Displaying publications 1 - 20 of 151 in total

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  1. Assessing the potential of liposomes loaded with curcumin as a therapeutic intervention in asthma
    Ng ZY, Wong JY, Panneerselvam J, Madheswaran T, Kumar P, Pillay V, et al.
    Colloids Surf B Biointerfaces, 2018 Dec 01;172:51-59.
    PMID: 30134219 DOI: 10.1016/j.colsurfb.2018.08.027
    Curcumin a component of turmeric, which is derived from Curcuma longa is used as a colouring agent and as a dietary spice for centuries. Extensive studies have been done on the anti-inflammatory activity of curcumin along with its molecular mechanism involving different signalling pathways. However, the physicochemical and biological properties such as poor solubility and rapid metabolism of curcumin have led to low bioavailability and hence limits its application. Current therapies for asthma such as bronchodilators and inhaled corticosteroids (ICS) are aimed at controlling disease symptoms and prevent asthma exacerbation. However, this approach requires lifetime therapy and is associated with a constellation of side effects. This creates a clear unmet medical need and there is an urgent demand for new and more-effective treatments. The present study is aimed to formulate liposomes containing curcumin and evaluate for its anti-inflammatory effects on lipopolysaccharide (LPS)-induced inflammation on BCi-NS1.1 cell line. Curcumin and salbutamol liposomes were formulated using lipid hydration method. The prepared liposomes were characterized in terms of particle size, zeta potential, encapsulation efficiency and in-vitro release profile. The liposomes were tested on BCI-NS1.1 cell line to evaluate its anti-inflammatory properties. The various pro-inflammatory markers studied were Interleukin-6 (IL-6), Interleukin-8 (IL-8), Interleukin-1β (IL-1β) and Tumour Necrosis Factor-a (TNF-a). Additionally, molecular mechanics simulations were used to elucidate the positioning, energy minimization, and aqueous dispersion of the liposomal architecture involving lecithin and curcumin. The prepared curcumin formulation showed an average size and zeta potential of 271.3 ± 3.06 nm and -61.0 mV, respectively. The drug encapsulation efficiency of liposomal curcumin is 81.1%. Both curcumin-loaded liposomes formulation (1 μg/mL, 5 μg/mL) resulted in significant (p curcumin with the dose of 1 μg/mL reduced the inflammatory markers more effectively compared to that of 5 μg/mL. Liposomal curcumin could be a promising intervention for asthma therapy showing their efficacy in suppressing the important pro-inflammatory markers involved in the pathogenesis of asthma.
    Matched MeSH terms: Curcumin*
  2. Fulltext Curcumin Metabolite Tetrahydrocurcumin in the Treatment of Eye Diseases
    Kao YW, Hsu SK, Chen JY, Lin IL, Chen KJ, Lee PY, et al.
    Int J Mol Sci, 2020 Dec 28;22(1).
    PMID: 33379248 DOI: 10.3390/ijms22010212
    Curcumin is one of the most valuable natural products due to its pharmacological activities. However, the low bioavailability of curcumin has long been a problem for its medicinal use. Large studies have been conducted to improve the use of curcumin; among these studies, curcumin metabolites have become a relatively new research focus over the past few years. Additionally, accumulating evidence suggests that curcumin or curcuminoid metabolites have similar or better biological activity than the precursor of curcumin. Recent studies focus on the protective role of plasma tetrahydrocurcumin (THC), a main metabolite of curcumin, against tumors and chronic inflammatory diseases. Nevertheless, studies of THC in eye diseases have not yet been conducted. Since ophthalmic conditions play a crucial role in worldwide public health, the prevention and treatment of ophthalmic diseases are of great concern. Therefore, the present study investigated the antioxidative, anti-inflammatory, antiangiogenic, and neuroprotective effects of THC on four major ocular diseases: age-related cataracts, glaucoma, age-related macular degeneration (AMD), and diabetic retinopathy (DR). While this study aimed to show curcumin as a promising potential solution for eye conditions and discusses the involved mechanistic pathways, further work is required for the clinical application of curcumin.
    Matched MeSH terms: Curcumin/analogs & derivatives*; Curcumin/metabolism; Curcumin/therapeutic use
  3. Exploring recent developments to improve antioxidant, anti-inflammatory and antimicrobial efficacy of curcumin: A review of new trends and future perspectives
    Hussain Z, Thu HE, Amjad MW, Hussain F, Ahmed TA, Khan S
    Mater Sci Eng C Mater Biol Appl, 2017 Aug 01;77:1316-1326.
    PMID: 28532009 DOI: 10.1016/j.msec.2017.03.226
    Curcumin derivatives have been well-documented due to their natural antioxidant, antimicrobial and anti-inflammatory activities. Curcuminoids have also gained widespread recognition due to their wide range of other activities which include anti-infective, anti-mutagenic, anticancer, anti-coagulant, antiarthrititc, and wound healing potential. Despite of having a wide range of activities, the inherent physicochemical characteristics (poor water solubility, low bioavailability, chemical instability, photodegradation, rapid metabolism and short half-life) of curcumin derivatives limit their pharmaceutical significance. Aiming to overcome these pharmaceutical issues and improving therapeutic efficacy of curcuminoids, newer strategies have been attempted in recent years. These advanced techniques include polymeric nanoparticles, nanocomposite hydrogels, nanovesicles, nanofibers, nanohybrid scaffolds, nanoconjugates, nanostructured lipid carriers (NLCs), nanoemulsion, polymeric micelles and polymeric blend films. Incorporation of curcumin in these delivery systems has shown improved solubility, transmembrane permeability, long-term stability, improved bioavailability, longer plasma half-life, target-specific delivery, and upgraded therapeutic efficacy. In this review, a range of in vitro and in vivo studies have been critically discussed to explore the pharmaceutical significance and therapeutic viability of the advanced delivery systems to improve antioxidant, anti-inflammatory and antimicrobial efficacies of curcumin and its derivatives.
    Matched MeSH terms: Curcumin/pharmacology*
  4. Current prospects of synthetic curcumin analogs and chalcone derivatives against mycobacterium tuberculosis
    Bukhari SN, Franzblau SG, Jantan I, Jasamai M
    Med Chem, 2013 Nov;9(7):897-903.
    PMID: 23305394
    Tuberculosis, caused by Mycobacterium tuberculosis, is amongst the foremost infectious diseases. Treatment of tuberculosis is a complex process due to various factors including a patient's inability to persevere with a combined treatment regimen, the difficulty in eradicating the infection in immune-suppressed patients, and multidrug resistance (MDR). Extensive research circumscribing molecules to counteract this disease has led to the identification of many inhibitory small molecules. Among these are chalcone derivatives along with curcumin analogs. In this review article, we summarize the reported literature regarding anti tubercular activity of chalcone derivatives and synthetic curcumin analogs. Our goal is to provide an analysis of research to date in order to facilitate the synthesis of superior antitubercular chalcone derivatives and curcumin analogs.
    Matched MeSH terms: Curcumin/analogs & derivatives; Curcumin/pharmacology*; Curcumin/therapeutic use; Curcumin/chemistry
  5. Fulltext Curcumin: the spicy modulator of breast carcinogenesis
    Banik U, Parasuraman S, Adhikary AK, Othman NH
    J Exp Clin Cancer Res, 2017 Jul 19;36(1):98.
    PMID: 28724427 DOI: 10.1186/s13046-017-0566-5
    Worldwide breast cancer is the most common cancer in women. For many years clinicians and the researchers are examining and exploring various therapeutic modalities for breast cancer. Yet the disease has remained unconquered and the quest for cure is still going on. Present-day strategy of breast cancer therapy and prevention is either combination of a number of drugs or a drug that modulates multiple targets. In this regard natural products are now becoming significant options. Curcumin exemplifies a promising natural anticancer agent for this purpose. This review primarily underscores the modulatory effect of curcumin on the cancer hallmarks. The focus is its anticancer effect in the complex pathways of breast carcinogenesis. Curcumin modulates breast carcinogenesis through its effect on cell cycle and proliferation, apoptosis, senescence, cancer spread and angiogenesis. Largely the NFkB, PI3K/Akt/mTOR, MAPK and JAK/STAT are the key signaling pathways involved. The review also highlights the curcumin mediated modulation of tumor microenvironment, cancer immunity, breast cancer stem cells and cancer related miRNAs. Using curcumin as a therapeutic and preventive agent in breast cancer is perplexed by its diverse biological activity, much of which remains inexplicable. The information reviewed here should point toward potential scope of future curcumin research in breast cancer.
    Matched MeSH terms: Curcumin/pharmacology; Curcumin/therapeutic use*
  6. Fulltext Rapid Green Synthesis and Characterization of Silver Nanoparticles Arbitrated by Curcumin in an Alkaline Medium
    Khan MJ, Shameli K, Sazili AQ, Selamat J, Kumari S
    Molecules, 2019 Feb 16;24(4).
    PMID: 30781541 DOI: 10.3390/molecules24040719
    Green synthesis of silver nanoparticles is desirable practice. It is not only the required technique for industrial and biomedical purposes but also a promising research area. The aim of this study was to synthesize green curcumin silver nanoparticles (C-Ag NPs). The synthesis of C-Ag NPs was achieved by reduction of the silver nitrate (AgNO₃) in an alkaline medium. The characterizations of the prepared samples were conducted by ultraviolet visible (UV-vis) spectroscopy, powder X-ray diffraction (PXRD), field emission scanning electron microscopy (FESEM), high-resolution transmission electron microscopy (HRTEM), selected area electron diffraction (SAED) and zeta potential (ZP) analyses. The formation of C-Ag NPs was evaluated by the dark color of the colloidal solutions and UV-vis spectra, with 445 nm as the maximum. The size of the crystalline nanoparticles, recorded as 12.6 ± 3.8nm, was confirmed by HRTEM, while the face-centered cubic (fcc) crystallographic structure was confirmed by PXRD and SAED. It is assumed that green synthesized curcumin silver nanoparticles (C-Ag NPs) can be efficiently utilized as a strong antimicrobial substance for food and meat preservation due to their homogeneous nature and small size.
    Matched MeSH terms: Curcumin/administration & dosage*; Curcumin/chemistry
  7. Fulltext A review on antibacterial, antiviral, and antifungal activity of curcumin
    Moghadamtousi SZ, Kadir HA, Hassandarvish P, Tajik H, Abubakar S, Zandi K
    Biomed Res Int, 2014;2014:186864.
    PMID: 24877064 DOI: 10.1155/2014/186864
    Curcuma longa L. (Zingiberaceae family) and its polyphenolic compound curcumin have been subjected to a variety of antimicrobial investigations due to extensive traditional uses and low side effects. Antimicrobial activities for curcumin and rhizome extract of C. longa against different bacteria, viruses, fungi, and parasites have been reported. The promising results for antimicrobial activity of curcumin made it a good candidate to enhance the inhibitory effect of existing antimicrobial agents through synergism. Indeed, different investigations have been done to increase the antimicrobial activity of curcumin, including synthesis of different chemical derivatives to increase its water solubility as well ass cell up take of curcumin. This review aims to summarize previous antimicrobial studies of curcumin towards its application in the future studies as a natural antimicrobial agent.
    Matched MeSH terms: Curcumin/analogs & derivatives; Curcumin/pharmacology*
  8. Solubility of core materials in aqueous polymeric solution effect on microencapsulation of curcumin
    Aziz HA, Peh KK, Tan YT
    Drug Dev Ind Pharm, 2007 Nov;33(11):1263-72.
    PMID: 18058323
    Curcumin, the main active constituent of turmeric herb (Curcuma longa L.) have been reported to possess many medicinal values. The application of curcumin in dermatological preparations is limited by their intense yellow color property, which stains the fabric and skin. The objectives of this study were to reduce the color staining effect and enhance the stability of curcumin via microencapsulation using gelatin simple coacervation method. As for curcumin, ethanol and acetone were used as coacervating solvents. Curcumin was dispersed in ethanol while dissolved in acetone. Irrespective of the types of coacervating solvents used, microencapsulation resolved the color-staining problem and enhanced the flow properties and photo-stability of curcumin. Nevertheless, it was found that more spherical curcumin microcapsules with higher yield, higher curcumin loading, and higher entrapment efficiency were obtained with acetone than ethanol. The in vitro release of curcumin after microencapsulation was slightly prolonged. Further evaluation of the effects of solubility of core materials in coacervating solvent or polymeric aqueous solution using six different drug compounds, namely, ketoconazole, ketoprofen, magnesium stearate, pseudoephedrine HCl, diclofenac sodium, and paracetamol, suggested that the solubility of core materials in aqueous polymeric solution determined the successful formation of microcapsules. Microcapsules could only be formed if the core materials were not dissolved in the aqueous polymeric solution while the core materials could either be dissolved or dispersed in the coacervating solvent. In summary, microencapsulation not only circumvents the color-staining problem but also improved the stability and flowability of curcumin. The solubility of core material in aqueous polymeric solution plays a pivotal role in determining the successful formation of microcapsules.
    Matched MeSH terms: Curcumin/administration & dosage*; Curcumin/chemistry*
  9. Fulltext Curcuma longa rhizome extract and Curcumin reduce the adhesion of Acanthamoeba triangularis trophozoites and cysts in polystyrene plastic surface and contact lens
    Mitsuwan W, Sangkanu S, Romyasamit C, Kaewjai C, Jimoh TO, de Lourdes Pereira M, et al.
    Int J Parasitol Drugs Drug Resist, 2020 12;14:218-229.
    PMID: 33238231 DOI: 10.1016/j.ijpddr.2020.11.001
    Curcuma longa and Curcumin have been documented to have a wide spectrum of pharmacological effects, including anti-Acanthamoeba activity. Hence, this study sought to explore the anti-adhesion activity of C. longa extract and Curcumin against Acanthamoeba triangularis trophozoites and cysts in plastic and contact lenses. Our results showed that C. longa extract and Curcumin significantly inhibited the adhesion of A. triangularis trophozoites and cysts to the plastic surface, as investigated by the crystal violet assay (P Curcumin at 1/2 × MIC, compared to the control. In the contact lens model, approximately 1 log cells/mL of the trophozoites and cysts was reduced when the cells were treated with Curcumin, when compared to the control. Pre-treatment of the plastic surface with Curcumin at 1/2-MIC reduced 60% and 90% of the adhesion of trophozoites and cysts, respectively. The reduction in 1 Log cells/mL of the adhesion of A. triangularis trophozoites was observed when lenses were pre-treated with both the extract and Curcumin. Base on the results obtained from this study, A. triangularis trophozoites treated with C. longa extract and Curcumin have lost strong acanthopodia, thorn-like projection pseudopodia observed by scanning electron microscope. This study also revealed the therapeutic potentials of C. longa extract and Curcumin, as such, have promising anti-adhesive potential that can be used in the management/prevention of A. triangularis adhesion to contact lenses.
    Matched MeSH terms: Curcumin*
  10. Curcumin in a model skin lotion formulation
    Suhaimi H, Ahmad FB, Friberg SE
    J Pharm Sci, 1995 Mar;84(3):376-80.
    PMID: 7616381
    A lamellar liquid crystalline region was identified in a typical skin lotion formulation system composed of a mixture of isostearic acid and triethanolamine (TEA) at 65:35 (w/w), decane, and water (the temperature was controlled at 30 degrees C). The interlayer spacings were determined by a small-angle X-ray diffraction technique. Incorporation of a natural dye, curcumin, resulted in lower interlayer spacings and higher penetration of water into the layered structure. However, the higher penetration of water was not apparent at all compositions of isostearic acid:TEA, decane, and water.
    Matched MeSH terms: Curcumin/chemistry*
  11. Selective antibacterial activities and storage stability of curcumin-loaded nanoliposomes prepared from bovine milk phospholipid and cholesterol
    Wu Y, Wang K, Liu Q, Liu X, Mou B, Lai OM, et al.
    Food Chem, 2022 Jan 15;367:130700.
    PMID: 34352694 DOI: 10.1016/j.foodchem.2021.130700
    Present study prepared curcumin-loaded nanoliposomes using bovine milk, krill phospholipids and cholesterol; and investigated the effects of cholesterol on membrane characteristics, storage stability and antibacterial properties of the curcumin nanoliposomes. Bovine milk phospholipids which have higher saturation than krill phospholipids resulted in formation of curcumin-loaded nanoliposomes with higher encapsulation efficiency (84.78%), larger absolute value of zeta potential and vesicle size (size: 159.15 ± 5.27 nm, zeta potential: -28.3 ± 0.62 mV). Cholesterol helps to formation of a more hydrophobic, compact and tighter bilayer membrane structure which improved the storage stability of nanoliposomes under alkaline (66.25 ± 0.46%), heat (43.25 ± 0.69%) and sunlight (49.44 ± 1.78%) conditions. In addition, curcumin-loaded nanoliposomes can effectively target infectious bacteria which secrete pore-forming toxins such as Staphylococcus aureus by causing the bacterial cell wall to lysis. Findings from present work can guide future development of novel antibacterial agents for use in food preservation.
    Matched MeSH terms: Curcumin*
  12. An Evaluation of Curcumin-Encapsulated Chitosan Nanoparticles for Transdermal Delivery
    Nair RS, Morris A, Billa N, Leong CO
    AAPS PharmSciTech, 2019 Jan 10;20(2):69.
    PMID: 30631984 DOI: 10.1208/s12249-018-1279-6
    Curcumin-loaded chitosan nanoparticles were synthesised and evaluated in vitro for enhanced transdermal delivery. Zetasizer® characterisation of three different formulations of curcumin nanoparticles (Cu-NPs) showed the size ranged from 167.3 ± 3.8 nm to 251.5 ± 5.8 nm, the polydispersity index (PDI) values were between 0.26 and 0.46 and the zeta potential values were positive (+ 18.1 to + 20.2 mV). Scanning electron microscopy (SEM) images supported this size data and confirmed the spherical shape of the nanoparticles. All the formulations showed excellent entrapment efficiency above 80%. FTIR results demonstrate the interaction between chitosan and sodium tripolyphosphate (TPP) and confirm the presence of curcumin in the nanoparticle. Differential scanning calorimetry (DSC) studies of Cu-NPs indicate the presence of curcumin in a disordered crystalline or amorphous state, suggesting the interaction between the drug and the polymer. Drug release studies showed an improved drug release at pH 5.0 than in pH 7.4 and followed a zero order kinetics. The in vitro permeation studies through Strat-M® membrane demonstrated an enhanced permeation of Cu-NPs compared to aqueous curcumin solution (p ˂ 0.05) having a flux of 0.54 ± 0.03 μg cm-2 h-1 and 0.44 ± 0.03 μg cm-2 h-1 corresponding to formulations 5:1 and 3:1, respectively. The cytotoxicity assay on human keratinocyte (HaCat) cells showed enhanced percentage cell viability of Cu-NPs compared to curcumin solution. Cu-NPs developed in this study exhibit superior drug release and enhanced transdermal permeation of curcumin and superior percentage cell viability. Further ex vivo and in vivo evaluations will be conducted to support these findings.
    Matched MeSH terms: Curcumin/administration & dosage*; Curcumin/pharmacology; Curcumin/chemistry
  13. Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats
    Satyavert, Gupta S, Choudhury H, Jacob S, Nair AB, Dhanawat M, et al.
    Pharmacol Rep, 2021 Dec;73(6):1734-1743.
    PMID: 34283375 DOI: 10.1007/s43440-021-00312-5
    BACKGROUND: Curcumin, a natural polyphenol from Curcuma longa, is known to possess diversified pharmacological roles including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic properties; however, its bioavailability is severely limited due to its poor solubility, poor absorption, rapid metabolism, and significant elimination. Hydrazinocurcumin (HZC), a novel analogue of curcumin has been reported to overcome the limitations of curcumin and also possesses multiple pharmacological activities. The present study aimed to evaluate the unexplored pharmacokinetic profile of this agent in experimental rats.

    METHODS: Drug formulations were administered to the experimental animals via oral, intravenous and intraperitoneal routes. Blood samples were collected at different pre-determined time intervals to determine the pharmacokinetic parameters. To understand the biodistribution profile of HCZ, tissue samples were isolated from different groups of Sprague-Dawley rats at different time points. The pharmacokinetic parameters of HZC were evaluated after administration through oral (100 mg/kg), intraperitoneal (100 mg/kg) and intravenous (10 mg/kg) routes.

    RESULTS: Significantly (p 

    Matched MeSH terms: Curcumin/administration & dosage; Curcumin/analogs & derivatives*; Curcumin/pharmacokinetics
  14. Fulltext Curcumin minimises histopathological and immunological progression in the ankle joints of collagen-induced arthritis rats
    Kevin, T.T.M., Nur Idanis, A.S., Anastasha, B., Mohd Faris, M.R., Faizah, O., Taty Anna, K.
    Medicine & Health, 2020;15(2):26-36.
    MyJurnal
    Curcumin adalah satu rempah tradisional yang mempunyai potensi untuk menyembuhkan pelbagai jenis penyakit inflamatori, termasuk artritis. Kajian ini dijalankan untuk memerhatikan kesan-kesan curcumin ke atas perubahan histopatologi dan aras interleukin-1β (IL-1β) di dalam artritis aruhan kolagen (CIA). Tiga puluh ekor tikus jantan Sprague-Dawley (150+50 g) dibahagikan kepada lima kumpulan secara rawak. Satu kumpulan dijadikan kumpulan kawalan normal (CTRL), manakala selebihnya disuntik dengan 150 μg emulsi kolagen secara subkutan pada hari 0. Kumpulan CTRL dan CIA-Curcumin-d0 masing-masing diberi suplimentasi harian minyak zaitun oil (1 ml/kg) dan curcumin (110 mg/ml/ kg) bermula pada hari 0. Kumpulan CIA-OV (kawalan negatif), CIA-Beta dan CIA-Curcumin-d14 pula, masing-masing diberi suplimentasi harian minyak zaitun (1 ml/kg), Betamethasone (0.5 mg/ml/kg), dan curcumin (110 mg/ml/kg) bermula pada hari 14. Suplimentasi harian tersebut diberi kepada tikus-tikus sehingga hari ke 42. Kajian ini menunjukkan bahawa kumpulan CIA-Beta (**P=0.00) dan CIA-Curcumin-d0 (**P=0.01) masing-masing mempamerkan purata skor histologi yang lebih rendah secara signifikan berbanding kumpulan CIA-OV. Aras IL-1β di dalam serum untuk kumpulan CIA-Beta dan CIA-Curcumin-d0 tidak meningkat secara signifikan pada hari ke 42 berbanding hari 0. Purata peningkatan aras IL-1β dari hari 0 ke hari 42 juga adalah rendah secara signifikan (**P≤0.01) untuk semua kumpulan CIA berbanding kumpulan CIA-OV. Tidak terdapat perbezaan yang signifikan dalan purata skor histologi dan aras IL-1β kumpulan of CIA-Curcumin-d0 berbanding kumpulan CIA-Beta. Kesimpulannya suplimentasi awal curcumin berpotensi untuk meminimakan perubahan yang disebabkan penyakit artritis aruhan kolagen pada tikus.
    Matched MeSH terms: Curcumin
  15. Fulltext Development and validation of a bioanalytical method for quantification of 2,6-bis-(4-hydroxy-3-methoxybenzylidene)-cyclohexanone (BHMC) in rat plasma
    Lee YZ, Ming-Tatt L, Lajis NH, Sulaiman MR, Israf DA, Tham CL
    Molecules, 2012 Dec 07;17(12):14555-64.
    PMID: 23222902 DOI: 10.3390/molecules171214555
    A sensitive and accurate high performance liquid chromatography with ultraviolet/visible light detection (HPLC-UV/VIS) method for the quantification of 2,6-bis-(4-hydroxy-3-methoxybenzylidene)-cyclohexanone (BHMC) in rat plasma was developed and validated. BHMC and the internal standard, harmaline, were extracted from plasma samples by a simple liquid-liquid extraction using 95% ethyl acetate and 5% methanol. Plasma concentration of BHMC and internal standard were analyzed by reversed phase chromatography using a C₁₈ column (150 × 4.6 mm I.D., particle size 5 µm) and elution with a gradient mobile phase of water and methanol at a flow rate of 1.0 mL/min. Detection of BHMC and internal standard was done at a wavelength of 380 nm. The limit of quantification was 0.02 µg/mL. The calibration curves was linear (R² > 0.999) over the concentration range of 0.02-2.5 µg/mL. Intra- and inter-day precision were less than 2% coefficient of variation. The validated method was then applied to a pharmacokinetic study in rats by intravenous administration of BHMC at a single dose of 10 mg/kg. Pharmacokinetic parameters such as half-life, maximum plasma concentration, volume of distribution, clearance and elimination rate constant for BHMC were calculated.
    Matched MeSH terms: Curcumin/analogs & derivatives*; Curcumin/isolation & purification; Curcumin/pharmacokinetics
  16. Fulltext Crystal structures of 3,5-bis-[(E)-3-hy-droxy-benzyl-idene]-1-methyl-piperidin-4-one and 3,5-bis-[(E)-2-chloro-benzyl-idene]-1-methyl-piperidin-4-one
    Eryanti Y, Zamri A, Herlina T, Supratman U, Rosli MM, Fun HK
    Acta Crystallogr E Crystallogr Commun, 2015 Dec 01;71(Pt 12):1488-92.
    PMID: 26870411 DOI: 10.1107/S2056989015020976
    The title compounds, C20H19NO3, (1), and C20H17Cl2NO, (2), are the 3-hy-droxy-benzyl-idene and 2-chloro-benzyl-idene derivatives, respectively, of curcumin [systematic name: (1E,6E)-1,7-bis-(4-hy-droxy-3-meth-oxy-phen-yl)-1,6-hepta-diene-3,5-dione]. The dihedral angles between the benzene rings in each compound are 21.07 (6)° for (1) and 13.4 (3)° for (2). In both compounds, the piperidinone rings adopt a sofa confirmation and the methyl group attached to the N atom is in an equatorial position. In the crystal of (1), two pairs of O-H⋯N and O-H⋯O hydrogen bonds link the mol-ecules, forming chains along [10-1]. The chains are linked via C-H⋯O hydrogen bonds, forming undulating sheets parallel to the ac plane. In the crystal of (2), mol-ecules are linked by weak C-H⋯Cl hydrogen bonds, forming chains along the [204] direction. The chains are linked along the a-axis direction by π-π inter-actions [inter-centroid distance = 3.779 (4) Å]. For compound (2), the crystal studied was a non-merohedral twin with the refined ratio of the twin components being 0.116 (6):0.886 (6).
    Matched MeSH terms: Curcumin
  17. Fulltext DK1 Induces Apoptosis via Mitochondria-Dependent Signaling Pathway in Human Colon Carcinoma Cell Lines In Vitro
    Hussin Y, Aziz MNM, Che Rahim NF, Yeap SK, Mohamad NE, Masarudin MJ, et al.
    Int J Mol Sci, 2018 Apr 11;19(4).
    PMID: 29641445 DOI: 10.3390/ijms19041151
    Extensive research has been done in the search for innovative treatments against colon adenocarcinomas; however, the incidence rate of patients remains a major cause of cancer-related deaths in Malaysia. Natural bioactive compounds such as curcumin have been substantially studied as an alternative to anticancer drug therapies and have been surmised as a potent agent but, nevertheless, remain deficient due to its poor cellular uptake. Therefore, efforts now have shifted toward mimicking curcumin to synthesize novel compounds sharing similar effects. A synthetic analog, (Z)-3-hydroxy-1-(2-hydroxyphenyl)-3-phenylprop-2-ene-1-one (DK1), was recently synthesized and reported to confer improved bioavailability and selectivity toward human breast cancer cells. This study, therefore, aims to assess the anticancer mechanism of DK1 in relation to the induction of in vitro cell death in selected human colon cancer cell lines. Using the3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay, the cytotoxicity of DK1 towards HT29 and SW620 cell lines were investigated. Acridine orange/propidium iodide (AO/PI) dual-staining assay and flow cytometry analyses (cell cycle analysis, Annexin/V-FITC and JC-1 assays) were incorporated to determine the mode of cell death. To further determine the mechanism of cell death, quantitative real-time polymerase chain reaction (qRT-PCR) and proteome profiling were conducted. Results from this study suggest that DK1 induced changes in cell morphology, leading to a decrease in cell viability and subsequent induction of apoptosis. DK1 treatment inhibited cell viability and proliferation 48 h post treatment with IC50 values of 7.5 ± 1.6 µM for HT29 cells and 14.5 ± 4.3 µM for SW620 cells, causing cell cycle arrest with increased accumulation of cell populations at the sub-G₀/G₁phaseof 74% and 23%, respectively. Flow cytometry analyses showed that DK1 treatment in cancer cells induced apoptosis, as indicated by DNA fragmentation and depolarization of the mitochondrial membrane. qRT-PCR results show significant upregulation in the expression of caspase-9 in both HT29 and SW620 cell lines, further supporting that cell death induction by DK1 is via an intrinsic pathway. These outcomes, therefore, demonstrate DK1 as a potential anticancer agent for colon adenocarcinoma due to its anti-apoptotic attributes.
    Matched MeSH terms: Curcumin/analogs & derivatives*; Curcumin/chemical synthesis; Curcumin/pharmacology*; Curcumin/chemistry
  18. Antioxidative constituents of Etlingera elatior
    Mohamad H, Lajis NH, Abas F, Ali AM, Sukari MA, Kikuzaki H, et al.
    J Nat Prod, 2005 Feb;68(2):285-8.
    PMID: 15730265
    Phytochemical studies on the rhizomes of Etlingera elatior have resulted in the isolation of 1,7-bis(4-hydroxyphenyl)-2,4,6-heptatrienone (1), demethoxycurcumin (2), 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (3), 16-hydroxylabda-8(17),11,13-trien-15,16-olide (4), stigmast-4-en-3-one, stigmast-4-ene-3,6-dione, stigmast-4-en-6beta-ol-3-one, and 5alpha,8alpha-epidioxyergosta-6,22-dien-3beta-ol. Compounds 1 and 4 are new, and their structures were elucidated by analysis of spectroscopic data. Diarylheptanoids 1-3 were found to inhibit lipid peroxidation in a more potent manner than alpha-tocopherol.
    Matched MeSH terms: Curcumin/analogs & derivatives*; Curcumin/isolation & purification; Curcumin/pharmacology; Curcumin/chemistry
  19. Hydrophobic kenaf nanocrystalline cellulose for the binding of curcumin
    Zainuddin N, Ahmad I, Kargarzadeh H, Ramli S
    Carbohydr Polym, 2017 May 01;163:261-269.
    PMID: 28267505 DOI: 10.1016/j.carbpol.2017.01.036
    Nanocrystalline cellulose (NCC) extracted from lignocellulosic materials has been actively investigated as a drug delivery excipients due to its large surface area, high aspect ratio, and biodegradability. In this study, the hydrophobically modified NCC was used as a drug delivery excipient of hydrophobic drug curcumin. The modification of NCC with a cationic surfactant, cetyl trimethylammonium bromide (CTAB) was used to modulate the loading of hydrophobic drugs that would not normally bind to NCC. The FTIR, Elemental analysis, XRD, TGA, and TEM were used to confirm the modification of NCC with CTAB. The effect of concentration of CTAB on the binding efficiency of hydrophobic drug curcumin was investigated. The amounts of curcumin bound onto the CTAB-NCC nanoparticles were analyzed by UV-vis Spectrophotometric. The result showed that the modified CTAB-NCC bound a significant amount of curcumin, in a range from 80% to 96% curcumin added. Nevertheless, at higher concentration of CTAB resulted in lower binding efficiency.
    Matched MeSH terms: Curcumin/chemistry*
  20. Modulation of implants PEEK to composite resin shear bond strength and surface roughness on pre-treatment with contemporary air abrasion techniques vs photodynamic therapy vs conventional diamond grit bur
    Qamar Z, Zeeshan T, Alqahtani WMS, Alanazi A, Khalid Aqeel Almejlad N, Ahmed Khan T, et al.
    Photodiagnosis Photodyn Ther, 2023 Sep;43:103689.
    PMID: 37414110 DOI: 10.1016/j.pdpdt.2023.103689
    AIM: The chief aim of the study was to determine/equate the surface roughness (SRa) and shear bond strength (BS) of pretreated PEEK discs with contemporary air abrasion techniques, photodynamic (PD) therapy by curcumin photosensitizer (PS) and conventional diamond grit straight fissure bur adhered to the composite resin discs.

    MATERIAL AND METHOD: Two hundred discs of PEEK were prepared of 6 mm × 2 mm × 10 mm dimension. The discs were randomly divided into five groups (n = 40) for treatment, Group I: treatment with deionized distilled water (control group); Group II: PD therapy using curcumin PS; Group III: discs treated and abraded with air-borne particles (ABP) silica (30 μm particle size) modified alumina (Al); Group IV: ABP of alumina (110 μm particle size); and Group V: The PEEK were finished with 600-μm grit size straight diamond cutting bur installed in high speed hand-piece. The surface profilometer was used to evaluate the values of surface roughness (SRa) of pretreated PEEK discs. The discs were luted and bonded to discs of composite resin. The bonded PEEK samples were placed in Universal testing machine to evaluate shear BS. The type of BS failure for PEEK discs pre-treated with five regimes respectively was evaluated under stereo-microscope. The data was statistically analyzed using one-way ANOVA and the comparisons between mean values of shear BS were evaluated by Tukey's test (ρ≤0.05).

    RESULTS: The PEEK samples pre-treated with diamond cutting straight fissure burs displayed statistically significant highest value of SRa values (3.258± 0.785 µm). Similarly, the shear BS was observed to be higher for the PEEK discs pre-treated with straight fissure bur (22.37±0.78 MPa). A comparable difference but not statistically significant difference was observed between PEEK discs pre-treated by curcumin PS and ABP-silica modified alumina (ρ ≥ 0.05).

    CONCLUSION: PEEK discs pre-treated with diamond grit straight fissure bur displayed highest values of SRa and shear BS. It was trailed by ABP-Al pre-treated discs; whereas the SRa and shear BS values for the discs pre-treated with ABP-silica modified Al and curcumin PS did not show competitive difference.

    Matched MeSH terms: Curcumin*
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