not seen 7 days later. On the other hand, a decrease observed in NE levels, at the 7th day, was totally reversed by curcumin. Furthermore, curcumin treatments increased neuronal viability and attenuated the immunoreactivity for COX-2 and TNF-alpha, in the hippocampus in both protocols. We showed that curcumin exerts neuroprotective actions, in a model of brain ischemia that are probably related to its anti-inflammatory activity.
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Synthesis and preclinical safety evaluation in mice and rats of Curcumin (1) and curcumin analogs (2, 3) were done. Besides, the chemopreventive effects in DMH-induced colon cancer in albino rats model were performed. Sections of mammary gland, heart, kidney, liver, spleen, and colon were done. Administration of the prophylactic treatment for four weeks before the induction of cancer by DMH, showed that compound 3 is the most active one. Chemopreventive treatment with different forms of curcumin extracts for 2 and 4 weeks caused a reduction in the number of aberrant crypt foci (ACF) especially compound 3. Chemopreventive treatment with different forms of curcumin extracts for 2 and 4 weeks caused a reduction in the number of tumor cells.
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Ginger [Zingiber officinale Roscoe (Zingiberaceae)] and turmeric [Curcuma longa Linn (Zingiberaceae)] rhizomes have been reportedly used in folk medicine for the treatment of hypertension. However, the prevention of its complication such as male infertility remains unexplored. Hence, the aim of the present study was to investigate the preventive effects of ginger and turmeric rhizomes on some biomarkers of male reproductive function in L-NAME-induced hypertensive rats. Male Wistar rats were divided into seven groups (. n=. 10): normotensive control rats; induced (L-NAME hypertensive) rats; hypertensive rats treated with atenolol (10. mg/kg/day); normotensive and hypertensive rats treated with 4% supplementation of turmeric or ginger, respectively. After 14 days of pre-treatment, the animals were induced with hypertension by oral administration of L-NAME (40. mg/kg/day). The results revealed significant decrease in serum total testosterone and epididymal sperm progressive motility without affecting sperm viability in hypertensive rats. Moreover, increased oxidative stress in the testes and epididymides of hypertensive rats was evidenced by significant decrease in total and non-protein thiol levels, glutathione S-transferase (GST) activity with concomitant increase in 2',7'-dichlorofluorescein (DFCH) oxidation and thiobarbituric acid reactive substances (TBARS) production. Similarly, decreased testicular and epididymal NO level with concomitant elevation in arginase activity was observed in hypertensive rats. However, dietary supplementation with turmeric or ginger efficiently prevented these alterations in biomarkers of reproductive function in hypertensive rats. The inhibition of arginase activity and increase in NO and testosterone levels by both rhizomes could suggest possible mechanism of action for the prevention of male infertility in hypertension. Therefore, both rhizomes could be harnessed as functional foods to prevent hypertension-mediated male reproductive dysfunction.
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Food Chemistry 194(2016): 695-704, http://dx.doi.org/10.1016/j.foodchem.2015.07.150
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To investigate the effects of bisdemethoxycurcumin (BDMC) on non-small cell lung cancer (NSCLC) cell line, A549, and the highly metastatic lung cancer 95D cells. CCK-8 assay was used to assess the effect of BDMC on cytotoxicity. Flow cytometry was used to evaluate apoptosis. Western blot analysis, electron microscopy, and quantification of GFP-LC3 punctuates were used to test the effect of BDMC on autophagy and apoptosis of lung cancer cells. BDMC inhibited the viability of NSCLC cells, but had no cytotoxic effects on lung small airway epithelial cells (SAECs). The apoptotic cell death induced by BDMC was accompanied with the induction of autophagy in NSCLC cells. Blockage of autophagy by the autophagy inhibitor 3-methyladenine (3-MA) repressed the growth inhibitory effects and induction of apoptosis by BDMC. In addition, BDMC treatment significantly decreased smoothened (SMO) and the transcription factor glioma-associated oncogene 1 (Gli1) expression. Furthermore, depletion of Gli1 by siRNA and cyclopamine (a specific SMO inhibitor) induced autophagy. Aberrant activation of Hedgehog (Hh) signaling has been implicated in several human cancers, including lung cancers. The present findings provide direct evidence that BDMC-induced autophagy plays a pro-death role in NSCLC, in part, by inhibiting Hedgehog signaling. Copyright © 2015 The Editorial Board of Biomedical and Environmental Sciences. Published by China CDC. All rights reserved.
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Tuberculosis (TB) is a major public health concern worldwide with over 2 billion people currently infected. The rise of strains of Mycobacterium tuberculosis (Mtb) that are resistant to some or all first and second line antibiotics, including multidrug-resistant (MDR), extensively drug resistant (XDR) and totally drug resistant (TDR) strains, is of particular concern and new anti-TB drugs are urgently needed. Curcumin, a natural product used in traditional medicine in India, exhibits anti-microbial activity that includes Mtb, however it is relatively unstable and suffers from poor bioavailability. To improve activity and bioavailability, mono-carbonyl analogs of curcumin were synthesized and screened for their capacity to inhibit the growth of Mtb and the related Mycobacterium marinum (Mm). Using disk diffusion and liquid culture assays, we found several analogs that inhibit in vitro growth of Mm and Mtb, including rifampicin-resistant strains. Structure activity analysis of the analogs indicated that Michael acceptor properties are critical for inhibitory activity. However, no synergistic effects were evident between the monocarbonyl analogs and rifampicin on inhibiting growth. Together, these data provide a structural basis for the development of analogs of curcumin with pronounced anti-mycobacterial activity and provide a roadmap to develop additional structural analogs that exhibit more favorable interactions with other anti-TB drugs. Copyright © 2015. Published by Elsevier Masson SAS.
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New fourteen 3,4-dihydropyrimidine derivatives/analogues of curcumin (2a–2n) were designed, synthesized and biologically evaluated for their cytotoxicity and antioxidant activity. Cytotoxicity effect has been evaluated against three cell lines HeLa, HCT-116 and QG-56 by MTT assay method. From SAR study, it has been revealed that particularly, compound 2e and 2j (IC50 value 12.5 μM) have shown better cytotoxicity effect against three cell lines. According to results of SAR study, it was found that 3,4-dihydropyrimidines of curcumin, 2c, 2d, 2j and 2n exhibited better antioxidant activity than curcumin. A correlation of structure and activities relationship of these compounds with respect to drug score profiles and other physico-chemical properties of drugs are described and verified experimentally. Therefore, we conclude that physico-chemical analyses may prove structural features of curcumin analogues with their promising combined cytotoxicity/antioxidant activity and it is also concluded from virtual and practical screening that the compounds were varied to possess a broad range of lipophilic character, revealed by Log P values.
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In the present study, three series of dimethylamino curcuminoids viz. 4-phenylaminomethyl curcumin (3a-d), arylidene curcumin (3e) and pyrazole curcumin (3f-i) derivatives have been synthesized and studied for their in vitro anti-inflammatory, antioxidant and antibacterial activities. Synthesized dimethylamino curcuminoid derivatives namely 3d, 3e, 3h and 3i have shown potent anti-inflammatory properties than parent curcumin. Molecular docking interactions of dimethylamino curcuminoids derivatives against cyclooxygenase enzymes (COX-1 and COX-2) were studied.
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The active ingredient curcuminoid (including curcumin, demethoxycurcumin and bisdemethoxycurcumin) from the Asian medicinal and culinary herb turmeric possesses anti-tumour effects, but poor oral absorption in the intestine impedes its widespread clinical application. Our previous study showed that turmerones increased the accumulation of curcumin inside colonic cells. The present study demonstrates the enhanced anti-proliferative and anti-angiogenic activities of curcumin in the presence of turmerones in human colon cancer cells and endothelial cells, respectively. Furthermore, in HT29 tumour xenograft-bearing mice fed with curcumin alone or turmeric ethanolic extract (in which the concentration of curcumin was kept the same), the tumour burden of turmeric extract-fed mice was the lowest, suggesting turmeric extract provided better anti-tumour activities than the same amount of curcumin alone did. The superior anti-tumour effects of turmeric extract, which contains curcumin, turmerones and other constituents, were verified in tumour-bearing mice, indicating the potential use of turmeric for colorectal cancer adjuvant therapy.
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Radiotherapy effectively treats cancers of the head and neck. We investigated the possible protective effects of lycopene and curcumin on the parotid glands of 40 female Sprague Dawley rats during irradiation. The study followed European Union regulations 86/609/EEC, 2010/63/EU for animal experimentation. The animals were divided into 4 groups: those treated with curcumin and radiation, those treated with lycopene and radiation, those treated with dimethyl sulphoxide (DMSO) and radiation, and those treated with radiation alone. All compounds were given intraperitoneally the day before irradiation. The total dose of radiation was 20 Gy. Morphological and histopathological analyses showed less cell necrosis in the group treated with curcumin than in the other groups, but the difference was not significant. Analysis of structural damage to the parotid ducts and vacuolisation showed significant differences among all groups (p=0.023, p<0.01). Lycopene and curcumin given 24 hours before irradiation reduced the structural damage to the salivary glands. Further studies are needed to confirm these findings.
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Cancer is a hyper proliferative disorder that metastasize into the vital organs in the body through invasion followed by angiogenesis and distant metastasis. Curcumin suppresses the proliferation of a wide variety of tumor cells, including breast carcinoma, colon carcinoma, renal cell carcinoma, hepatocellular carcinoma etc. The poor bio availability is the main drawback of the regular curcumin, which was addressed by Aurea biolabs and made a unique bio available formulation known as “cureit”. The cytotoxic effect of cureit was established by a spectrophotometrical study using MTT on the effects of cureit on cell proliferation. It is inferred that the test sample – “cureit” could serve as an anti cancer medication. © 2014, Journal of Chemical and Pharmaceutical Research. All rigthts reserved.
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Curcumin (Cur) has been demonstrated to have wide pharmacological window including anti-oxidant and anti-inflammatory properties. However, phototoxicity under sunlight exposure and poor biological availability limits its applicability. We have synthesized biodegradable and non-toxic polymer-poly (lactic-co-glycolic) acid (PLGA) encapsulated formulation of curcumin (PLGA-Cur-NPs) of 150 nm size range. Photochemically free curcumin generates ROS, lipid peroxidation and induces significant UVA and UVB mediated impaired mitochondrial functions leading to apoptosis/necrosis and cell injury in two different origin cell lines viz., mouse fibroblasts-NIH-3T3 and human keratinocytes-HaCaT as compared to PLGA-Cur-NPs. Molecular docking studies suggested that intact curcumin from nanoparticles, bind with BAX in BIM SAHB site and attenuate it to undergo apoptosis while upregulating anti-apoptotic genes like BCL2. Real time studies and western blot analysis with specific phosphorylation inhibitor of ERK1 and AKT1/2/3 confirm the involvement of ERK/AKT signaling molecules to trigger the survival cascade in case of PLGA-Cur-NPs. Our finding demonstrates that low level sustained release of curcumin from PLGA-Cur-NPs could be a promising way to protect the adverse biological interactions of photo-degradation products of curcumin upon the exposure of UVA and UVB. Hence, the applicability of PLGA-Cur-NPs could be suggested as prolonged radical scavenging ingredient in curcumin containing products.
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A test rig for double-sided labyrinth seals, which simulated the rim seal of a gas turbine rotor disk, was set up and aerodynamic performances of two different configurations (straight and stepped) were tested. Influences of pressure ratio and various combinations of tip clearances of the two sides on the seal performance were investigated. In addition to the overall seal performance, leakage behaviors of the individual seals (upstream and downstream) were separately analyzed and compared. The leakage reduction effect of step decreases with decreasing clearance. If the difference in the clearances of the two sides is sufficiently large, the smaller clearance side fully dominates the overall seal leakage behavior. Predictions by an analytic model and CFD were also carried out, and CFD gives better agreements with the test n general.
Article
Curcuminoids possess powerful antioxidant activity as demonstrated in many chemical in vitro tests and in several in vivo trials. Nevertheless, the mechanism of this activity is not completely elucidated and studies on the in vivo antioxidant effects are still needed. Metabolomics may be used as an attractive approach for such studies and in this paper, we describe the effects of oral administration of a Curcuma longa L. extract (150mg/kg of total curcuminoids) to 12 healthy rats with particular attention to urinary markers of oxidative stress. The experiment was carried out over 33days and changes in the 24-h urine samples metabolome were evaluated by (1)H-NMR and HPLC-MS. Both techniques produced similar representations for the collected samples confirming our previous study. Modifications of the urinary metabolome lead to the observation of different variables proving the complementarity of (1)H-NMR and HPLC-MS for metabolomic purposes. The urinary levels of allantoin, m-tyrosine, 8-hydroxy-2'-deoxyguanosine, and nitrotyrosine were decreased in the treated group thus supporting an in vivo antioxidant effect of the oral administration of Curcuma extract to healthy rats. On the other hand, urinary TMAO levels were higher in the treated compared to the control group suggesting a role of curcumin supplementation on microbiota or on TMAO urinary excretion. Furthermore, the urinary levels of the sulfur containing compounds taurine and cystine were also changed suggesting a role for such constituents in the biochemical pathways involved in Curcuma extract bioactivity and indicating the need for further investigation on the complex role of antioxidant curcumin effects.
Article
Series of curcumin derivatives/analogues were designed and efficient method for synthesis thereof is described. All the synthesized compounds have been screened for their cytotoxicity and evaluated their antioxidant activity. Cytotoxicity effect has been evaluated against three cell lines Hep-G2, HCT-116 and QG-56 by MTT assay method. Structure activity relationship has revealed that particularly, compound 3c, (IC50 value 6.25 μM) has shown better cytotoxicity effect against three cell lines. According to results of SAR study, it was found that 4H-pyrimido[2,1-b]benzothiazole derivatives (2e and 2f), pyrazoles (3a, 3b, 3c and 3d) benzylidenes (4d) exhibited better antioxidant activity than curcumin. A correlation of structure and activities relationship of these compounds with respect to drug score profiles and other physico-chemical properties of drugs are described and verified experimentally.
Article
Curcumin due to its various medicinal, biological, pharmacological activities is high on demand and has high market potential, high cost. Since curcumin has variety of uses, extracting it in a less expensive method other Super Critical Fluid Extraction is the main aim or objective of this work. Usage of food grade solvents is a main prerequisite of this work and optimization of the parameters in order to find an effective means of extraction sum ups the cause of this project work. Besides working on the extraction of curcumin, other properties such as curcumin's antioxidant, antimicrobial properties are to be envisaged upon. This project work mainly deals with the topic on 'extraction of curcumin' from its common source turmeric, using an effective low cost method of solvent extraction. Different solvents are used either in their pure form or being mixed in definite ratio's, while taking into consideration of other parameters such as particle size, time, temperature, solid: solvent ratio. The qualitative analysis of its antimicrobial property is also done along with the product development of Cake. Keywords - Antiflatulent, Antifibrotic, Antimutagenic, Carcinogenesis, Ulcerogenic 1.1 Chemical composition of turmeric Turmeric contains protein (6.3%), fat (5.1%), minerals (3.5%), carbohydrates (69.4%) and moisture (13.1%). The essential oil (5.8%) obtained by steam distillation of rhizomes has a-phellandrene (1%), sabinene (0.6%), cineol (1%), borneol (0.5%), zingiberene (25%) and sesquiterpines (53%)5. Curcumin
Article
Photoactive metal complexes have emerged as potential candidates in the photodynamic therapy (PDT) of cancer. We present here the synthesis, characterization and visible light-triggered anticancer activity of two novel mixed-ligand oxo-bridged iron(III) complexes, viz., [{Fe(L)(acac)}2(μ-O)](ClO4)2 (1) and [{Fe(L)(cur)}2(μ-O)](ClO4)2 (2) where L is bis-(2-pyridylmethyl)-benzylamine, acac is acetylacetonate and cur is the monoanion of curcumin (bis(4-hydroxy-3-methoxyphenyl)-1,6-diene-3,5-dione). The crystal structure of complex 1 (as PF6- salt, 1a) shows distorted octahedral geometry of each iron(III) centre formed by the FeN3O3 core. The 1:2 electrolytic complexes are stable in solution and retain their oxo-bridged identity in aqueous medium. Complex 2 has a strong absorption band in the visible region and shows promising photocytotoxicity in HeLa and MCF-7 cancer cells in visible light giving respective IC50 values of 3.1 ± 0.4 μM and 4.9 ± 0.5 μM while remains non-toxic in the dark (IC50 > 50 μM). The control complex 1 is inactive both in the light and dark. Complex 2 accumulates in cytoplasm of HeLa and MCF-7 cells as evidenced from fluorescence microscopy and triggers apoptotic cell death via light-assisted generation of reactive oxygen species (ROS). Taken together, complex 2 with its promising photocytotoxicity but negligible dark toxicity in cancer cells has significant photochemotherapeutic potential for applications in PDT.
Article
Background: Curcumin has a wide range of pharmacological activities including antioxidant, anti-inflammatory, antidiabetic, antibacterial, wound healing, antiatherosclerotic, hepatoprotective and anti-carcinogenic. However, its clinical applications are limited owing to its poor aqueous solubility, multidrug pump P-gp efflux, extensive in vivo metabolism and rapid elimination due to glucuronidation/sulfation. Purpose: The objective of the current work was to prepare novel curcumin loaded mixed micelles (CUR-MM) of Pluronic F-127 (PF127) and Gelucire(®) 44/14 (GL44) in order to enhance its oral bioavailability and cytotoxicity in human lung cancer cell line A549. Study design: 3(2) Factorial design was used to assess the effect of formulation variables for optimization of mixed micelle batch. Methods: CUR-MM was prepared by a solvent evaporation method. The optimized CUR-MM was evaluated for size, entrapment efficiency (EE), in vitro curcumin release, cytotoxicity and oral bioavailability in rats. Results: The average size of CUR-MM was found to be around 188 ± 3 nm with an EE of about 76.45 ± 1.18% w/w. In vitro dissolution profile of CUR-MM revealed controlled release of curcumin. Additionally, CUR-MM showed significant improvement in cytotoxic activity (3-folds) and oral bioavailability (around 55-folds) of curcumin as compared to curcumin alone. Such significant improvement in cytotoxic activity and oral bioavailability of curcumin when formulated into mixed micelles could be attributed to solubilization of hydrophobic curcumin into micelle core along with P-gp inhibition effect of both, PF127 and GL44. Conclusion: Thus the present work propose the formulation of mixed micelles of PF127 and GL44 which can act as promising carrier systems for hydrophobic drugs such as curcumin with significant improvement in their oral bioavailability.
Article
The first total synthesis of a C5-curcumin-2-hexadecynoic acid (C5-Curc-2-HDA, 6) conjugate was successfully performed. Through a three-step synthetic route, conjugate 6 was obtained in 13% overall yield and tested for antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) strains. Our results revealed that 6 was active against eight MRSA strains at MICs that range between 31.3 and 62.5μg/mL. It was found that the presence of 2-hexadecynoic acid (2-HDA, 4) in conjugate 6 increased 4-8-fold its antibacterial activity against MRSA strains supporting our hypothesis that the chemical connection of 4 to C5-curcumin (2) increases the antibacterial activity of 2 against Gram-positive bacteria. Combinational index (CIn) values that range between 1.6 and 2.3 were obtained when eight MRSA strains were treated with an equimolar mixture of 2 and 4. These results demonstrated that an antagonistic effect is taking place. Finally, it was investigated whether conjugate 6 can affect the replication process of S. aureus, since this compound inhibited the supercoiling activity of the S. aureus DNA gyrase at minimum inhibitory concentrations (MIC) of 250μg/mL (IC50=100.2±13.9μg/mL). Moreover, it was observed that the presence of 4 in conjugate 6 improves the anti-topoisomerase activity of 2 towards S. aureus DNA gyrase, which is in agreement with results obtained from antibacterial susceptibility tests involving MRSA strains.
Article
Curcumin is a natural antioxidant dye that has a wide spectrum of biological activities (e.g., anti-cancer, anti-hypertensive, anti-inflammatory and neuroprotective activities), and there is a high interest within the food industry to increase its use as a natural additive. However, due to its high hydrophobicity, it is difficult to incorporate into aqueous formulations and its bioavailability can be severely decreased. Lipid-based encapsulation systems such as nanoemulsions can help to overcome both of these drawbacks. In this study, curcumin-loaded nanoemulsions were produced by the emulsification inversion point method, for which some of the operational parameters were optimized. The most stable formulations were composed of 20% soybean oil, 10% Tween 80 and 20% glycerol and were produced with an anchor blade impeller operating at 300 rpm; this combination of parameters resulted in 0.07% encapsulation of the curcumin. After 60 days, 70% of the initial amount of curcumin remained in the nanoemulsions, which is a promising result when compared with those of other lipid-based encapsulation systems. The data also indicated that the catastrophic phase inversion occurred due to the formation of multiple o/w/o emulsions.
Article
Turmeric (Curcuma longa) is a popular Indian spice that has been used for centuries in herbal medicines for the treatment of a variety of ailments such as rheumatism, diabetic ulcers, anorexia, cough and sinusitis. Curcumin (diferuloylmethane) is the main curcuminoid present in turmeric and responsible for its yellow color. Curcumin has been shown to possess significant anti-inflammatory, anti-oxidant, anti-carcinogenic, anti-mutagenic, anticoagulant and anti-infective effects. This review summarizes and discusses recently published papers on the key biomedical applications of curcumin based materials. The highlighted studies in the review provide evidence of the ability of curcumin to show the significant vitro antioxidant, diabetic complication, antimicrobial, neuroprotective, anti-cancer activities and detection of hypochlorous acid, wound healing, treatment of major depression, healing of paracentesis, and treatment of carcinoma and optical detection of pyrrole properties. Hydrophobic nature of this polyphenolic compound along with its rapid metabolism, physicochemical and biological instability contribute to its poor bioavailability. To redress these problems several approaches have been proposed like encapsulation of curcumin in liposomes and polymeric micelles, inclusion complex formation with cyclodextrin, formation of polymer-curcumin conjugates, etc.
Article
We synthesized a library of curcumin mimics with diverse alkylsulfonyl and substituted benzenesulfonyl modifications through a simple addition reaction of important intermediate, 1-(3-Amino-phenyl)-3-(4-hydroxy-3-methoxy-phenyl)-propenone (10), with various sulfonyl chloride reactants and then tested their vasodilatation effect on depolarization (50mM K(+))- and endothelin-1 (ET-1)-induced basilar artery contraction. Generally, curcumin mimics with aromatic sulfonyl groups showed stronger vasodilation effect than alkyl sulfonylated curcumin mimics. Among the tested compounds, six curcumin mimics (11g, 11h, 11i, 11j, 11l, and 11s) in a depolarization-induced vasoconstriction and seven compounds (11g, 11h, 11i, 11j, 11l, 11p, and 11s) in an ET-1-induced vasoconstriction showed strong vasodilation effect. Based on their biological properties, synthetic curcumin mimics can act as dual antagonist scaffold of L-type Ca(2+) channel and endothelin A/B2 receptor in vascular smooth muscle cells. In particular, compounds 11g and 11s are promising novel drug candidates to treat hypertension related to the overexpression of L-type Ca(2+) channels and ET peptides/receptors-mediated cardiovascular diseases.
Article
Rhizoma Paridis saponins combined with turmeric (RT) showed well anti-hepatocarcinoma activities in our previous research. The aim of this study was to investigate the progression of the biochemical response to RT and capture metabolic variations during intragastric administration of their compatibility. In the experiment, histopathological examination and (1)H NMR method were developed and validated for the metabolic profiling of RT intervention in H22 tumor growth. Data were analyzed with principal components analysis (PCA) and partial least-squares discrimination analysis (PLS-DA). As a result, Rhizoma paridis saponins (RPS) or RT induced inflammatory cell infiltration in tumors. RT also mediated the tumor microenvironment to promote anti-tumor immunity of mice. RT significantly inhibited tumor growth rate through suppressing levels of amino acids containing alanine, asparagine, glutamine, putrescine, and sarcosine, lipid compounds, and carbohydrates like myo-inositol and arabinose in the tumor tissues. In conclusion, these results uncovered unexpectedly poor nutritional conditions in the RT-treated tumor tissues whose effect was stronger than RPS's. Therefore, RT could be a novel anticancer agent that targets on cancer metabolism through starving tumors reducing viability of cancer cells.
Article
A series of novel curcumin bisacetamides aiming of enriching their biological activities have been synthesized. The synthesized compounds were screened for their in vitro antioxidant, anti-inflammatory and cytotoxic activities. All the compounds exhibited potent to good anti-inflammatory, antioxidant and noteworthy cytotoxic activities. Copyright © 2015. Published by Elsevier Ltd.
Article
Curcumin, a polyphenolic compound abundant in the rhizome of Curcuma longa, has been reported to have various beneficial biological and pharmacological activities. Recent research revealed that curcumin might be valuable in the prevention and therapy of numerous disorders including neurodegenerative diseases like Alzheimer's disease. Due to its low absorption and quick elimination from the body, curcumin bioavailability is rather low which poses major problems for the use of curcumin as a therapeutic agent. There are several approaches to ameliorate curcumin bioavailability after oral administration, amongst them simultaneous administration with secondary plant compounds, micronization and micellation. We examined bioavailability in vivo in NMRI mice and the effects of native curcumin and a newly developed curcumin micelles formulation on mitochondrial function in vitro in PC12 cells and ex vivo in isolated mouse brain mitochondria. We found that curcumin micelles improved bioavailability of native curcumin around 10- to 40-fold in plasma and brain of mice. Incubation with native curcumin and curcumin micelles prevented isolated mouse brain mitochondria from swelling, indicating less mitochondrial permeability transition pore (mPTP) opening and prevention of injury. Curcumin micelles proved to be more efficient in preventing mitochondrial swelling in isolated mouse brain mitochondria and protecting PC12 cells from nitrosative stress than native curcumin. Due to their improved effectivity, curcumin micelles might be a suitable formulation for the prevention of mitochondrial dysfunction in brain aging and neurodegeneration. Copyright © 2015. Published by Elsevier Ltd.
Article
Sexually transmitted infections and unplanned pregnancies present a great risk to the reproductive health of women. Therefore, female-controlled vaginal products directed toward disease prevention and contraception is needed urgently. The purpose of this investigation was to develop poloxamer based thermo sensitive contraceptive vaginal in situ hydrogel of curcumin, a plant-derived diferuloylmethane compound. Different formulations using different ratio of poloxamer 407/188 and mucoadhesive polymer - HPMC K4M were prepared and optimized by box behnken experimental design (BBD). Formulations were optimized on the basis of gelation temperature (0C), gel strength (gm/cm2), Mucoadhesive strength (dyne/cm2), viscosity (Pa) and % drug release. Optimized formulation was subjected to In Vitro sperm immobilization study on 5 fertile human volunteers’ ejaculate sample. The quantitative effect of independent variables on dependent variables at different levels could be predicted by polynomial equations. From BBD, that batch containing 19.96% Poloxamer 407, 3.83% Poloxamer 188, 0.91% HPMC K4M was optimized. Total 100 % Sperm immobilization was achieved within 15 min. by optimized formulation for 3.5 ml of dose. Stability study of optimized batch shows no change in physical and chemical characteristics. Curcumin would be successfully formulated as thermo sensitive In Situ gelling mucoadhesive system for contraception.
Article
In this study, the isolation of curcuminoids from turmeric (Curcuma longa L.) was performed using different solvent extraction methods and solvents. Obtained extracts were analyzed for the contents of curcumin, demethoxycurcumin and bisdemethoxycurcumin by HPLC and the radical scavenging and antibacterial activities of extracts were determined. Extract with highest content of curcuminoids was mixed with polyethylene glycol (PEG) and formulated into powder using PGGS™ method. Obtained powder was pressed into tablets and a release study of the curcuminoids from the product was observed in simulated gastric and intestinal fluids.
Article
Arsenic (As) is a well-known human carcinogen and a potent hepatotoxin. Environmental exposure to arsenic imposes a serious health hazard to humans and other animals worldwide. Tetrahydrocurcumin (THC), one of the major metabolites of curcumin, exhibits many of the same physiological and pharmacological activities as curcumin and in some systems may exert greater antioxidant activity than the curcumin. It has been reported that THC has antioxidant efficacy attributable to the presence of identical β-diketone of 3rd and 5th substitution in heptane moiety. In the present study, rats were orally treated with arsenic alone (5mgkg(-1)bw/day) with THC (80mgkg(-1)bw/day) for 28days. Hepatotoxicity was measured by the increased activities of serum hepatospecific enzymes, namely aspartate transaminase, alanine transaminase, alkaline phosphatase and bilirubin along with increased elevation of lipid peroxidative markers, thiobarbituric acid reactive substances. And also elevated levels of serum cholesterol, triglycerides, free fatty acids and phospholipids were observed in arsenic intoxicated rats. These effects of arsenic were coupled with enhanced mitochondrial swelling, inhibition of cytochrome c oxidase, Ca(2+)ATPase and a decrease in mitochondrial calcium content. The toxic effect of arsenic was also indicated by significantly decreased activities of enzymatic antioxidants such as superoxide dismutase, catalase, and glutathione peroxidase along with non-enzymatic antioxidant such as reduced glutathione. Administration of THC exhibited significant reversal of arsenic induced toxicity in hepatic tissue. All these changes were supported by the reduction of arsenic concentration and histopathological observations of the liver. These results suggest that THC has a protective effect over arsenic induced toxicity in rat. Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.
Article
Angiogenesis is essential for tumor growth and there is a continuing need for exploring new anti-angiogenic agents from natural products including herbs. Aromatic (Ar)-turmerone isolated from the rhizome of Curcuma longa Linn. (Turmeric) exhibits anti-tumor and immunomodulatory activities. In this study, the anti-angiogenic effects of Ar-turmerone were evaluated in human microvascular endothelial cells, zebrafish and Matrigel plugs mouse models. The data obtained indicate that Ar-turmerone treatment significantly inhibits the proliferation, tube formation and motility of HMEC-1 cells at non-cytotoxic concentrations (4.6–9.2 µM, p < 0.05). The mRNA expressions of metalloproteinase-2 and -9 as well as adhesion molecules could be down-regulated by Ar-turmerone at 18.4 µM (p < 0.05). In zebrafish model, the new blood vessel growth in embryos was significantly blocked by Ar-turmerone treatment (12.5–25 µg/mL medium). The bFGF-induced blood vessel formation in Matrigel plugs in C57BL/6 mice was suppressed by Ar-turmerone (25–50 µg/mL Matrigel). Thus, the in vitro and in vivo anti-angiogenic activities of Ar-turmerone were demonstrated for the first time. The findings suggest that such a component of turmeric essential oil has the potential to be further developed as an anti-angiogenic agent.
Article
Curcumin (CUR) has been proven to be clinically effective in rheumatoid arthritis (RA) therapy, but its low oral bioavailability eclipses existent evidence that attempts to explain the underlying mechanism. Small intestine, the only organ exposed to a relatively high concentration of CUR, is the main site that generates gut hormones which are involved in the pathogenesis of RA. This study aims at addressing the hypothesis that one or more gut hormones serve as an intermediary agent for the anti-arthritic action of CUR. The protein and mRNA levels of gut hormones in CUR-treated rats were analyzed by ELISA and RT-PCR. Somatostatin (SOM) depletor and receptor antagonist were used to verify the key role of SOM in CUR-mediated anti-arthritic effect. The mechanisms underlying CUR-induced upregulation of SOM levels were explored by cellular experiments and immunohistochemical staining. The data showed that oral administration of CUR (100 mg/kg) for consecutive two weeks in adjuvant-induced arthritis rats still exhibited an extremely low plasma exposure despite of a dramatic amelioration of arthritis symptoms. When injected intraperitoneally, CUR lost anti-arthritic effect in rats, suggesting that it functions in an intestine-dependent manner. CUR elevated SOM levels in intestines and sera, and SOM depletor and non-selective SOM receptor antagonist could abolish the inhibitory effect of CUR on arthritis. Immunohistochemical assay demonstrated that CUR markedly increased the number of SOM-positive cells in both duodenum and jejunum. In vitro experiments demonstrated that CUR could augment SOM secretion from intestinal endocrine cells, and this effect could be hampered by either MEK1/2 or Ca2+/calmodulin-dependent kinase II (CAMKII) inhibitor. In summary, oral administration of CUR exhibits anti-arthritic effect through augmenting SOM secretion from the endocrine cells in small intestines via cAMP/PKA and Ca2+/CaMKII signaling pathways.
Article
Turmeric (Curcuma longa L.) powder was used to substitute 0%, 2%, 4%, 6% and 8% of wheat flour for making turmeric wheat breads. Proximate composition, physical quality, functional components (curcumin and total phenols) and antioxidant properties of breads containing turmeric were analysed and compared with those of wheat bread. Hardness, crumb colour a and b values, curcumin content and total phenolic contents of breads significantly increased with the addition of turmeric powder. Water activity, specific volume and crumb colour L value of breads decreased with the addition of turmeric powder. Breads containing turmeric powder also showed good antioxidant activity as tested by the b-carotene-linoleate bleaching assay. A 4% substitution of wheat flour with turmeric powder showed acceptable sensory scores which were comparable to wheat bread. Breads containing turmeric powder can thus be developed as a health-promoting functional food.
Article
Two ruthenium-arene complexes containing curcuminoid ligands, (eta(6)-cymene)Ru(curc)Cl (1 and 2, curc = thiophene aromatic curcuminoids) have been synthesized and characterized by NMR, elemental analysis and HR-ESI-mass spectrometry. The molecular structures of the two complexes were determined by single-crystal X-ray diffraction analysis. The complexes were further evaluated for their in vitro antiproliferative activities against Hela human cervical epithelioid cancer, as well as BEL-7404 and SMMC-7721 human liver cancer cell lines. Furthermore, the interactions of the complexes with DNA were followed by electrophoretic mobility spectrometry studies.
Article
Curcumin (CCM) is a bioactive polyphenolic compound that suffers a low bioavailability because of its low water solubility. In this work β-lactoglobulin (β-Lg) and nanoemulsion were used as carriers to deliver curcumin. The pH stability of β-Lg-CCM was investigated. The digestion of β-Lg-CCM and the nanoemulsion was studied using an in vitro gastrointestinal model. The effect of different carriers on the permeability of curcumin was assessed using the Caco-2 cell monolayer model. The results revealed that the water solubility and the pH stability of curcumin significantly increased by binding with β-Lg. In SDS-PAGE experiments the β-Lg-CCM complex and nanoemulsion were found to be resistant to pepsin digestion but sensitive to trypsin. In the permeability experiment it was shown that the digested nanoemulsion and β-Lg-CCM improved significantly the permeation rate of curcumin. Copyright © 2015 Elsevier Ltd. All rights reserved.
Article
In vitro gastrointestinal digestion models were used to investigate bioaccessibility of curcuminoids delivered with buttermilk. The percentage of solubilised curcuminoids that partitioned into the micelle in aqueous phase was determined. In fasted states (0–2.5 mg bile extract/mL sample), the bioaccessibility of curcuminoids (2% v/v ethanol) ranged from 16.3% to 26.7% in buttermilk, and from 11.4% to 18.7% with neat curcuminoids. In fed states (10–40 mg bile extract/mL sample), the bioaccessibility of curcuminoids in buttermilk was 21.3% (no ethanol) and ranged from 37.1% to 69.2% (2% v/v ethanol), while for neat curcuminoids bioaccessibility was 14.1% (no ethanol), ranging from 45.6% to 79.6% (2% v/v ethanol). The in vitro bioaccessibility of curcuminoids was influenced by the presence of the carrier (buttermilk) and ethanol, and increased significantly with increasing amount of bile extract. Curcuminoids did not markedly influence the digestibility of protein or lipids. These findings demonstrated that buttermilk could be used as a carrier for curcuminoids especially if delivered with food.
Article
The aim of the present study was to examine the protective effect of curcumin (CUR) on carbon tetrachloride (CCl4)-induced nephrotoxicity to evaluate the detailed mechanisms by which CUR exerts its protective action. Thirty male Wistar-Albino rats weighing 250-300g were randomly divided into three groups: administrations of olive oil (control, po), CCl4 (0.5mg/kg in olive oil sc) every other day for 3 weeks, and CCl4 (0.5mg/kg in olive oil sc) plus CUR (200mg/kg) every day for 3 weeks. Administration of CCl4 significantly (p<0.001) increased the levels of renal function test such as creatinine and blood urea nitrogen (BUN). Furthermore, treatment of CCl4 significantly elevated the oxidant status of renal tissues while decreasing its anti-oxidant status (p<0.001). CUR displayed a renal protective effect as evident by significant decrease in inflammation and apoptosis during histopathological examination. The administration of CCl4 resulted in an increase in malondialdehyde (MDA) production due to an increase in membrane lipid peroxidation; however, the administration of CUR attenuated this, probably via its antioxidant and free radical scavenging properties. The finding of our study indicates that CUR may have an important role to play in protecting the kidney from oxidative insult. Copyright © 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.