Curcumin as a privileged scaffold molecule for various biological targets in drug development

Mir, Reyaz Hassan; Mohi-ud-din, Roohi; Mir, Prince Ahad; Shah, Abdul Jalil; Banday, Nazia; Sabreen, Saba; Maqbool, Mudasir; Jan, Rafia; Shafi, Nyira; Masoodi, Mubashir Hussain

doi:10.1016/b978-0-323-91097-2.00010-8

Cited by 11 publications

(4 citation statements)

References 173 publications

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“…Curcuminoids possess diverse pharmacological properties, including but not limited to anti-inflammatory, anti-angiogenic, antioxidant, anticancer, and immunomodulating actions [13]. Curcumin, the principal constituent of curcuminoids, exhibits remarkable therapeutic potential owing to its pleiotropic characteristics, which facilitate its efficacious targeting of a multitude of molecules implicated in various pathological states [14][15][16]. PC was shown to exert anti-inflammatory and antioxidant properties, as was extensively documented previously [17,18].…”

Section: Introductionmentioning

confidence: 74%

Comparative Study of the Effects of Curcuminoids and Tetrahydrocurcuminoids on Melanogenesis: Role of the Methoxy Groups

Goenka

2024

Future Pharmacology

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Curcuminoids are naturally occurring yellow-colored compounds that, when hydrogenated to remove their conjugated double bond, become colorless and are referred to as tetrahydrocurcuminoids. Curcuminoids consist of pure curcumin (PC) in major amounts and demethoxycurcumin (DC) and bisdemethoxycurcumin (BDC) in minor amounts. Tetrahydrocurcuminoids similarly consist mainly of tetrahydrocurcumin (THC), along with minor amounts of tetrahydrodemethoxycurcumin (THDC) and tetrahydrobisdemethoxycurcumin (THBDC). Previous studies have shown the inhibitory effects of PC, DC, and BDC on melanin production, but there are contradictory findings about THC. In addition, there are currently no reports on the effects of THDC and THBDC on melanogenesis. Our previous report described that, in contrast to PC, which suppressed melanin production, THC stimulated melanin production in B16F10 and MNT-1 cells; this effect was ascribed to the loss of the conjugated heptadiene moiety of PC. However, whether this finding can be generalized to the two curcumin derivatives (DC and BDC), such that THDC and THBDC might also stimulate melanogenesis, has not been addressed. Herein, a comparative study of six curcumin derivatives (PC, DC, BDC, THC, THDC, and THBDC) was undertaken to identify their effects on melanogenesis with the goal of elucidating the structure–activity relationships (SARs) focused on assessing the two regions of the parent curcumins’ structure: (i) the hydrogenation of the two double bonds bridging the phenyl rings to the β-diketone moiety, and (ii) the effect of the ortho-methoxy substituent (-OCH3) on the two phenyl rings. To determine the direct effects of the six compounds, antioxidant activity and tyrosinase activity were assessed in cell-free systems before cellular experiments utilizing the B16F10 mouse melanoma cells, MNT-1 human melanoma cells, and primary cells. Evaluations were made on cytotoxicity, melanin concentration, and cellular tyrosinase activity. The results showed that BDC inhibited melanogenesis in B16F10 and MNT-1 cells. However, it was ineffective in primary human melanocytes, while THBDC continued to exhibit anti-melanogenic capacity in normal human melanocytes. Moreover, these findings provide a novel perspective into the role of the methoxy groups of PC on the biological effects of melanogenesis and also confirm that the removal of the conjugated double bonds abolishes the anti-melanogenic capacity of PC and DC only, but not BDC, as THBDC maintained anti-melanogenic activity that was greater than BDC. However, the outcome is contingent upon the specific kind of cell involved. To the best of our knowledge, this work presents novel findings indicating that the anti-melanogenic capacity of the colored BDC is not only intact but enhanced after its hydrogenation as observed in THBDC. The findings show potential for using colorless THBDC as a pharmacological candidate to diminish the increased pigmentation characteristic of skin hyperpigmentation disorders. Future pharmacological therapeutics that incorporate pure THBDC or THBDC-enriched extracts, which retain both a colorless appearance and potent anti-melanogenic activity, can be applied to compounds for anti-melanoma therapeutics where the demand for nontoxic novel molecules is desired for established efficacies.

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Section: Introductionmentioning

confidence: 74%

Comparative Study of the Effects of Curcuminoids and Tetrahydrocurcuminoids on Melanogenesis: Role of the Methoxy Groups

Goenka

2024

Future Pharmacology

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“… 105 , 106 Curcumin has anti-inflammatory, antitumor, wound healing, and antibacterial properties. 107 , 108 Amyloid plaques and inflammatory cytokines are both inhibited by curcumin, similar to the JNK-mediated pathway. 109 Curcumin (400 mg) was evaluated by Chin et al 109 in 60 persons aged 60–65 years for its acute and chronic effects on mood and cognition.…”

Section: Plant Materials and Derived Phytochemicals For Treatment Of Admentioning

confidence: 97%

“…Turmeric, known as “golden spice”, commonly used in Indian and Middle Eastern cooking style, contains a natural compound called curcumin. Similar to resveratrol, it has been investigated for possible advantages in treating a range of ailments, including AD. , Curcumin has anti-inflammatory, antitumor, wound healing, and antibacterial properties. , Amyloid plaques and inflammatory cytokines are both inhibited by curcumin, similar to the JNK-mediated pathway . Curcumin (400 mg) was evaluated by Chin et al in 60 persons aged 60–65 years for its acute and chronic effects on mood and cognition.…”

Section: Plant Materials and Derived Phytochemicals For Treatment Of Admentioning

confidence: 99%

Synthetic and Natural Bioactive Molecules in Balancing the Crosstalk among Common Signaling Pathways in Alzheimer’s Disease: Understanding the Neurotoxic Mechanisms for Therapeutic Intervention

Shah,

Mir,

Adnan

et al. 2023

ACS Omega

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The structure and function of the brain greatly rely on different signaling pathways. The wide variety of biological processes, including neurogenesis, axonal remodeling, the development and maintenance of pre- and postsynaptic terminals, and excitatory synaptic transmission, depends on combined actions of these molecular pathways. From that point of view, it is important to investigate signaling pathways and their crosstalk in order to better understand the formation of toxic proteins during neurodegeneration. With recent discoveries, it is established that the modulation of several pathological events in Alzheimer’s disease (AD) due to the mammalian target of rapamycin (mTOR), Wnt signaling, 5′-adenosine monophosphate activated protein kinase (AMPK), peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1α), and sirtuin 1 (Sirt1, silent mating-type information regulator 2 homologue 1) are central to the key findings. These include decreased amyloid formation and inflammation, mitochondrial dynamics control, and enhanced neural stability. This review intends to emphasize the importance of these signaling pathways, which collectively determine the fate of neurons in AD in several ways. This review will also focus on the role of novel synthetic and natural bioactive molecules in balancing the intricate crosstalk among different pathways in order to prolong the longevity of AD patients.

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“…TNF-α has been shown to mediate metabolic activities with high levels observed to be associated with diabetes mellitus type 2 and decreased muscle strength and muscle mass [8]. As one ages, in ammatory factors like TNF-α increase in the body, which contributes to the pathogenesis of common chronic diseases experienced by the elderly including Alzheimer's disease, heart-related diseases, in ammatory bowel disease, rheumatoid arthritis, and certain infections [9].…”

Section: Introductionmentioning

confidence: 99%

Association Between Handgrip Strength, TNF-αlpha Levels and the Presence of Chronic Diseases Among the Elderly

Ntiamoah,

Ananni-Akollor,

Frempong

et al. 2024

Preprint

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Background: There is a rapid surge in the elderly population globally and in Ghana. Ageing is frequently associated with the emergence of some chronic diseases due to a decline in physiological and physical functions. Early detection of chronic diseases or possible risk factors of disease development is critical in reducing mortality and morbidity among the elderly. This study, therefore, sought to explore the relationship between the inflammatory cytokine-tumour necrosis factor (TNF-α), handgrip strength and the presence of chronic diseases among the elderly population seeking medical care from a hospital in Ghana. Methods: This was a hospital-based cross-sectional study carried out among individuals 60 years or above. A total of 104 persons who met the inclusion criteria and consented were enrolled on the study. Handgrip strength was measured using a digital hand dynamometer and plasma TNF-α levels were determined using sandwich ELISA. Data on demographics and chronic disease conditions were collected from participants using a standardized questionnaire and from the participant’s hospital folder. Results: The study recruited 104 participants, of which 53% were females and 47% were males. The median age (median (IQR)) was 65 (62–71) years. Again, of the total participants, 63.5% had at least one chronic disease while 36.5% had no chronic disease. Whereas 12.5% of participants had low handgrip strength, 87.5% had normal hand grip strength. There was no significant association between disease status and low handgrip strength (p = 0.709). However, there was a significant association between disease status and increased plasma levels of TNF-α among participants of the study (p = 0.0435). There was also a significant association between low handgrip strength and increased plasma levels of TNF-α among participants of the study (p = 0.0001). Conclusion: In conclusion, the present study observed that low hand grip strength is significantly associated with high circulating TNF-α levels which is also associated with increased presence of chronic disease among the elderly. Low handgrip strength may not independently represent an increased risk of developing chronic diseases.

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Curcumin as a privileged scaffold molecule for various biological targets in drug development

Cited by 11 publications

References 173 publications

Comparative Study of the Effects of Curcuminoids and Tetrahydrocurcuminoids on Melanogenesis: Role of the Methoxy Groups

Comparative Study of the Effects of Curcuminoids and Tetrahydrocurcuminoids on Melanogenesis: Role of the Methoxy Groups

Synthetic and Natural Bioactive Molecules in Balancing the Crosstalk among Common Signaling Pathways in Alzheimer’s Disease: Understanding the Neurotoxic Mechanisms for Therapeutic Intervention

Association Between Handgrip Strength, TNF-αlpha Levels and the Presence of Chronic Diseases Among the Elderly

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