Uncaria Tomentosa Research Articles

Herbal-drug interaction through the pregnane X receptor

The interaction potential of Cynara scolymusL.,Mikania glomerataSpreng.,Rhamnus purshianaDC and Uncaria tomentosa(Willd. Ex Roem. & Schult.) with conventional drugs metabolized by the CYP3A4 metabolic route was tested in HeLa cell lines, using the in vitromodel of the hPXR. The herbal medicines C. scolymus(1.5 mg/mL dry extract) did not affect the receptor. On the other hand, M. glomerata(5.5 mg/mL dry extract), R. purshiana(1.5 mg/mL dry extract), and U. tomentosa(2.0 mg/mL dry extract) showed to be hPXR agonist, suggesting a potential interaction with the conventional drugs metabolized by the same isoforms of the CYP superfamily. The results from this study contribute to the use safer and more effective of these herbal medicines.

Development, optimization, and invitro evaluation of novel fast dissolving oral films (FDOF's) of Uncaria tomentosa extract to treat osteoarthritis

Fast dissolving oral films(FDOF's) are the popular dosage forms when placed in the oral cavity, disintegrate rapidly and dissolve to release the medication for improving oral absorption. Traditionally Uncaria tomentosa plant is used in the treatment of rheumatoid arthritis as Non-steroidal Anti-inflammatory agent along with analgesic properties. The plant extract is reported to be used in low dose as analgesic and anti-inflammatory agent in Rheumatoid Arthritis. No scientific data was reported on Uncaria plant formulation as FDOF's for treating osteoarthritis. This study aims to formulate fast oral dissolving film(FDOFs) Uncaria tomentosa bark extract and evaluate using Invitro studies for osteoarthritis. About 14 formulations were prepared using standard Box Behnken design protocol for optimization using the natural film formers, synthetic polymers, super disintegrants, plasticizers as independent variables with folding endurance and disintegration time as dependent variables by solvent casting method. Further the formulation characteristics including physical and mechanical behavior of films and drug release behavior was evaluated. The 3D countour plots and response curves suing the design expert software were investigated which proved that the optimized oral dissolving films of extract with Pullalan gum, HPMC (polymers), Propylene glycol, PEG 400 (Co-solvents) and Croscarmellose sodium (super Disintegrant) are stable and uniform with formulation characteristics. The drug release rates prove that F5 and F13 formulations showed 99.90% drug release within 30 min following first order kinetics with satisfactory mechanical properties. The study results suggest that the fast dissolving oral films of Uncaria tomentosa extract is novel, attractive and alternative to the available marketed products resulting in improved patient adherence in treatment of osteoarthritis.

Identification of PXR Activators from Uncaria Rhynchophylla (Gou Teng) and Uncaria Tomentosa (Cat's Claw).

Uncaria rhynchophylla (Gou Teng) and Uncaria tomentosa (cat's claw) are frequently used herbal supplements in Asia and America, respectively. Despite their common usage, information is limited regarding potential herb-drug interactions associated with Gou Teng and cat's claw. The pregnane X receptor (PXR) is a ligand-dependent transcription factor that regulates cytochrome P450 3A4 (CYP3A4) expression and contributes to some known herb-drug interactions. A recent study found that Gou Teng induces CYP3A4 expression, but its mechanism is unknown. Cat's claw has been determined as a PXR-activating herb, but the PXR activators in cat's claw have not been identified. Using a genetically engineered PXR cell line, we found that the extracts of Gou Teng and cat's claw can dose-dependently activate PXR and induce CYP3A4 expression. We next used a metabolomic approach to profile the chemical components in the extracts of Gou Teng and cat's claw followed by screening for PXR activators. Four compounds, isocorynoxeine, rhynchophylline, isorhynchophylline, and corynoxeine, were identified as PXR activators from both Gou Teng and cat's claw extracts. In addition, three more PXR activators were identified from the extracts of cat's claw, including isopteropodine, pteropodine, and mitraphylline. All seven of these compounds showed the half-maximal effective concentration <10 µM for PXR activation. In summary, our work determined Gou Teng as a PXR-activating herb and discovered novel PXR activators from Gou Teng as well as cat's claw. SIGNIFICANCE STATEMENT: This study's data can be used to guide the safe use of Gou Teng and cat's claw by avoiding PXR-mediated herb-drug interactions.

Effect of Uncaria Tomentosa leaves extract on Histopathological changes in Murine Model of Asthma

Background: Bronchial asthma is the leading respiratory disease among all chronic inflammatory conditions. Due to various causative factors, it's incidence has been drastically increased over last decades. Despite the availability of potent anti inflammatory &amp; bronchodilator therapies, there is a need to find new pharmacological molecules possessing targeted mechanism and lesser side effects towards it's pathogenesis. In this study, Uncaria tomentosa belonging to family Rubiacae was selected to evaluate anti asthmatic effect owing to it's specific anti inflammatory properties. Aim: To evaluate the effectiveness of uncaria tomentosa leaves on respiratory smooth muscles in case of bronchospasm and constriction. Study Design: Experimental comparative type Place and Duration of Research: University of health sciences. Duration of study is 1 year Methodology: Ethanolic extract of Uncaria tomentosa leaves was prepared according to the protocol. We took 24 male mice and divided them equally in groups of four. These groups represented control, diseased, UT (Uncaria tomentosa) leaves and MP (Methylprednisolone) treated. Bronchial asthma was induced by Ova sensitization on day 0 and OVA challenge on day 14 followed by treatment with UT leaves extract (200µg/animal/day) and MP (15mg/kg b.w) for next 7 days. Animals were sacrificed and lungs were removed to check histopathological findings. Results: The animals belonging to diseased group showed all histopathological features suggestive of bronchial asthma as compared to control group. Inflammatory score, epithelial cell hyperplasia and vascular congestion was found to be significantly decreased in both treatment groups. Conclusion: UT leave extract may possess anti asthmatic activity comparable to Methylprednisolone. Keywords: Phosphate Buffer Saline PBS, Tumor necrosis factor alpha TNF-α, Methylprednisolone MP, Uncaria tomentosa UT

Phytochemical Screening and Antioxidant Activity of Uncaria tomentosa Extract

Background: Uncaria tomentosa is a traditional medicinal herb with antiviral, antioxidant, immunostimulating, anti-inflammatory, and anticancer effects. Objective: The present study was conducted to evaluate the antioxidant capacity in vitro and in vivo and the phytochemical analysis of Uncaria tomentosa. Materials and Methods: The plant extract was screened for phytochemical compounds and antioxidant capacity in vitro using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method and in vivo using acetic acid-induced colitis. Colitis was induced in rats by transrectal administration (5 mL/kg) of 4% (v/v) acetic acid. Forty adult albino rats were divided into four groups: control group, acetic acid group, acetic acid + sulfasalazine (100 mg/kg/day) group, and acetic acid + Uncaria tomentosa extract (250 mg/kg/day) group. After inducing colitis, sulfasalazine and Uncaria tomentosa extract were given orally for 10 days. Data were statistically analyzed, and P &lt; 0.05 was considered statistically significant throughout the study. Results: Preliminary phytochemical study showed that Uncaria tomentosa extract contains flavonoids, phenols alkaloids, saponin, and terpenoids. In the DPPH assay, the extract exhibited considerable antioxidant capacity in a dose-dependent manner. Also, Uncaria tomentosa extract dramatically decreased oxidative stress parameters, such as myeloperoxidase enzyme activity and malondialdehyde in colonic tissue. Moreover, Uncaria tomentosa treatment attenuated macroscopic colonic scores and histopathological changes induced by acetic acid. Conclusion: The findings of this study show that Uncaria tomentosa extract could be a source of natural antioxidants and may have a therapeutic effect on ulcerative colitis.

Immunostimulating activity of Uncaria tomentosa in RAW 264.7 macrophages.

Uncaria tomentosa is a plant native to the Amazon that has immunomodulatory and antitumor properties due to the alkaloids found in the plant, being able to modify the immune response by potentiating or suspending the action of cytokines secreted by macrophages that induce the immune response, either by the classical route (M1) or through the alternative route (M2). Macrophages activated by M1 convert L-arginine into L-citrulline and nitric oxide (NO), whereas macrophages activated by the M2 pathway use the enzymatic activity of arginase to convert the same substrate into L-ornithine and urea. The aim of this work was to evaluate the immunostimulating activity of the crude hydroalcoholic extract from the bark of the U. tomentosa stem in RAW 264.7 macrophages. Concentrations of 0.2, 0.1 and 0.05 mg/mL of U. tomentosa extract associated with LPS, INF-γ and IL-4 inducers were tested by determining NO production and arginase enzyme activity. Nitric oxide production was enhanced by the extract when associated with LPS and LPS + INF-γ inducers. In the activity of the arginase enzyme, the extract decreased the stimulation of IL-4 on the enzyme, mainly at 0.2 mg/mL concentration. Therefore, it is concluded that the crude hydroalcoholic extract of the stem bark of U. tomentosa in RAW 264.7 cells, at a concentration of 0.2 mg/mL, showed considerable pro-inflammatory activity.

Pengujian Kualitas Parameter Fisika Kimia dan Kandungan Total Fenol dari Teh Herbal Cakar Kucing (Uncaria tomentosa Wild. Ex Schult) Sebagai Minuman Fungsional

The many side effects of consuming chemical-based drugs in maintaining human health have led to a tendency to return to nature. Consumption of medicinal plants in fresh or dried form has been considered to minimize side effects. This research will examine the feasibility of cat's claw (Uncaria tomentosa Wild. Ex Schult) tea as a functional drink based on physicochemical parameters and total phenol content. The physicochemical parameters tested included pH, water content, ash content and organoleptic examination of herbal teas including taste, odor and color of the brewed solution, while the total content of phenolic compounds was carried out based on the Folin–Ciocalteu method. Organoleptic examination showed a characteristic odor of the leaves, such as the smell of herbal teas in general with a bland and astringent taste, and the juice of the solution was yellowish green. The results of the physicochemical parameter test showed that the pH of the solution was 6.9, the water content was 7.7, the ash content was 8.00%, while the total phenol content measured was 68.77 mg GAE/g sample. The physicochemical parameters measured from the testing of cat's claw herbal tea in this study met the quality requirements of dry tea according to SNI No 3836 BSN 2013

A comprehensive review on medicinal plants possessing antioxidant potential.

Many research studies have proposed that about two-thirds of the medicinal plant species of the world possess significant antioxidant potential. Antioxidants are very beneficial as they decrease oxidative stress (OS) in cells and hence play their role in management as well as treatment of numerous diseases like cancers, cardiovascular diseases, as well as many inflammatory illnesses. This review comprises the antioxidant potential of numerous parts of medicinal plants like leaves, stems, roots, seeds, fruits, as well as bark. Synthetic antioxidants named butylated hydroxyanisole (BHA) as well as butylated hydroxytoluene (BHT) are extensively employed in foods because of their role as food preservatives. Several natural antioxidants have better efficacy as compared to synthetic antioxidants. These medicinal plants include Geranium sanguineum L., Rheum ribes L., Diospyros abyssinica, Sargentodoxa cuneata Rehd. Et Wils, Pistacia lentiscus, Ficus microcarpa L. fil., Polyalthia cerasoides (Roxb.) Bedd, Cunn, Teucrium polium L., Crataeva nurvala Buch-Ham., Urtica dioica L., Dracocephalum moldavica L., Momordica Charantia L., Acacia auriculiformis A., Bidens pilosa Linn. The Lamiaceae species, Radiata, Leea indica, Pelargonium endlicherianum, Salvia officinalis L., and Uncaria tomentosa (Willd.) DC. The literature study disclosed more side effects of synthetic antioxidants (including food additives) in comparison with natural antioxidants and for prevention of many diseases.

Study on the Effectiveness of Two Biopolymer Coagulants on Turbidity and Chemical Oxygen Demand Removal in Urban Wastewater.

The present study investigated the effectiveness of two biopolymer coagulants on turbidity and chemical oxygen demand removal in urban wastewater. The biopolymers were produced from vegetal biomass using the mucilage extracted from Opuntia robusta cladodes, and Uncaria tomentosa leaves. Opuntia robusta is an abundant species in Mexico, which is not edible. Uncaria tomentosa is an exotic invasive species in Mexico and other countries, which negatively affects the ecosystems where it is introduced. A combined experimental design of mixture-process was selected to evaluate the effectiveness of both biopolymer coagulants regarding aluminum sulfate (conventional chemical coagulant). Results showed turbidity and chemical oxygen demand removal efficiencies of 42.3% and 69.6% for Opuntia robusta and 17.2% and 39.4% for Uncaria tomentosa biopolymer coagulant, respectively, at a dose of 200 mg/L. Furthermore, optimum conditions from the experimental design to reach the maximum turbidity and chemical oxygen demand removal were obtained at an Opuntia robusta biopolymer coagulant concentration of 10 mg/L, showing removal efficiencies of 68.7 ± 1.7% and 86.1 ± 1.4%, respectively. These results support using Opuntia robusta as an alternative biopolymer coagulant in urban wastewater treatment.

The Potency of the Genus Uncaria from East Borneo for Herbal Medicine Purposes: A Mini-review

Uncaria is a genus of plants that are widely distributed in the tropics. There are about 5 of the 38 species of this genus growing in the tropical rain forests of East Borneo, Indonesia. For a long time, Uncaria is commonly used as a traditional medicine to treat various diseases by the Dayak tribe in Kalimantan, traditional people believe that Uncaria may be cured cancer, tumors, mioms, and cycts. Based on previous studies, the activity of the genus Uncaria has been widely reported such as cytotoxic, antimicrobial, antioxidant, antidiabetic, and thrombolytic activities. This article aims to summarize the potential of the Uncaria genus, focusing on 5 species from East Borneo, namely Uncaria nervosa, Uncaria longiflora, Uncaria gambir, Uncaria tomentosa and Uncaria cordata. The method used in this article is a literature study by collecting previous research articles related to the Uncaria genus. The results of the literature study show that the Uncaria genus in East Borneo has many secondary metabolites with diverse chemical structures that show good biological potential so that they can be used as broad and promising insights for drug discovery and development. This paper is also expected to provide input for the policy of conservation of medicinal plants in the forests of East Borneo.

Cortex Uncariae: A Review on Pharmacology, Toxicology, Precautions, and Dosage

Cortex Uncariae is the stem of Uncaria tomentosa plant, which belongs to the family Rubiaceae. Cat's thorn and unha de gato are the famous names of Cortex Uncariae. Uncaria tomentosa plant is widely geographically distributed in Central and South American countries. The aim of this review was to focus on pharmacology, toxicology, precautions, and dosage of Cortex Uncariae. The indole alkaloids such as speciophylline, mitraphylline, pteropodine, uncarine F, and isomitraphylline, as well as tetracyclic alkaloids oxindoles such as isorhynchophylline and rhynchophylline are the major Cortex Uncariae chemical constituents. There are many medical applications of Cortex Uncariae, such as immunostimulant agents, increases the white blood cells and immunity, treatment of gastrointestinal ulcers, rheumatism, arthritis, viral infection, urinary tract infections, fever, asthma, abscesses, high blood pressure, high blood glucose, and high total cholesterol. Pharmacology of Cortex Uncariae includes experimental pharmacology and clinical pharmacology. Experimental pharmacology contains anti-inflammatory, antidepressant, neuroprotection, antitumor, immune-stimulating, and anti-obesity activities, while clinical pharmacology contains immune-stimulating activity. No acute or chronic toxicity was recorded after Cortex Uncariae water extract administration. Cortex Uncariae extract did not accompany loss of food intake, body or organ weight decrease, and no histopathological changes were recorded in the main body organs such as kidney, liver, spleen, and heart after Cortex Uncariae intake. Cortex Uncariae must store in a closely black container to avoid heat and light. In conclusion, Cortex Uncariae had anti-inflammatory, antidepressant and neuroprotection, antitumor, immune-stimulating, anti-inflammatory, and anti-obesity activities without acute or chronic toxicity.

Application of the Extracts of Uncaria tomentosa in Endodontics and Oral Medicine: Scoping Review.

Background: The main purpose of endodontic treatment is to eliminate the bacteria that are responsible for the contamination and infection of the internal surfaces in order to resolve any pulp or periapical pathology. In fact, some bacteria, such as Enterococcus faecalis, can escape the action of root canal irrigants by aggregating into a biofilm and penetrating deeply into the dentinal tubules. Uncaria tomentosa is a plant belonging to the Rubiaceae family and also commonly known as cat’s claw due to the shape and position of the spines; it is a traditional Peruvian medicinal plant of Amazonian origin. Applications in the dental field have been described both in the prevention and treatment of stomatitis and as an antibacterial and anti-inflammatory agent; it has also been investigated as an additive in irrigants and specifically as gels in endodontic cements. The aim of this scoping review is to summarize all the scientific evidence on the possible applications of Uncaria tomentosa extracts in endodontics and, more generally, in oral medicine, in order to understand whether the active ingredients extracted from Uncaria tomentosa can bring a real advantage in endodontics, in the reduction of endodontic failures and in the onset of recurrent endodontic lesions. Methods: The scoping review was carried out strictly following the PRISMA-ScR checklist; the search was carried out on five databases (PubMed, Scopus, Science Direct, EBSCO and Web of Science) and a register (Cochrane library). Results: The research produced a number of bibliographic sources totaling 2104. With the removal of duplicates, 670 were obtained; potentially eligible articles amounted to 23, of which only seven in vitro studies (four microbiological studies), five clinical studies (three randomized trials) and a case report were included. Conclusions: From the data in the literature, it can be stated that the active ingredients present in Uncaria tomentosa could represent an interesting product to be used in the endodontic field, both in endocanalary cements and as a gel.

Preparation and characterization of microcapsules loaded with polyphenols-enriched Uncaria tomentosa extract using spray-dryer technique

Preparation and characterization of microcapsules loaded with polyphenols-enriched Uncaria tomentosa extract using spray-dryer technique

Hybrid Nanoparticles of Proanthocyanidins from Uncaria tomentosa Leaves: QTOF-ESI MS Characterization, Antioxidant Activity and Immune Cellular Response.

Previous studies in Uncaria tomentosa have shown promising results concerning the characterization of polyphenols with leaves yielding more diverse proanthocyanidins and higher bioactivities values. However, the polyphenols-microbiota interaction at the colonic level and their catabolites avoid the beneficial effects that can be exerted by this medicinal plant when consumed. In this regard, a new generation of hybrid nanoparticles has demonstrated improvements in natural compounds’ activity by increasing their bioavailability. In this line, we report a detailed study of the characterization of a proanthocyanidin-enriched extract (PA-E) from U. tomentosa leaves from Costa Rica using UPLC-QTOF-ESI MS. Moreover, two types of hybrid nanoparticles, a polymeric-lipid (F-1) and a protein-lipid (F-2) loaded with PA-E were synthesized and their characterization was conducted by dynamic light scattering (DLS), attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FT-IR), high-resolution transmission electron microscopy (HR-TEM), and encapsulation efficiency (%EE). In addition, in vitro release, antioxidant activity through 2,2-diphenyl-1-picrylhidrazyl (DPPH) as well as in vivo delayed-type hypersensitivity (DTH) reaction was evaluated. Results allowed the identification of 50 different compounds. The PA-E loaded nanoparticles F-1 and F-2 achieved encapsulation efficiency of ≥92%. The formulations exhibited porosity and spherical shapes with a size average of 26.1 ± 0.8 and 11.8 ± 3.3 nm for F-1 and F-2, respectively. PA-E increased its release rate from the nanoparticles compared to the free extract in water and antioxidant activity in an aqueous solution. In vivo, the delayed-type hypersensitive test shows the higher immune stimulation of the flavan-3-ols with higher molecular weight from U. tomentosa when administered as a nanoformulation, resulting in augmented antigen-specific responses. The present work constitutes to our knowledge, the first report on these bioactivities for proanthocyanidins from Uncaria tomentosa leaves when administrated by nanosystems, hence, enhancing the cellular response in mice, confirming their role in immune modulation.

Computational Study of the Phytochemical Constituents from Uncaria tomentosa Stem Bark against SARS-CoV-2 Omicron Spike Protein

The SARS-CoV-2 Omicron variant has spread rapidly and is considered the predominant variant in the world, and its main characteristic is related to evade immunity from natural infection or vaccines, due to its multiple mutations in the spike protein. On the other hand, medicinal plants have been used as alternatives therapies to ameliorate some signs and symptoms in COVID-19, and in our previous work, the cat’s claw (Uncaria tomentosa) stem bark has been studied in vitro and showed antiviral activity on SARS-CoV-2 as well as in silico studies on the 3CLpro protein and as disruptor between the ACE-2 human receptor and the spike protein. The aim in this computational study was to determine the main phytochemical constituents from U. tomentosa stem bark against the SARS-CoV-2 Omicron spike protein based on molecular modeling. A molecular docking was carried out on the isolated phytochemicals in a previous work against the SARS-CoV-2 Omicron spike protein-binding domain (PDB ID: 7T9K). Next, a molecular dynamic study was carried out to monitor the stability during the MD simulations. As results proanthocyanidin-C1 (-10.76 kcal/mol), quinovic acid-type 2 (-9.86 kcal/mol), and proanthocyanidin-B2 (-9.82 kcal/mol) were the constituents with the best binding free energy on the SARS-CoV-2 Omicron spike protein, and the best compound was stable during the dynamic simulation under physiological conditions. It is concluded that the anthocyanidin-based compounds determined in the stem bark ethanol extract could be responsible for the potential antiviral activity on SARS-CoV-2 Omicron variant, and the proanthocyanidin-C1 emerged as a powerful candidate to combat new variants.

Uncaria tomentosa (Willd. ex Schult.): Focus on Nutraceutical Aspects

: Medicinal plants have been globally exploiting as an alternative to chemical drugs in the treatment of several diseases due to low unwanted side effects, environmentally friendly nature, and low production costs. Therefore, it is important to analyze the therapeutic properties of various medicinal plants to understand their potential bioactivity. Uncaria tomentosa is one of these medicinal plants with many health-promoting effects. Although the geographical resources of cat's claw go back to the remote tropics of the Amazon, industrialized countries use the plant extensively in trade. Various parts of the plants such as flowers, leaves, Stem, hooks, and seeds are mainly used medicinally to treat inflammation, asthma, allergies, skin impurities, microbial infections, neurodegenerative diseases, cancer, cirrhosis, gastrointestinal disorders, arthritis, heart disease, rheumatism, and fever. The endpoint of this review article is to prospectively scrutinize in vitro and in vivo the therapeutic potential of this plant, especially in terms of its nutritional applications and healthbeneficial effects.

Traditional medicinal plants used by hypertensive patients in Belize: a qualitative evaluation of beliefs and practices

BackgroundBelize is rich in rainforest and vast medicinal plants that have the potential for drug discoveries. Few studies have examined the use of medicinal plants in the management of chronic diseases in Belize. The present study appraised indigenous Belizeans' opinions, beliefs, and practices of medicinal plants used for hypertension management. Twenty-four hypertensive patients were interviewed using a semi-structured interview guide from January to May 2019. Interview results were transcribed using Microsoft Excel and loaded into qualitative data analysis (QDA) Miner Lite version 2.0.6 online software for coding. The integrated themes and sub-themes generated were presented in narrative passages and used to summarize study findings on medicinal plants used in the management of hypertension in Belize.ResultsFifteen medicinal plants belonging to 15 plant families were reported by the participants as medicinal plants used to manage hypertension. The plants include Annona muricata, Artocarpus altilis, Cecropia peltata, Ananas comosus, Cymbopogon andropogoneae, Uncaria tomentosa, Allium sativum, Bixa orellana, Moringa oleifera, Momordica charantia, and Cassia grandis. Leaves were the most commonly used plant part; decoction was the most common method of preparation, while ½ to 1 glass was the daily recommended dose. Mild side effects were reported, while antioxidant activity was the perceived efficacy.ConclusionHypertensive patients in Belize opined that medicinal plants and herbs were efficacious in lowering blood pressure, as evidenced by home monitoring and regular checkups at the hospital. They also reported minimal side effects in the use of the medicinal plants. There is a need for a comprehensive evaluation of Belize’s medicinal plants to unravel their potential for drug discovery.

Identifying potential natural inhibitors of Brucella melitensis Methionyl-tRNA synthetase through an in-silico approach

Brucellosis is an infectious disease caused by bacteria of the genus Brucella. Although it is the most common zoonosis worldwide, there are increasing reports of drug resistance and cases of relapse after long term treatment with the existing drugs of choice. This study therefore aims at identifying possible natural inhibitors of Brucella melitensis Methionyl-tRNA synthetase through an in-silico approach. Using PyRx 0.8 virtual screening software, the target was docked against a library of natural compounds obtained from edible African plants. The compound, 2-({3-[(3,5-dichlorobenzyl) amino] propyl} amino) quinolin-4(1H)-one (OOU) which is a co-crystallized ligand with the target was used as the reference compound. Screening of the molecular descriptors of the compounds for bioavailability, pharmacokinetic properties, and bioactivity was performed using the SWISSADME, pkCSM, and Molinspiration web servers respectively. The Fpocket and PLIP webservers were used to perform the analyses of the binding pockets and the protein ligand interactions. Analysis of the time-resolved trajectories of the Apo and Holo forms of the target was performed using the Galaxy and MDWeb servers. The lead compounds, Strophanthidin and Isopteropodin are present in Corchorus olitorius and Uncaria tomentosa (Cat's-claw) plants respectively. Isopteropodin had a binding affinity score of -8.9 kcal / ml with the target and had 17 anti-correlating residues in Pocket 1 after molecular dynamics simulation. The complex formed by Isopteropodin and the target had a total RMSD of 4.408 and a total RMSF of 9.8067. However, Strophanthidin formed 3 hydrogen bonds with the target at ILE21, GLY262 and LEU294, and induced a total RMSF of 5.4541 at Pocket 1. Overall, Isopteropodin and Strophanthidin were found to be better drug candidates than OOU and they showed potentials to inhibit the Brucella melitensis Methionyl-tRNA synthetase at Pocket 1, hence abilities to treat brucellosis. In-vivo and in-vitro investigations are needed to further evaluate the efficacy and toxicity of the lead compounds.

Beneficial effects of three natural products for the treatment of denture stomatitis

Aim: To evaluate the effect of three natural antifungal agents combined with routine denture care on the treatment of DS, using a quantitative mycological culture analysis. Methods: Thirty denture wearers with denture stomatitis DS were treated using five substances: sterile distilled water (G1), nystatin oral suspension (G2), 20% alcoholic extract propolis (G3), Punica granatum Linné gel (G4), and Uncaria tomentosa gel (G5). The substances were used 3 times a day for 14 days. Quantitative mycological culture analysis of samples collected from the palatal mucosa was performed at three stages: before treatment (T0), after 14 days of treatment (T1), and 30 days after treatment completion (T2). Data were evaluated using Kruskal-Wallis and Friedman tests (p &lt; 0.05). Results: Palatal mucosa intragroup analysis showed a significant reduction of Candida CFU/mL values for all groups at T1 compared to T0 (p &lt; 0.05). However, they did not present statistical differences when comparing T1 and T2 (p &gt; 0.05). The intergroup analysis demonstrated that there are no statistical differences, regardless of the evaluation time (p &gt; 0.05). Conclusion: The natural products tested showed a satisfactory result on DS treatment, which proved to be equivalent to conventional topical therapy with nystatin and to treatment using only regular oral hygiene procedures.

GlucoMedix®, an extract of Stevia rebaudiana and Uncaria tomentosa, reduces hyperglycemia, hyperlipidemia, and hypertension in rat models without toxicity: a treatment for metabolic syndrome

BackgroundThe objective of this in vivo study is to evaluate in five rat models the pharmacologic effects and toxicity of a commercial hydro-alcoholic extract, GlucoMedix®, derived from Stevia rebaudiana and the pentacyclic chemotype of Uncaria Tomentosa (Willd.) DC, for use as a treatment for metabolic syndrome. The extract contains phytochemicals of Stevia (e.g., steviol glycosides) and Uncaria (e.g., pentacyclic oxindole alkaloids, but lacks tetracyclic oxindole alkaloids).MethodsThe pharmacologic assessments in three rat models include reductions in chemically induced hyperglycemia, hyperlipidemia (cholesterol and triglycerides), and hypertension, all of which are comorbidities of metabolic syndrome. Acute toxicity and 28-day subacute toxicity were assessed in rat models at doses higher than those used in the efficacy models.ResultsThe acute oral toxicity was evaluated in Holtzman rats and the extract did not produce acute toxic effects or lethality, with the LD50 > 5000 mg/kg (extract wet weight). Furthermore, subacute oral toxicity was evaluated in rats for 28 days at daily doses as high as 2000 mg/kg without toxicity or abnormal clinical chemistry or hematological effects. Daily oral doses of 250 - 1000 mg/kg were used to evaluate the treatment effects in hyperglycemic (alloxan-induced and glibenclamide-controlled), hyperlipidemic (cholesterol-induced and atorvastatin-controlled), and hypertensive (L-NAME-induced and enalapril-controlled) rat models. Alloxan-induced hyperglycemia was reduced in a dose-dependent manner within 28 days or less. Cholesterol-induced hyperlipidemic rats exhibited dose-dependent reductions in cholesterol and triglycerides at 21 days. Furthermore, GlucoMedix® produced a dose-dependent decrease in systolic and diastolic arterial blood pressure in L-NAME-induced hypertensive rats at 28 days.ConclusionsThe five in vivo rat models revealed that the all-natural phytotherapy GlucoMedix® is a safe and effective treatment for hyperglycemia, hyperlipidemia, and hypertension. This extract is expected to affect multiple comorbidities of metabolic syndrome, without any acute or subacute oral toxicity in humans. Although multiple prescription drugs are well known for the treatment of individual comorbidities of metabolic syndrome, no drug monotherapy concurrently treats all three comorbidities.