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Biobased Products for Viral Diseases
Published in Mahendra Rai, Chistiane M. Feitosa, Eco-Friendly Biobased Products Used in Microbial Diseases, 2022
Gleice Ribeiro Orasmo, Giovanna Morghanna Barbosa do Nascimento, Maria Gabrielly de Alcântara Oliveira, Jéssica Missilany da Costa
Curcumin is the main curcuminoid obtained from the rhizomes of turmeric (Curcuma longa L.) (Patwardhan et al. 2020). In order to determine and compare the values for heat sensitization of hepatitis A virus and tulane virus, Patwardhan et al. (2020) used grape seed extract, gingerol (from ginger) and curcumin, which are foods ‘generally recognized as safe’ (GRA), which have anti-inflammatory, immunomodulatory and antiviral properties. The results suggest that GRA substances may help to inactivate hepatitis A virus and tulane virus.
Fenugreek
Published in Dilip Ghosh, Prasad Thakurdesai, Fenugreek, 2022
Ujjwala Kandekar, Sunil Ramdasi, Prasad Thakurdesai
When administered by the oral route, the drug needs to be solubilized and absorbed, and bioavailable to exert the pharmacological action. Curcuminoids, the bioactive constituents of turmeric (Curcuma longa L.) have many medicinal applications. However, poor solubility and permeability limit the oral bioavailability of curcuminoids and become a major for obstacle optimum usage (Anand et al. 2007; Lopresti 2018). Many approaches have been explored to enhance the solubility (Aditya et al. 2015; Kumar, Kesharwani et al. 2016; Li et al. 2016; Mohammadian et al. 2019; Peng et al. 2018; Rezaei and Nasirpour 2018; Sarika et al. 2015), but systemic oral bioavailability of unconjugated curcuminoids remains a challenge (Olotu et al. 2020; Sanidad et al. 2019). A water dispersible formulation of curcuminoids with fenugreek galactomannans (‘curcumagalactomannosides’ (CGM)) has reported improved blood-brain barrier permeability and tissue distribution of free curcuminoids following its oral administration to rats (Krishnakumar et al. 2015). A subsequent double-blind randomized controlled crossover study in 50 healthy volunteers demonstrated high relative bioavailability (45.5 fold) and pharmacokinetics of free curcuminoids, when formulated with fenugreek dietary fiber as CGM, when compared to unformulated standard curcumin (Kumar, Jacob et al. 2016). These results were attributed to the strong interaction of curcumin with mucoadhesive fenugreek galactomannans to generate sub-micronized colloidal particles of CGM complexes that were resistant to the enzymatic biotransformation (Kumar, Jacob et al. 2016).
Recent Advancements of Curcumin Analogs and Curcumin Formulations in Context to Modern Pharmacotherapeutics Perspectives
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Animeshchandra G. M. Haldar, Kanhaiya M. Dadure, Debarshi Kar Mahapatra
Zheng et al.42 synthesized five series of curcuminoids and evaluated their antioxidant activity in vitro. The compounds with pyrazoline ring containing N1 thiocarbamoyl substituent resulted in the highest antioxidant properties among the synthesized compounds with inhibition percentage of 84.52 and 88.17%. This also resulted that electron-donating groups were necessary for enhancing the free radical scavenging properties; especially the phenolic hydroxyl group is a necessary component.
Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Xinyi Qiao, Lei Ye, Jialin Lu, Chengshuang Pan, Qianjin Fei, Yang Zhu, Huitao Li, Han Lin, Ren-shan Ge, Yiyan Wang
In Asia and Africa, Curcuma (turmeric), the rhizome of the perennial herb Curcuma longa L., is widely used as functional food additive to humans and animals. Since the last century, the main bioactive component of turmeric has been identified as curcuminoids. The major component of curcuminoids is curcumin (Figure 1(A)), a beta-diketone polyphenol that is methane in which two of the hydrogens are substituted by feruloyl groups. Curcuminoids isolated from turmeric usually contain 65% curcumin (CUR) and 35% de-methoxylated curcumin: 25% demethoxycurcumin (DMC) that has one de-methoxylated group in one of benzene rings and 10% bisdemethoxycurcumin (BDMC) that has two de-methoxylated groups in two benzene rings (Figure 1(A))1. CUR in plants and animals can be metabolised into dihydrocurcumin (DHC) after one of the double bonds is reduced, or tetrahydrocurcumin (THC) after two double bonds are reduced by gut microbiota, and octahydrocurcumin (OHC) after all double bonds in the bridge moiety are reduced. Curcuminoids have been found to have anti-inflammatory, anti-oxidative, anti-malarial, anti-septic, anti-tumour, analgesic, and anti-virus COVID-19 activity2–6. DMC retains some of the beneficial properties of curcumin, including its antioxidant and anti-inflammatory effects7. BDMC has been reported to have anticancer effects in several cancer cell lines and animal models8.
Brain regional pharmacokinetics following the oral administration of curcumagalactomannosides and its relation to cognitive function
Published in Nutritional Neuroscience, 2022
Ramalingam G. Kannan, Maliakal B. Abhilash, Kumar Dinesh, Das S. Syam, Maliakel Balu, Ittiyavirah Sibi, I. M. Krishnakumar
Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is the bioactive polyphenol found in the rhizomes of Curcuma longa (turmeric) and other species of Curcuma. When isolated by solvent extraction, it is mainly obtained as a mixture consisting of curcumin (70–80%), demethoxycurcumin (DMC, 12–15%) and bisdemethoxycurcumin (BDMC, 2–5%), commonly referred to as curcuminoids or curcumin (Figure 1) [1]. A number of in vitro and in vivo studies have demonstrated the antioxidant, anti-inflammatory, antimutagenic, antimicrobial, gastroprotective, neuroprotective and anti-proliferative properties of curcuminoids and its unique multi-targeted mechanism of action [2]. The anti-neuroinflammatory effects and the ability of curcumin to stimulate neurogenesis, synaptogenesis and migration in brain derived adult neural stem cells have indicated its plausible efficacy in hippocampus dysfunction mediated by conditions of stroke, trauma, radiation and neurodegenerative diseases [3,4]. However, oral administration of curcumin was reported to provide only a negligible impact in clinical trials on diseases such as Alzheimer’s and cancer [5,6].
The effects of oral administration of curcumin–galactomannan complex on brain waves are consistent with brain penetration: a randomized, double-blinded, placebo-controlled pilot study
Published in Nutritional Neuroscience, 2022
Aman Khanna, Syam Das S, R. Kannan, Andrew G. Swick, Cristina Matthewman, Balu Maliakel, Sibi P. Ittiyavirah, I. M. Krishnakumar
Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione], the yellow pigment and the active principle of turmeric (Curcuma longa), has been shown to possess a multitude of health beneficial pharmacological effects comprising antioxidant, anti-inflammatory, anti-microbial, anti-cancer, antidiabetic, anti-allergic, hepatoprotective, gastroprotective, cardioprotective, radioprotective, immunomodulatory, neuroprotective and anti-dermatophyte properties mediating through a pleotropic mechanism of action involving many proteins, transcription factors and genes [1,2]. However, the poor pharmacokinetics and hence poor tissue distribution has been largely shown to compromise its therapeutic potential [3–5]. Low intestinal absorption of curcuminoids owing to its hydrophobicity and rapid biotransformation into impermeable and weak metabolites like glucuronides and sulphates have been regarded as the major reasons for its poor oral bioavailability and hence clinical efficacy [4–6].