This project looks at a novel way to enhance the sensory experience of vitamin D ingestion by incorporating it into marshmallows. This investigation used a human panel taste test with twelve individuals, an index of swelling, and a stability evaluation. Samples of vitamin D infused marshmallows were prepared and given to participants in the human panel taste test, which evaluated mouthfeel and flavor. By analyzing dissolving behavior, the swelling index test revealed unexpected erosion. In addition, a temperature threshold for storage conditions was found through a temperature sensitivity test. All of these techniques assessed the feasibility and palatability of vitamin D supplementation with marshmallow flavor, offering insights into both the possible advantages and difficulties. The marshmallow infusion technique effectively covered up the disagreeable taste of vitamin D pills, leading to reviews that were overwhelmingly favorable ("Moderate Sweet") and that indicated a pleasant mouthfeel. During the swelling index test, it showed erosion behavior, suggesting a certain kind of dissolution that is advantageous for nutritional absorption. Furthermore, the study discovered a temperature sensitivity threshold, highlighting how crucial proper storage conditions are.
This work deals with the synthesis and physicochemical characterizations of a new group of novel retinoidal ligands and their metal complexes. Their in vitro anti-proliferative activities have shown that ligand L1 is effective against human breast cancer BT-20 and MCF-7 cell lines. At the same time, compound L2 exerts its effect on human prostate cancer PC-3 and human breast cancer MDA-MB-231 and MCF-7 cell lines respectively. The retinoid ligands exert their pleiotropic action toward retinoic acid receptors (RARs) than their metal complexes but all compounds exhibit concentration-dependent.
The objective of this research was to elucidate the biological effect of novel compounds derived from natural product of syringaldehyde through novel semi-synthetic method in order to investigate the physicochemical properties and biological activities by using DPPH and FRAP techniques and its antibacterial activities against Klebsiella spp., Pseudomonas aeruginosa, Bacillus cereus, and Staphylococcus aureus. Moreover, to examine its ability against breast cancer cell line (MCF-7). The results showed that the syringaldehyde hydrazonate copper complexes possessed the covalent bonds with square-planar structure. In terms of antioxidant DPPH activities, it was found that syringaldehyde hydrazone possessed high potency against DPPH free radicals, with respect to syringaldehyde hydrazonate copper complexes. On the other hand, all compounds possessed low reducing properties for changing Fe3+ to Fe2+ in FRAP technique. For antibacterial activities revealed that the ligand L1 and L5 possessed high effect on Pseudomonas aeruginosa, but for all copper complexes possessed high potent antibacterial susceptibility to four bacteria with concentration dependence. For anti-breast cancer cell line (MCF-7), it was found that all compounds possessed high potent anticancer susceptibility with low IC50, especially, compound exhibit highly potency effective is C5 (IC50 9.75 μM). The tendency of anticancer effect from high to low was C5 > C2 > C1 > C4 > C3. Therefore, all synthetic compounds obtained from the present research possibly develop as the antibacterial drugs and the drugs for curing the diseases caused by free radicals, including breast cancer in metastatic phase. The most important feature of these drugs was the high specificity to the target and harmless to the normal cells.
Cancer is a leading cause of death globally, claiming about 9.6 million lives and approximately 420 million new cases of cancer will be diagnosed in the world by the year 2025. The aim of this study was to synthesize and computationally evaluate pharmacological potential of some derivatives of 9-amino-3-phenylacridone, as topoisomerase II (Topo II) inhibitors. In this study, 10 derivatives of 3-phenyl-9-aminoacridone were chemically synthesized and characterized, and the potential pharmacological indications of these compounds were computationally predicted by methods such as ADMET prediction, molecular target prediction and molecular docking. The results showed that two derivatives (58e and 58j) were non-permeant of blood-brain barrier, and this property was found similar to that of amsacrine and etoposide. The results of molecular docking of the ten derivatives of 3-phenyl-9-aminoacridone that were synthesized in this work showed that the synthetic compounds (58a-j) and the standard drugs have overall best binding affinities for human acetylcholine esterase than butyrylcholinesterase, and overall best binding affinities for human topo IIα than human topo IIβ. Overall, the results of this study suggest that the synthetic compounds 58a, 58c, 58f, 58g, and 58i could probably inhibit topo IIα by catalytic inhibition as seen with amsacrine, but only 58b and 58e possessed DNA non-intercalation properties as seen with etoposide, serving as topo II poison. In conclusion, this study showed that 3-phenyl-9-aminoacridone derivatives are potential inhibitor of topo IIα/β both by catalytic inhibition and poison as non-intercalator of DNA.
A series of 4-thioflavonols compounds were synthesized by treating flavonols with lawsons reagent with variable substituent groups at A, B, and AB rings. All the synthesized compounds were checked for antibacterial and antifungal activity. We report that many compounds were found active against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus, bacterial strains and, C. albicans, C. parapsilosisstrains and C. krusei fungal strains. Most of the synthesized 4-thioflavonols compounds were found to show enhanced antimicrobial activity than respective flavonol compounds.
The new ligand, 2-acetylpyrazine-tertbutylthiosemicarbazone (APZ-tBTSC), and its Cu(II), Pd(II) and Pt(II) complexes have been synthesized.This ligand coordinates to the metal ions in a tridentate monoanionic fashion forming monometallic complexes with the formula [M(APZ-tBTSC)Cl].The ligand and the three metal complexes [Cu(APZ-tBTSC)Cl], [Pd(APZ-tBTSC)Cl], and [Pt(APZ-tBTSC)Cl] were tested for anti-proliferative biological behavior with a panel of seven microbes, and the copper and palladium complexes were found to be highly active against Gram positive bacteria.The 4 compounds were also tested in human topoisomerase IIα DNA relaxation assays and all three metal complexes had topoisomerase inhibition at a concentration between 4 -6 micro-molar.The 4 compounds were also tested for activity with the HEK293T cell line and also the breast cell cancer line, MDA-MB-231.The most effective compound for activity against the HEK293T cell line was the [Cu(APZ-tBTSC)Cl] complex, and the MDA-MB-231 breast cancer cell line was the [Pt(APZ-tBTSC)Cl] complex.
A series of 2-(benzylthio)pyrimidines (6a-l) and 2-(benzimidazolylmethylthio)-pyrimidines derivatives (6m and 6n) analogues of ethyl 2-(benzylthio)-6-methyl-4-phenyl-1,4-dihydropyrimidine-5-carboxylates and ethyl 2-(((1H-benzimidazol-2-yl)methyl)thio)-6-methyl-4-phenyl-1,4-dihydropyri-midine-5-carboxylates were prepared and evaluated for antibacterial activity. These compounds were obtained by condensation of 2-thiopyrimidines (4) with benzyl halides or 2-(chloromethyl)-1H-benzimidazole (5) in the presence of a base. All compounds were characterized by 1H, 13C and HRMS spectra. Out of fourteen, only eight compounds were screened against multi-resistant strains of Escherichia coli and Staphylococcus aureus. The results revealed that all of them were found to possess significant antibacterial activity against the germs tested. Compounds 6c, 6d, 6h and 6m were more active on S. aureus and compounds 6h and 6m more active on E. coli.
Melaleuca (tea tree) oil has become increasingly commonly used in recent decades. The essential oil in Australia for the past 120 years is now available globally as an active component in various products. Historically, Melaleuca oil is known for its antiseptic and anti-inflammatory actions. Currently, microwave technology is applied to extract Melaleuca oil, but this extraction technology is not commercially under practice. Traditionally, Melaleuca oil extraction is possible through steam distillation of the Melaleuca alternifolia terminal branches and leaves, and the resultant extract is always either clear or pale yellowish. Melaleuca oil has been promoted as a therapeutic agent because scientific studies indicate that the Rideal-Walker (RW) coefficients of its extract composition include 8 for cymene, 16 for terpineol, 13.5 for tepinen-4-ol and 3.5 for cineole. The mode of action against bacteria is now partially elucidated, and assumptions exist. Hydrocarbons partition into biological membranes to disrupt the vital functions of Melaleuca oil, and also its components behave in the same manner. Therefore, the inhibition of respiration and the leakage of ions or loss of intracellular material and the inability to maintain homeostasis reflect the loss of membrane integrity and lysis in Melaleuca oil products containing lower than usual terpenes concentrations. Melaleuca oil possesses antifungal properties and is known exclusively for the treatment of Candida albicans. This essential oil strongly changes the permeability of Candida albican cells. C. albicans treatment with 0.25% tea tree oil leads to propidium iodide uptake. However, a significant loss of 260-nmlight-absorbing materials after staining with methylene blue occurs after 6 hours. Melaleuca extracts alter the permeability of Candida glabrata that ocHow to cite this paper: Kasujja, I. (2021) Critical Evaluation of Melaleuca alternifolia: A Review of the Phytochemical Profile, Pharmacological Attributes and Medicinal Properties in the Botanical, Human and Global Perspectives. Open Journal of Medicinal Chemistry, 11, 1-15. https://doi.org/10.4236/ojmc.2021.111001 Received: December 14, 2020 Accepted: March 28, 2021 Published: March 31, 2021 Copyright © 2021 by author(s) and Scientific Research Publishing Inc. This work is licensed under the Creative Commons Attribution International License (CC BY 4.0). http://creativecommons.org/licenses/by/4.0/
Over the past years, natural products have been used as useful candidates for prevention and treatment of skin disorders such as skin darkening.In this current research, Daniellia oliveri which was a potential source of cosmeceutical agent was selected to investigate its active components.Daniellic acid isolated from the oleoresin was characterized by using data from 1 H-NMR, 13 C-NMR, HSQC, IR, and online chemo-informatic analysis.The daniellic acid antioxidant, anti-proliferative, and tyrosinase inhibition capabilities were evaluated.This compound possessed an anti-DPPH and iron (III) reducing effect compared to quercetin.It was able to inhibit 9 tumor cells with IC 50 going from 0.03 mM (U373) to 0.14 mM (Malme-3M).Interestingly daniellic acid inhibits tyrosinase activity with 1.20 mM as IC 50 .The tyrosinase inhibition mechanism was noncompetitive mixed-type with un-significant effect on cell melanogenesis.Daniellic acids induced a half-reduction of melanin production in B16F10 cell in IBMX stimulation (p < 0.05).The same observation was effective in Malme-3M melanin production with a significant daniellic acid action than kojic acid (p < 0.05) without reducing cell viabilities.This bioactive daniellic acid could explain the traditional uses of oleoresins from Daniellia oliveri for genitor-urinary tract diseases treatments, wound healing, and skin ailments in Burkina Faso.
Due to the continuous emergence and rapid spread of drug-resistant strains of bacteria, there is an urgent need for the development of novel antimicrobials. Along this line, the synthesis and antibacterial activity of 4,5-diphenylimidazol-2-thiol derivatives 2a-g and 6a-e are reported. The structures of the synthesized compounds were confirmed by Nuclear Magnetic Resonance (NMR) and High Resolution Mass Spectrometry (HRMS). All compounds were screened in vitro for their antibacterial activity against Pseudomonas aeruginosa and Escherichia coli (Gram-negative bacteria) and also against Staphyloccocus aureus and Enterococcus faecalis (Gram-positive bacteria). The results showed most of the synthesized compounds have no antibacterial activity. However compound 6d was two-fold potent than ciprofloxacin against Staphylococcus aureus with Minimum Inhibitory Concentration (MIC) of 4 μg/mL and 6c showed moderate biological activity against Staphylococcus aureus (16 μg/mL) and Enterococcus faecalis (16 μg/mL).
The present pharmacochemical and modelling work focused on a benzimidazolyl-chalcone series.These previously synthesized compounds were evaluated in vitro for their anticancer activities against a panel of seven human cancer cell lines and normal fibroblasts.Among the new benzimidazole-supported chalcones, nine (9) compounds (compounds 1 -4, 6 -8 and compounds 10 and 11) showed promising anticancer activities with IC 50 s ranging from 0.83 to 2.58 µM.Compounds 2 and 6 with IC 50 s of 0.83 and 0.86 µM, respectively, were shown to be potent inhibitors of HCT-116 colon cancer cell proliferation.It was therefore necessary, for a development of this new series of chalcones, to establish through a QSAR study, their quantum descriptors according to the DFT calculation method and following the B3LYP/6-31+G (d,p) theory.These descriptive and predictive studies focused on the colon HCT 116 cell line which was found to be more sensitive to the anticancer action of our benzimidazolyl-retrochalcones.QSAR study showed that the electronic energy (E elec ), lipophilicity (logP), chemical softness (S) and chemical hardness (η) of benzimidazolyl-retrochalcones play an important role in inhibiting cancer cell proliferation.
Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents. A molecular docking study was employed to investigate the binding and functional properties of 3-amino pyranoquinolinone 2a-c as anti-cancer agents. The three 3-amino pyranoquinolinone 2a-c showed an interesting ability to intercalate the DNA-topoisomerase complex and were able to obtain energetically favorable binding modes (−8.3 - −7.5 kcal/mol). Compound 2c containing butyl chain superiority over the other two compounds 2a-b which appeared to be involved in arene-H interactions with the two dG13 aromatic centers. The butyl chain also appeared to be immersed into a side subpocket formed by the side chains of Asn520 and Glu522 and the backbone amide of Arg503, Gly504, Lys505 and Ile506. Hence, the 3-amino pyranoquinolinone 2c used as starting material to prepare derivatives of pyrano[3,2-c]quinolone containing 1,2,4-triazine ring 4a-b which will enhance the anti-cancer activity. Pyrano[3,2-c]quinoline-2,5-diones 2a-c and 4a-b were evaluated in vitro on cell lines Ehrlich Ascites carcinoma cells (EAC), liver cancer cell line Hep-G2 and breast cancer cell line MCF-7 for the development of novel anticancer agents. The screening results revealed that compounds 4a-b were found most active candidates as anticancer agents.
