| 1. |
- Arya, Ashwani, et al.
(författare)
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Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer's Disease Therapy
- 2021
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Ingår i: Biomolecules. - : MDPI AG. - 2218-273X. ; 11:3
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Forskningsöversikt (refereegranskat)abstract
- Alzheimer’s disease (AD) is a gradually growing irreversible illness of the brain that almost affects every fifth person (aged > 80 years) in the world. World Health Organization (WHO) also revealed that the prevalence of this disease will enhance (upto double) significantly upto 2030. The poor cholinergic transmission at the synapse is considered to be one of the main reasons behind the progression and occurrence of this disorder. Natural inhibitors of acetylcholine (ACh) such as galanthamine and rivastigmine are used commercially in the treatmentof AD. The biomolecules such assesquiterpenes, possess a great structural diversity and are responsible for a plethora of pharmacological properties. The potential of various sesquiterpenes as anticholinesterase has been reviewed in this article. For this purpose, the various databases, mainly PubMed, Scopus, and Web of Science were investigatedwith different keywords such as “sesquiterpenes+acetylcholinesterase” and “sesquiterpenes+cholinesterase+inhibitors” in the surveyed time frame (2010–2020). A vast literature was evident in the last decade, which affirms the potential of various sesquiterpenes in the improvement of cholinergic transmission by inhibiting the AChE. After data analysis, it was found that 12 compounds out of a total of 58 sesquiterpenes were reported to possess IC50 < 9 μM and can be considered as potential candidates for the improvement of learning and memory. Sesquiterpene is an important category of terpenoids, found to possess a large spectrum of biological activities. The outcome of the review clearly states that sesquiterpenes (such as amberboin, lipidiol, etc.) from herbs could offer fresh, functional compounds for possible prevention and treatment of AD.
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| 2. |
- Kabir, Md. Tanvir, et al.
(författare)
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Potential Role of Curcumin and Its Nanoformulations to Treat Various Types of Cancers
- 2021
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Ingår i: Biomolecules. - : MDPI AG. - 2218-273X. ; 11:3
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Forskningsöversikt (refereegranskat)abstract
- Cancer is a major burden of disease globally. Each year, tens of millions of people are diagnosed with cancer worldwide, and more than half of the patients eventually die from it. Significant advances have been noticed in cancer treatment, but the mortality and incidence rates of cancers are still high. Thus, there is a growing research interest in developing more effective and less toxic cancer treatment approaches. Curcumin (CUR), the major active component of turmeric (Curcuma longa L.), has gained great research interest as an antioxidant, anticancer, and anti-inflammatory agent. This natural compound shows its anticancer effect through several pathways including interfering with multiple cellular mechanisms and inhibiting/inducing the generation of multiple cytokines, enzymes, or growth factors including IκB kinase β (IκKβ), tumor necrosis factor-alpha (TNF-α), signal transducer, and activator of transcription 3 (STAT3), cyclooxygenase II (COX-2), protein kinase D1 (PKD1), nuclear factor-kappa B (NF-κB), epidermal growth factor, and mitogen-activated protein kinase (MAPK). Interestingly, the anticancer activity of CUR has been limited primarily due to its poor water solubility, which can lead to low chemical stability, low oral bioavailability, and low cellular uptake. Delivering drugs at a controlled rate, slow delivery, and targeted delivery are other very attractive methods and have been pursued vigorously. Multiple CUR nanoformulations have also been developed so far to ameliorate solubility and bioavailability of CUR and to provide protection to CUR against hydrolysis inactivation. In this review, we have summarized the anticancer activity of CUR against several cancers, for example, gastrointestinal, head and neck, brain, pancreatic, colorectal, breast, and prostate cancers. In addition, we have also focused on the findings obtained from multiple experimental and clinical studies regarding the anticancer effect of CUR in animal models, human subjects, and cancer cell lines.
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| 3. |
- Shakir, Nida, et al.
(författare)
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Pirarubicin loaded biodegradable nanoparticles downregulate IL-6, COX-II and TNF-alpha along with oxidative stress markers in comparison to conventional pirarubicin in healthy albino rats
- 2023
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 84
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Tidskriftsartikel (refereegranskat)abstract
- Pirarubicin (PRB) is an anthracycline antibiotic that has shown equal or superior cytotoxicity compared to doxorubicin. However, the detailed toxicological profile for Pirarubicin has not yet been investigated. The present study was designed to access the acute and chronic toxicity of the nanoformulation coupled with in-flammatory and oxidative stress responses. PRB was encapsulated in PLGA nanoparticles and was physico-chemically evaluated. The nanoparticle size was found to be 420.0 +/- 8.2 nm with an encapsulation efficiency of 80.3 +/- 3.1%. The SEM images showed spherical nanoparticles while the drug release in PBS (pH 7.4) was estimated to be 72.5 +/- 3.5%. Acute toxicity in female albino rats was conducted for 14 days at two dosage levels (i.e., 5 and 300 mg/kg) once a week through an intravenous route. A repeated toxicity study was conducted for 28 days at 3 different dosage levels (i.e., 30, 60 and 100 mg/kg) weekly. No mortality was observed during the experimentation period. Toxicity assessment of body weights, hematological parameters, blood biochemistry, histopathological evaluation of internal organs and relative organ weight percentage was done. Inflammatory markers quantification (COX-II, TNF-alpha, IL-6) along with the generation of oxidative stress (SOD, GSH-ST, GSH-PX, MDA, and H2O2) was also investigated in a repeated 28 days toxicity study. The nanoformulation did not have any effect on the behavioral pattern, food, water consumption or body weights. The abnormalities in function and morphology of the organs produced by nano-formulated PRB were dose-dependent and reversible. The serum sample of rats treated with nanoparticles exhibited a non-significant difference in levels of COX-II, TNF-alpha, and IL-6 as compared to the normal saline (NS) group. Altogether the results offered us evidence about the safety profile of Pirarubicin loaded PLGA nanoparticles (PRB-NP) as compared to PRB alone.
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