Pharmaceutical Chemistry
Rana Naeem Jibroo; Yasser Fakri Mustafa; Wejdan Al-Shakarchi
Abstract
Background: Coumarin-based derivatives (Cou-Ds) are one of the most important types of heterocycles, with a wide range of uses in synthetic and medicinal chemistry. Cou-Ds have interested researchers due to their wide range of biomedical potential and application as valuable synthetic scaffolds, which ...
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Background: Coumarin-based derivatives (Cou-Ds) are one of the most important types of heterocycles, with a wide range of uses in synthetic and medicinal chemistry. Cou-Ds have interested researchers due to their wide range of biomedical potential and application as valuable synthetic scaffolds, which have been instrumental in the creation of coumarin chemistry. Cou-Ds are a unique class of bioactive candidates with novel therapeutic attributes due to their bacteriostatic, antifungal, antioxidant, anticancer, antidepressant, and other pharmacological properties. In addition to their biomedical uses, the literature illustrates the uses of Cou-Ds from a material point of view, such as those in food additives, fragrances, beauty products, optical brighteners, and would disperse fluorescent and laser dyes. Numerous optical purposes using Cou-Ds have been thoroughly investigated. A wide range of natural sources and newly created Cou-Ds are being isolated or produced at a growing rate. The procedures of synthesis and therapeutic uses of Cou-Ds in the treatment of various illnesses were critically found in many published papers. Aim: The aim of this review article is to highlight the most up-to-date information about Cou-Ds and clarify the various natural sources, synthetic strategies, reactions, biological activity, and different pharmaceutical applications of Cou-Ds. Conclusion: From the collected and discussed reviewing information, the authors concluded that the Cou-Ds can open the drug development door for producing more potent, biosafe medicines.
Pharmacognosy & Natural Products
Raghad Riyadh Khalil
Abstract
Background: for a long time, natural bio-actives have been used to treat, cure, and prevent illnesses. Fruit seed crude extracts have been found to have various beneficial biological activities, such as anti-inflammatory, antioxidant, and antitumoral potential. Methods: this study investigated quince ...
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Background: for a long time, natural bio-actives have been used to treat, cure, and prevent illnesses. Fruit seed crude extracts have been found to have various beneficial biological activities, such as anti-inflammatory, antioxidant, and antitumoral potential. Methods: this study investigated quince seed extract made using absolute ethanol as a solvent regarding flavonoid and phenolic content, as well as antioxidant, anti-inflammatory, and anticancer properties. The extract was obtained using two methods, microwave-facilitated extraction and sequential microwave-ultrasound-assisted extraction. Results: the extract from the microwave-facilitated method had higher flavonoid and phenolic content with superior antioxidant activity. Hydroxyl free radical and DPPH assays' IC50 were 121.04±1.10 and 112.98±1.02, respectively, compared to the sequential method, which had IC50 values of 193.19±0.86 and 187.23±0.95. The microwave method also displayed significantly higher inhibitory activity against inflammatory enzymes and selectivity against COX2 compared to the sequential one. However, the extracts did not exhibit any antiproliferative effect on malignant or healthy cellular lines at the applied concentrations, and they did not enhance the effectiveness of 5-FU (5-Fluorouracil) in preventing the growth of cancerous cells. However, the mutual application in general results in increasing the IC50 value of 5-FU toward the healthy cellular line (MCF-A10). Therefore, the mutual application of these extracts with 5-FU can be seen as a protective measure. Conclusion: the crude extract obtained through the microwave-facilitated method had better TPC, TFC, antioxidant, anti-inflammatory activity, and protective potential than the sequential method.
Pharmaceutical Chemistry
Yasser Fakri Mustafa; Sarah Ahmed Waheed; Sara Firas Jasim; Rahma Mowaffaq Jebir; Reem Nadher Ismael; Omar Qutachi
Abstract
Background: Coumarins and their derivatives excel in chemical diversity, coupled with a wide variety of biological potentials, and tend to be beneficial to the health of the human body. One of these derivatives that has sparked the attention of medicinal chemistry specialists in recent decades is benzo-fused ...
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Background: Coumarins and their derivatives excel in chemical diversity, coupled with a wide variety of biological potentials, and tend to be beneficial to the health of the human body. One of these derivatives that has sparked the attention of medicinal chemistry specialists in recent decades is benzo-fused coumarins, which have demonstrated their potential as antioxidants, antimicrobials, antidiabetics, antithrombotics, and many more. Objective: This paper discusses the medicinal importance of benzo-fused coumarins derived from natural or synthetic sources. Conclusion: The researchers documented that benzo-fused coumarin's basic structure is a promising framework that opens up the chance of discovering innovative applicants with advanced therapeutic potentials.
Ashwaq Najeem Eldeen; Mohammed Mahmood Mohammed; Mohammad Dakhel
Abstract
Lead is a neurotoxic metallic element that can be absorbed by the body, primarily through the lungs and stomach. Generally, lead poisoning occurs slowly, resulting from the gradual accumulation of lead in bone and tissue after repeated exposure. Left untreated, lead poisoning can damage many internal ...
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Lead is a neurotoxic metallic element that can be absorbed by the body, primarily through the lungs and stomach. Generally, lead poisoning occurs slowly, resulting from the gradual accumulation of lead in bone and tissue after repeated exposure. Left untreated, lead poisoning can damage many internal organs, including the kidney and the nervous system. Recent studies have shown that lead causes oxidative stress by inducing the generation of reactive oxygen species and reducing the antioxidant defense system of cells. This suggests that antioxidants may play an important role in the treatment of lead poisoning as a kind of scavengers of free radicals.
Antioxidant is any substance that reduces oxidative damage such as that caused by free radicals. Free radicals are highly reactive chemicals that attack molecules by capturing electrons and thus modifying chemical structures. Melatonin, a powerful antioxidant, is a hormone produced naturally in the pineal gland at the base of the brain.
This study was designed to evaluate the clinical significance of melatonin in ameliorating the oxidative stress induced due to chronic exposure to lead.
Twenty male patients with chronic lead poisoning and their 20 aged matched normal controls with an age range 35-45 years were included in this study. Treatment included 3 mg capsule of melatonin antioxidant at night for two months. Heparinized venous blood samples were collected from patients before treatment and at one and two months after treatment as well as from controls to measure erythrocytes malondialdehyde (RMDA), plasma total antioxidant status (TAS), blood lead (Pb) and serum zinc (Zn) levels.
The results of the study showed a significant antioxidant activity of melatonin in eliminating the oxidative consequences of lead exposure revealed by significant reduction in oxidative stress markers ( RMDA and Pb) with a significant increase in body antioxidant defense mechanisms(TAS and Zn).