Adenosine signalling has long been a target for drug development, with adenosine itself or its derivatives being used clinically since the 1940s. In addition, methylxanthines such as caffeine have profound biological effects as antagonists at adenosine receptors. Moreover, drugs such as dipyridamole and methotrexate act by enhancing the activation of adenosine receptors. There is strong evidence that adenosine has a functional role in many diseases, and several pharmacological compounds specifically targeting individual adenosine receptors — either directly or indirectly — have now entered the clinic. However, only one adenosine receptor-specific agent — the adenosine A2A receptor agonist regadenoson (Lexiscan; Astellas Pharma) — has so far gained approval from the US Food and Drug Administration (FDA). Here, we focus on the biology of adenosine signalling to identify hurdles in the development of additional pharmacological compounds targeting adenosine receptors and discuss strategies to overcome these challenges.

/pdf/adenosine-receptors-as-drug-targets-what-are-the-challenges-25torexxs0.pdf

Adenosine receptors as drug targets — what are the challenges?

Neurodegenerative diseases affect not only the life quality of aging populations, but also their life spans. All forms of neurodegenerative diseases have a massive impact on the elderly. The major threat of these brain diseases includes progressive loss of memory, Alzheimer’s disease (AD), impairments in the movement, Parkinson’s disease (PD), and the inability to walk, talk, and think, Huntington’s disease (HD). Oxidative stress and mitochondrial dysfunction are highlighted as a central feature of brain degenerative diseases. Oxidative stress, a condition that occurs due to imbalance in oxidant and antioxidant status, has been known to play a vital role in the pathophysiology of neurodegenerative diseases including AD, PD, and HD. A large number of studies have utilized oxidative stress biomarkers to investigate the severity of these neurodegenerative diseases and medications are available, but these only treat the symptoms. In traditional medicine, a large number of medicinal plants have been used to treat the symptoms of these neurodegenerative diseases. Extensive studies scientifically validated the beneficial effect of natural products against neurodegenerative diseases using suitable animal models. This short review focuses the role of oxidative stress in the pathogenesis of AD, PD, and HD and the protective efficacy of natural products against these diseases.

/pdf/the-role-of-reactive-oxygen-species-in-the-pathogenesis-of-2zsq1lmx8x.pdf

The Role of Reactive Oxygen Species in the Pathogenesis of Alzheimer’s Disease, Parkinson’s Disease, and Huntington’s Disease: A Mini Review

Therapeutic orchids: traditional uses and recent advances--an overview.

Many of the epiphytic orchids are used as traditional medicine. Chemical components and pharmacology have been studied in recent 15 years. Medicinal orchids, in general, are not subjected to detailed pharmacological studies. A wide range of chemical compounds are presented including alkaloids, bibenzyl derivatives, flavonoids, phenanthrenes and terpenoids which have been isolated recently from this species. Extracts and metabolites of these plants, particularly those from flowers and leaves, possess useful pharmacological activities. Particular attention has been given to diuretic, anti-rheumatic, anti-inflammatory, anti-carcinogenic, hypoglycemic activities, antimicrobial, anticonvulsive, relaxation, neuroprotective, and antivirus, activities. A comprehensive account of chemical constituents and biological activities is presented and a critical appraisal of the ethnopharmacological issues is included in view of the many recent findings of importance of these orchids. A large number of orchids have been empirically used for treatment of different diseases, thus, several studies have been undertaken to provide scientific proof to justify the medicinal use of various plants in treatment of diseases. The aim of this review is to up-date and to present a comprehensive analysis of traditional and folklore uses, pharmacological reports and phyto-constituents isolated from the orchids family.

	 

	Key words: Orchids, medicinal plant, traditional uses, chemical constituents, biological activities.

https://www.academicjournals.org/article/article1380546355_Gutiérrez.pdf

Orchids : A review of uses in traditional medicine, its phytochemistry and pharmacology

The rhizome of Gastrodia elata Blume - An ethnopharmacological review.

Serum deprivation-induced neuronal-like PC12 cell apoptosis was used as an ischemic/hypoxic model to screen neuroprotective compounds from the rhizomes of Gastrodia elata, a traditional Chinese medicine. Two active compounds, bis(4-hydroxybenzyl)sulfide (1) and N6-(4-hydroxybenzyl)adenine riboside (2), together with 15 known compounds were obtained from the active fraction. Compound 2 was further elucidated by chemical synthesis. Compounds 1 and 2 potently prevented PC12 cell apoptosis in concentration-dependent manners with EC50 values of 7.20 microM and 3.7 x 10-8 M, respectively, and IC50 values of 42.90 microM (Ki 24.10 microM) and 4.660 microM (Ki 2.620 microM), respectively, in an adenosine A2A receptor binding assay.

Neuroprotective Principles from Gastrodia elata

Background
Huntington's disease (HD) is a neurodegenerative disease caused by a CAG trinucleotide expansion in the Huntingtin (Htt) gene. The expanded CAG repeats are translated into polyglutamine (polyQ), causing aberrant functions as well as aggregate formation of mutant Htt. Effective treatments for HD are yet to be developed.

/pdf/a-new-drug-design-targeting-the-adenosinergic-system-for-30aba16rjr.pdf

A New Drug Design Targeting the Adenosinergic System for Huntington's Disease

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Neuroprotective Principles from Gastrodia elata

A New Drug Design Targeting the Adenosinergic System for Huntington's Disease