Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice

Meena, Chhuttan Lal; Thakur, Avinash; Nandekar, Prajwal P.; Sangamwar, Abhay T.; Sharma, Shyam Sundar; Jain, Rahul

doi:10.1016/j.bmc.2015.07.022

Cited by 15 publications

(8 citation statements)

References 36 publications

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“…Stroke is a neurological condition that occurs due to sudden reduction or loss of blood supply to an area of the brain leading to the death of neurons and, ultimately, loss of neurological functions. It is the third leading cause of death in the developed countries and may cause deficits, including paralysis, problems with memory, language, and movement [ 10 , 73 ]. Depending on the underlying pathology, stroke can be classified as either ischaemic stroke caused due to lack of blood flow or haemorrhagic stroke resulting from bleeding [ 10 , 74 ].…”

Section: Therapeutic Potential Of Cape In Strokementioning

confidence: 99%

Neuroprotective Potential of Caffeic Acid Phenethyl Ester (CAPE) in CNS Disorders: Mechanistic and Therapeutic Insights

Kulkarni

Vaidya

Narula

et al. 2021

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: Neurological disorders like Alzheimer’s disease (AD), Parkinson’s disease (PD), stroke, amyotrophic lateral sclerosis, Huntington’s disease (HD), epilepsy, traumatic brain injury (TBI), depression and anxiety are responsible for thousands of deaths worldwide every year. With the increase in life expectancy, there has been a rise in the prevalence of these disorders. Age is one of the major risk factors for these neurological disorders and with the aged population is set to rise to 1.25 billion by 2050. There is a growing concern to look for new therapeutic molecules to treat age-related diseases. Caffeic acid phenethyl ester (CAPE) is a molecule obtained from a number of botanical sources such as the bark of conifer trees as well as propolis which is extracted from beehives. Though CAPE remains relatively unexplored in human trials, it possesses antioxidant, anti-inflammatory, antimitogenic and anti-cancer activities as shown by preclinical studies. Apart from this, it also exhibits tremendous potential for the treatment of neurological disorders through modulation of multiple molecular pathways and attenuation of behavioural deficits. In the present article, we have reviewed the therapeutic potential of CAPE and its mechanisms in the treatment of neurological disorders.

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Section: Therapeutic Potential Of Cape In Strokementioning

confidence: 99%

Neuroprotective Potential of Caffeic Acid Phenethyl Ester (CAPE) in CNS Disorders: Mechanistic and Therapeutic Insights

Kulkarni

Vaidya

Narula

et al. 2021

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“…Among them, only taltirelin hydrate (CEREDIST), which is an agonist at the human TRH-R has been launched in Japan as an orally effective agent for treatment of SCD (Figure ). ,, After 2000, new types of TRH analogues such as NP-647, which binds to TRH-R subtype selectively and has only CNS effects or prodrugs for brain targeting, were found and evaluated.…”

Section: Introductionmentioning

confidence: 99%

Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1-{N-[(4S,5S)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate)

et al. 2018

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We have explored orally effective thyrotropin-releasing hormone (TRH) mimetics, showing oral bioavailability and brain penetration by structure–activity relationship (SAR) study on the basis of in vivo antagonistic activity on reserpine-induced hypothermia in mice. By primary screening of the synthesized TRH mimetics, we found a novel TRH mimetic: l-pyroglutamyl-[3-(thiazol-4-yl)-l-alanyl]-l-prolinamide with a high central nervous system effect compared with TRH as a lead compound. Further SAR optimization studies of this lead compound led to discovery of a novel orally effective TRH mimetic: 1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine trihydrate (rovatirelin hydrate), which was selected as a candidate for clinical trials.

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“…1,2 Conventionally, nanoparticles of sizes ranging to as low as several nanometers are often produced as byproducts of anthropogenic activities, such as simple combustion, chemical manufacturing, welding, smelting, vehicular combustion, airplane engines, and ore refining. 3 TiO 2 nanoparticles are widely used because of their unique properties in various biological and allied domains, such as medicine, drug delivery, transfection vectors, food industry, and fluorescent labels. 4 It has been known from long that mitochondria acts as a powerhouse of the cell.…”

Section: ■ Introductionmentioning

confidence: 99%

“…The rapid breakthrough in nanoscience research has resulted in growth in the manufacture and usage of nanoparticles, which are less than 100 nm in dimension. , Conventionally, nanoparticles of sizes ranging to as low as several nanometers are often produced as byproducts of anthropogenic activities, such as simple combustion, chemical manufacturing, welding, smelting, vehicular combustion, airplane engines, and ore refining . TiO 2 nanoparticles are widely used because of their unique properties in various biological and allied domains, such as medicine, drug delivery, transfection vectors, food industry, and fluorescent labels .…”

Section: Introductionmentioning

confidence: 99%

Modulatory Role of Quercetin in Mitochondrial Dysfunction in Titanium Dioxide Nanoparticle-Induced Hepatotoxicity

et al. 2022

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Background: Titanium dioxide (TiO 2 ) nanoparticles are among the largely manmade nanomaterials worldwide and are broadly used as both industrial and user products. The primary target site for several nanoparticles is the liver, including TiO 2 nanoparticles (TNPs), exposed directly or indirectly through ingestion of contaminated water, food, or animals and elevated environmental contamination. Oxidative stress is a known facet of nanoparticle-induced toxicity, including TNPs. Mitochondria are potential targets for nanoparticles in several types of toxicity, such as hepatotoxicity. Nevertheless, its causal mechanism is still controversial due to scarcity of literature linking the role of mitochondria-mediated TNP-induced hepatotoxicity. Aim: The objective of the current study was to evaluate the relation of mitochondrial oxidative stress and respiratory chain mechanisms with TNPinduced mitochondrial dysfunction in vitro, and explore the hepatoprotective effect of quercetin (QR), which is a polyphenolic flavonoid abundant in fruits and vegetables with known antioxidant properties, on TNP-induced mitochondrial oxidative stress and disturbance in respiratory chain complex enzymes in the liver of rats. Results: Enzymatic and non-enzymatic antioxidant levels, oxidative stress markers, and mitochondrial complexes were assessed with regard to TNP-induced hepatotoxicity. The depleted lipid peroxidation levels and protein carbonyl content, in mitochondria, induced by TNPs were restored significantly by pretreatment with QR. QR modulated the altered non-enzymatic and enzymatic antioxidants and mitochondrial complex enzymes. Conclusion: Based on the findings, we conclude that QR, which mitigates oxidative stress caused by mitochondrial dysfunction, holds promising capability to potentially diminish TNP-induced adverse effects in the liver.

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Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice

Cited by 15 publications

References 36 publications

Neuroprotective Potential of Caffeic Acid Phenethyl Ester (CAPE) in CNS Disorders: Mechanistic and Therapeutic Insights

Neuroprotective Potential of Caffeic Acid Phenethyl Ester (CAPE) in CNS Disorders: Mechanistic and Therapeutic Insights

Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1-{N-[(4S,5S)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate)

Modulatory Role of Quercetin in Mitochondrial Dysfunction in Titanium Dioxide Nanoparticle-Induced Hepatotoxicity

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