scholarly journals Mānuka Oil—A Review of Antimicrobial and Other Medicinal Properties

2020 ◽  
Vol 13 (11) ◽  
pp. 343
Author(s):  
Cynthia Mathew ◽  
Wubshet Tesfaye ◽  
Phil Rasmussen ◽  
Gregory M Peterson ◽  
Andrew Bartholomaeus ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Grey Literature ◽  
Indigenous Populations ◽  
Chemical Structures ◽  
Medicinal Properties ◽  
Conventional Antibiotics ◽  
Google Search ◽  
Manuka Oil

Mānuka oil is an essential oil derived from Leptospermum scoparium, a plant that has been used by the indigenous populations of New Zealand and Australia for centuries. Both the extracted oil and its individual components have been associated with various medicinal properties. Given the rise in resistance to conventional antibiotics, natural products have been targeted for the development of antimicrobials with novel mechanism of action. This review aimed to collate available evidence on the antimicrobial, anti-parasitic and anti-inflammatory activities of mānuka oil and its components. A comprehensive literature search of was conducted using PubMed and Embase (via Scopus) targeting articles from database inception until June 2020. Chemical structures and IUPAC names were sourced from PubChem. Unpublished information from grey literature databases, Google search, targeted websites and Google Patents were also included. The present review found extensive in vitro data supporting the antimicrobial effects of mānuka oil warrants further clinical studies to establish its therapeutic potential. Clinical evidence on its efficacy, safety and dosing guidelines are necessary for its implementation for medical purposes. Further work on regulation, standardization and characterization of the medicinal properties of mānuka oil is required for establishing consistent efficacy of the product.

scholarly journals Chemical Derivatization and Characterization of Novel Antitrypanosomals for African Trypanosomiasis

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4488
Author(s):  
Aboagye Kwarteng Dofuor ◽  
Temitayo Samson Ademolue ◽  
Cynthia Mmalebna Amisigo ◽  
Kwaku Kyeremeh ◽  
Theresa Manful Gwira
Keyword(s):  
Structural Modification ◽  
Spectroscopic Analysis ◽  
Microscopic Analysis ◽  
The Novel ◽  
Chemical Derivatization ◽  
African Trypanosomiasis ◽  
Chemical Structures ◽  
Normal Ratio

The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.

scholarly journals Efficacy of natural formulations in bovine mastitis pathology: alternative solution to antibiotic treatment

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Claudia Pașca ◽  
Liviu Alexandru Mărghitaș ◽  
Daniel Severus Dezmirean ◽  
Ioana Adriana Matei ◽  
Victorița Bonta ◽  
...  
Keyword(s):  
Natural Products ◽  
Therapeutic Potential ◽  
Dairy Product ◽  
Bovine Mastitis ◽  
Antimicrobial Effect ◽  
Economic Losses ◽  
Standard Plate ◽  
Conventional Antibiotics

AbstractIntroductionBovine mastitis is an inflammatory disease of the udder that causes important economic losses in the animal breeding and dairy product industries. Nowadays, the conventional livestock antibiotic treatments are slowly being replaced by alternative treatments. In this context, the main aim of this study was to evaluate the efficacy of natural products in alternative treatment of bovine mastitis.Material and MethodsTwo natural formulations with previously suggested in vitro antimicrobial effect were tested in vivo on mastitic cows. Animals with a positive diagnosis for mastitis (n = 20) were divided into three treatment groups: two groups (n = 8) were administered formulations of propolis, alcoholic extracts of Brewers Gold and Perle hops, plum lichen, common mallow, marigold, absinthe wormwood, black poplar buds, lemon balm, and essential oils of oregano, lavender, and rosemary designated R4 and R7 (differing only in the latter being more concentrated) and one group (n = 4) a conventional antibiotic mixture. In vivo efficacy of treatments was evaluated by somatic cell and standard plate counts, the treatment being considered efficacious when both parameters were under the maximum limit.ResultsR7 was effective in the most cases, being therapeutically bactericidal in six out of eight cows, while R4 gave good results in three out of eight cows, and conventional antibiotics cured one out of four.ConclusionThese results suggest the possible therapeutic potential of these natural products in bovine mastitis.

scholarly journals Synthesis and Characterization of 2-Pyrazoline Derivatives and their in silico and in vitro Studies on Antimicrobial and Anticancer Activities

2019 ◽  
Vol 31 (10) ◽  
pp. 2191-2196 ◽  
Author(s):  
S. Rathinamanivannan ◽  
K. Megha ◽  
Raja Chinnamanayakar ◽  
Ashok Kumar ◽  
M.R. Ezhilarasi
Keyword(s):  
Breast Cancer ◽  
Synthesis And Characterization ◽  
Anticancer Activities ◽  
1H And 13C Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Affinity Score ◽  
High Binding Affinity

The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives chemical structures were confirmed from spectral data such as FT-IR, 1H and 13C NMR. 2-Pyrazoline derivatives were docked with bacterial (1UAG) and breast cancer (1OQA) protein. Based on high binding affinity score, the best compound was subjected to in vitro anticancer activity by MTT assay. Also, antimicrobial activity were studied for synthesized 2-pyrazoline derivatives.

scholarly journals Therapeutic Potential Of Multifunctional Derivatives Of Cholinesterase Inhibitors

2020 ◽  
Vol 19 ◽  
Author(s):  
Maja Przybyłowska ◽  
Krystyna Dzierzbicka ◽  
Szymon Kowalski ◽  
Klaudia Chmielewska ◽  
Iwona Inkielewicz-Stepniak
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Therapeutic Potential ◽  
Amyloid Plaque ◽  
Β Amyloid ◽  
Derivatives Of ◽  
And Oxidative Stress ◽  
Pro Inflammatory Cytokines

: The aim of this work is review of tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant, decreasing β-amyloid plaque aggregation, nitric oxide production, pro-inflammatory cytokines release, monoamine oxidase-B activity, cytotoxicity and oxidative stress in vitro and in animal model that classify these hybrids as potential multifunctional therapeutic agents for Alzheimer’s disease. Moreover, herein, we have described the cholinergic hypothesis, mechanisms of neurodegeneration and current pharmacotherapy of Alzheimer’s disease which is based on the restoration of cholinergic function through blocking enzymes that break down acetylcholine.

scholarly journals Computational Insight into the Effect of Natural Compounds on the Destabilization of Preformed Amyloid-β(1-40) Fibrils

2018 ◽  
Author(s):  
Francesco Tavanti ◽  
Alfonso Pedone ◽  
Maria Cristina Menziani
Keyword(s):  
Therapeutic Strategy ◽  
Therapeutic Potential ◽  
Structure Stability ◽  
Insoluble Form ◽  
The Brain ◽  
Identification And Characterization ◽  
Insight Into

One of the principal hallmarks of Alzheimer’s disease (AD) is related to the aggregation of amyloid-β fibrils in an insoluble form in the brain, also known as amyloidosis. Therefore, a prominent therapeutic strategy against AD consists either in blocking the amyloid aggregation and/or destroying the already formed aggregates. Natural products have shown significant therapeutic potential as amyloid inhibitors from in vitro studies as well as in vivo animal tests. In this study, the interaction of five natural biophenols (curcumin, dopamine, (-)-Epigallocatechin-3-gallate, Quercetin, and Rosmarinic acid) with the amyloid-β(1-40) fibrils has been studied through computational simulations. The results allowed the identification and characterization of the different binding modalities of each compounds and their consequences on fibril dynamics and aggregation. It emerges that the lateral aggregation of the fibrils is strongly influenced by the intercalation of the ligands, which modulate the double-layered structure stability.

scholarly journals Pharmacogenomics characterization of the MDM2 inhibitor MI-773 reveals candidate tumours and predictive biomarkers

2021 ◽  
Vol 5 (1) ◽  
Author(s):  
Vincent Vuaroqueaux ◽  
Hans R. Hendriks ◽  
Hoor Al-Hasani ◽  
Anne-Lise Peille ◽  
Samayita Das ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Predictive Biomarkers ◽  
Wild Type ◽  
Mutation Status ◽  
Anti Tumour Activity ◽  
Molecule Inhibitor ◽  
Tumour Activity ◽  
Selection Of

AbstractMI-773 is a recently developed small-molecule inhibitor of the mouse double minute 2 (MDM2) proto-oncogene. Preclinical data on the anti-tumour activity of MI-773 are limited and indicate that tumour cell lines (CLs) with mutated TP53 are more resistant to MI-773 than wild type TP53. Here, we explored the compound’s therapeutic potential in vitro using a panel of 274 annotated CLs derived from a diversity of tumours. MI-773 exhibited a pronounced selectivity and moderate potency, with anti-tumour activity in the sub-micromolar range in about 15% of the CLs. The most sensitive tumour types were melanoma, sarcoma, renal and gastric cancers, leukaemia, and lymphoma. A COMPARE analysis showed that the profile of MI-773 was similar to that of Nutlin-3a, the first potent inhibitor of p53–MDM2 interactions, and, in addition, had a superior potency. In contrast, it poorly correlates with profiles of compounds targeting the p53 pathway with another mechanism of action. OMICS analyses confirmed that MI-773 was primarily active in CLs with wild type TP53. In silico biomarker investigations revealed that the TP53 mutation status plus the aggregated expression levels of 11 genes involved in the p53 signalling pathway predicted sensitivity or resistance of CLs to inhibitors of p53–MDM2 interactions reliably. The results obtained for MI-773 could help to refine the selection of cancer patients for therapy.

scholarly journals Chromatographic determination of bioactive compounds in Hippophae leaf extracts: a comparative study of three varieties.

2018 ◽  
Vol 3 (3) ◽  
pp. 255 ◽  
Author(s):  
Rakhee Ms ◽  
Jigni Mishra ◽  
Priyanka Sharma ◽  
Kshipra Misra
Keyword(s):  
Therapeutic Potential ◽  
Chromatographic Determination ◽  
Hippophae Rhamnoides ◽  
Antioxidant Potential ◽  
Leaf Extracts ◽  
Hippophaë Rhamnoides ◽  
R Programming

<p>Seabuckthorn plants (<em>Hippophae Linn</em>), belonging to the family Elaeagnaceae have shown diverse therapeutic potential and the adaptogenic activity of some of the species have also been established in our previous studies. The present study aims to characterize aqueous and alcoholic leaf extracts of three different varieties of seabuckthorn, namely, <em>Hippophae salicifolia</em>, <em>Hippophae rhamnoides mongolica </em>and <em>Hippophae rhamnoides turkestanica</em> and evaluate their antioxidant potential <em>in vitro. </em>An elaborate characterization of phytochemicals such as volatile organic compounds (VOC) and flavonoids occurring in the concerned extracts has been carried out by GC-MS and HPTLC respectively. GC-MS demonstrated the presence of 35 distinct VOCs in the seabuckthorn leaf extracts which are known to possess substantial pharmacological and antioxidant potential. The most abundant VOCs identified were trimethylsilyl palmitate, methyl octadec-9-enoate, methyl palmitate, methyl stearate and methyl (9E)-9-octadecenoate. HPTLC results revealed variable quantities of quercetin, gallic acid, ascorbic acid and rutin in all the seabuckthorn leaf extracts. HPTLC-centered chemometric analysis using R programming helped to distinguish among the various extracts based on pattern recognition and unsupervised clustering, thus, enabling grouping of the extracts for further studies.</p>

Design, Synthesis and Therapeutic Potential of Some 6, 6'-(1,4- phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine)analogues

2019 ◽  
Vol 19 (7) ◽  
pp. 609-621
Author(s):  
Sanjiv Kumar ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Bacterial Species ◽  
Cancer Cell Line ◽  
Docking Study ◽  
Binding Pocket ◽  
Fungal Species ◽  
Molecular Docking Study ◽  
Reference Drug ◽  
Chemical Structures

<P>Background: A series of 6, 6'-(1,4-phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine) derivatives has been synthesized by Claisen-Schmidt condensation and its chemical structures was confirmed by FT-IR, 1H/13C-NMR spectral and elemental analyses. The molecular docking study was carried out to find the interaction between active bis-pyrimidine compounds with CDK-8 protein. The in vitro antimicrobial potential of the synthesized compounds was determined against Gram-positive and Gram-negative bacterial species as well fungal species by tube dilution technique. Antimicrobial results indicated that compound 11y was found to be most potent one against E. coli (MICec = 0.67 µmol/mL) and C. albicans (MICca = 0.17 µmol/mL) and its activity was comparable to norfloxacin (MIC = 0.47 µmol/mL) and fluconazole (MIC = 0.50 µmol/mL), respectively. Conclusion: Anticancer screening of the synthesized compounds using Sulforhodamine B (SRB) assay demonstrated that compounds 2y (IC50 = 0.01 µmol/mL) and 4y (IC50= 0.02 µmol/mL) have high antiproliferative potential against human colorectal carcinoma cancer cell line than the reference drug (5- fluorouracil) and these compounds also showed best dock score with better potency within the ATP binding pocket and may also be used lead for rational drug designing.</P>

A Review on Phytochemistry, Pharmacological Action, Ethanobotanical Uses and Nutritional Potential of Kedrostis foetidissima (Jacq.) Cogn.,

2020 ◽  
Vol 18 (1) ◽  
pp. 5-20 ◽  
Author(s):  
Kalaiseziyen Pavithra ◽  
Ganapathy Saravanan
Keyword(s):  
Biological Activities ◽  
Research Work ◽  
Pharmacological Action ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Traditional Medicines ◽  
Chemical Structures ◽  
Medicinal Properties

Nature is an amazing source for food, shelter, clothing and medicine. An impressive number of modern drugs are isolated from many sources like plants, animals and microbes. The development of natural products from traditional medicines is of great importance to society. Modern concepts and methodologies with abundant clinical studies, unique diversity of chemical structures and biological activities aid the modern drug discovery process. Kedrostis foetidissima (Jacq.) Cogn., a traditional medicinal plant of the Cucurbitaceae family, is found in India, Sri Lanka, Ethiopia and Western Malaysia. Almost all parts of the plant are used in traditional systems of medicines and reported having medicinal properties in both in vitro and in vivo studies. In the last few years, extensive research work had been carried out using extracts and isolated phytoconstituents from Kedrostis foetidissima to confirm its pharmacology and biological activities. Many scientific reports show that crude extracts and extensive numbers of phytochemical constituents isolated from Kedrostis foetidissima have activities like antimicrobial, antioxidant, anticancer, gastroprotective, anti-inflammatory and various other important medicinal properties. The therapeutic properties of the plants are mainly attributed to the existence of phytoconstituents like phenols, alkaloids, flavonoids, tannins, terpenoids and steroids. This comprehensive review in various aspects gave a brief overview of phytoconstituents, nutritional values and medicinal property of the plant and might attract the researchers to explore its medicinal activity by discovering novel biologically active compounds that can serve as a lead compound in pharmaceutical and food industry.

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