Plant-sourced antimicrobials are known for their therapeutic potency against multi-drug-resistant pathogens. The members of Scutellaria L. have been used to cure several diseases in East Asia, Europe, and North America. The genus Scutellaria belonging to Lamiaceae family is composed of around 360 species worldwide and 18 species in Turkey. In this study, 36 extracts prepared with different solvents from aerial parts and roots of S. salviifolia Benth., S. diffusa Benth. and S. pontica C. Koch were investigated for their antimicrobial activity against four bacteria (Escherichia coli ATCC 25922, Enterococcus faecalis ATCC 29212, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 29213) and three yeasts (Candida albicans ATCC 90028, C. krusei ATCC 6258, C. parapsilosis ATCC 90018) by using the broth microdilution method. Gentamicin, vancomycin and fluconazole were used as positive control. According to our results, all of the tested extracts showed stronger antimicrobial activity against yeasts than bacteria. The chloroform extract of S. salviifolia root showed the highest antifungal effect against C. krusei with 32 μg/ml MIC value compared with all the tested extracts and the positive control fluconazole (64 μg/ml MIC value).
Resistance to therapeutic agents and the highly toxic side effects of synthetic drugs has spurred new research in the treatment of colon cancer, which has high morbidity and mortality ratios. This study aims to clarify the molecular mechanisms of the anticarcinogenic properties of methanol extract of Viburnum opulus L. (EVO)and its main active compound, trans-p -coumaric acid ( p -CA), on human colon cancer cells (DLD-1, HT-29, SW-620, Caco-2) and healthy colon epithelial cells (CCD-18Co). The effects of EVO on controlled cell death (apoptosis) and the cell division cycle were determined by flow cytometry. Alteration in mRNA and protein expressions of switch genes in colorectal carcinoma (APC, MLH1, TP53, SMAD4, KRAS, and BRAF) were determined by qRT-PCR and Western blot, respectively. Our results show that EVO possesses a strong reducing capacity and free-radical scavenging activity. HPLC analyses prove that p -CAis the main compound of EVO. EVO and p -CA inhibit the proliferation of human colon cancer cells DLD-1 and HT-29 in a dose-dependent manner. EVO increases apoptosis of DLD-1 cells and halts the cell cycle in the G2 stage in HT-29 cells. mRNA and protein expressions of p53 and SMAD-4 are upregulated, while BRAFs are downregulated. The results were directly proportional to p -CA. EVO and p -CA up- and downregulate switch genes and protein expressions of DLD-1 cells, which alter the expression of 186 other genes. This is the first study of pharmacological exploration of V.opulus in human colon cancer. Its antiproliferative effects may be due to the presence of p -CA.
Approximately 70% of the world's population has been using medicinal herbs as a complementary or alternative medicine that has grown tremendously in both developed and developing countries over the past 20 years (World Health Organization Drugs Strategy 2002-2005). This increase in consumer demand for medicinal plants continues, although scientific data are rare to create safety and efficacy profiles. Its popularity is also related to easy availability, cost-effectiveness leading to better purchasing power, and various factors that perceive that they are generally safe. Herbs are often administered simultaneously with therapeutic drugs for the treatment of major ailments, and herb-drug interactions (HDIs) increase their potential. The main routes proposed for HDIs include cytochrome P450 (CYP450)-mediated inhibition or induction and transport and flow proteins. In our review, we highlighted herbal medicines used for the treatment of various diseases with pharmacokinetic, pharmacodynamic analysis and case reports together with their adverse effects and herb-drug interactions. Therefore, this review can be used as a quick reference database for physicians and healthcare professionals involved in therapy, aiming to maximize clinical outcomes by reducing the negative and toxic effects of plants along with avoiding herb-drug interactions.
Brain-derived neurotrophic factor (BDNF) and its receptor tyrosine receptor kinase B (TrkB) have been shown to play an important role in numerous neurological disorders, such as Alzheimer’s disease. The identification of biologically active compounds interacting with TrkB serves as a drug discovery strategy to identify drug leads for neurological disorders. Here, we report effective immobilization of functional TrkB on magnetic iron oxide nanoclusters, where TrkB receptors behave as “smart baits” to bind compounds from mixtures and magnetic nanoclusters enable rapid isolation through magnetic separation. The presence of the immobilized TrkB was confirmed by specific antibody labeling. Subsequently, the activity of the TrkB on iron oxide nanoclusters was evaluated with ATP/ADP conversion experiments using a known TrkB agonist. The immobilized TrkB receptors can effectively identify binders from mixtures containing known binders, synthetic small molecule mixtures, and Gotu Kola (Centella asiatica) plant extracts. The identified compounds were analyzed by an ultrahigh-performance liquid chromatography system coupled with a quadrupole time-of-flight mass spectrometer. Importantly, some of the identified TrkB binders from Gotu Kola plant extracts matched with compounds previously linked to neuroprotective effects observed for a Gotu Kola extract approved for use in a clinical trial. Our studies suggest that the possible therapeutic effects of the Gotu Kola plant extract in dementia treatment, at least partially, might be associated with compounds interacting with TrkB. The unique feature of this approach is its ability to fast screen potential drug leads using less explored transmembrane targets. This platform works as a drug-screening funnel at early stages of the drug discovery pipeline. Therefore, our approach will not only greatly benefit drug discovery processes using transmembrane proteins as targets but also allow for evaluation and validation of cellular pathways targeted by drug leads.
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