MyMedR

Displaying publications 21 - 27 of 27 in total

Abstract:

Sort:

Fulltext Optimization of a Luteolin-Loaded TPGS/Poloxamer 407 Nanomicelle: The Effects of Copolymers, Hydration Temperature and Duration, and Freezing Temperature on Encapsulation Efficiency, Particle Size, and Solubility

Mod Razif MRF, Chan SY, Widodo RT, Chew YL, Hassan M, Hisham SA, et al.

Cancers (Basel), 2023 Jul 24;15(14).
PMID: 37509402 DOI: 10.3390/cancers15143741

BACKGROUND: Luteolin is a flavonoid compound that has been widely studied for its various anti-cancer properties and sensitization to multidrug-resistant cells. However, the limited solubility and bioavailability of Lut hindered its potential clinical use. Theoretically, the combination of this compound with vitamin E TPGS and poloxamer 407 can produce a synergistic effect to enhance tumor apoptosis and P-glycoprotein inhibition. This study aimed to develop and optimize vitamin E TPGS/Poloxamer 407 micelles loaded with luteolin through investigating certain factors that can affect the encapsulation efficiency and particle size of the micelle.
METHODS: A micelle was prepared using the film hydration method, and the micellar solution was lyophilized. The cake formed was analyzed. The factors investigated include the concentrations of the surfactants, ratio of vitamin E TPGS/Poloxamer 407, temperature of the hydrating solution, duration of hydration, and freezing temperature before lyophilization. The effects of these factors on the encapsulation efficiency and particle size of the micelle were also studied. The encapsulation efficiency was measured using a UV-Vis spectrophotometer, while particle size was measured using dynamic light scattering.
RESULTS: The optimized micelle was found to have 90% encapsulation efficiency with a particle size of less than 40 nm, which was achieved using a 10% concentration of surfactants at a vitamin E TPGS/Poloxamer 407 ratio of 3:1. The optimized temperature for hydrating the micellar film was 40 °C, the optimized mixing time was 1 h, and the optimized freezing temperature was -80 °C. The solubility of the luteolin-loaded micelles increased 459-fold compared to pure Lut in water. The critical micelle concentration of the vitamin E TPGS/Poloxamer 407 micelle was 0.001 mg/mL, and the release study showed that luteolin-loaded micelles exhibited sustained release behavior. The release of luteolin from a micelle was found to be higher in pH 6.8 compared to pH 7.4, which signified that luteolin could be accumulated more in a tumor microenvironment compared to blood.
CONCLUSION: This study demonstrated that several factors need to be considered when developing such nanoparticles in order to obtain a well-optimized micelle.
Fulltext Comparative Investigation of Chemical Constituents of Kernels, Leaves, Husk, and Bark of Juglans regia L., Using HPLC-DAD-ESI-MS/MS Analysis and Evaluation of Their Antioxidant, Antidiabetic, and Anti-Inflammatory Activities

Bourais I, Elmarrkechy S, Taha D, Badaoui B, Mourabit Y, Salhi N, et al.

Molecules, 2022 Dec 16;27(24).
PMID: 36558122 DOI: 10.3390/molecules27248989

Leaves, husk, kernels, and bark methanolic extracts of Juglans regia L. were tested for their in vitro antidiabetic, anti-inflammatory, and antioxidant activities. For these purposes, α-amylase and α-glucosidase were used as the main enzymes to evaluate antidiabetic activities. Moreover, lipoxidase and tyrosinase activities were tested to estimate anti-inflammatory properties. Antioxidant properties of Juglans regia L., extracts were determined using three different assays. Leaves extract has an important radical scavenging activity and a-amylase inhibition. Similarly, husk extracts showed high total phenolic content (306.36 ± 4.74 mg gallic acid equivalent/g dry extract) with an important α-amylase inhibition (IC50 = 75.42 ± 0.99 µg/mL). Kernels exhibit significant tyrosinase (IC50 = 51.38 ± 0.81 µg/mL) correlated with antioxidant activities (p < 0.05). Husk and bark extracts also showed strong anti-lipoxidase activities with IC50 equal to 29.48 ± 0.28 and 28.58 ± 0.35 µg/mL, respectively. HPLC-DAD-ESI-MS/MS analysis highlights the phenolic profile of methanolic extracts of Juglans regia L. plant parts. The identified polyphenols were known for their antioxidant, antidiabetic (dicaffeoyl-quinic acid glycoside in kernels), and anti-inflammatory (3,4-dihydroxybenzoic acid in leaves) activities. Further investigations are needed to determine molecular mechanisms involved in these effects as well as to study the properties of the main identified compounds.
Fulltext A Comprehensive Review of the Pharmacological Properties and Bioactive Components of Retama monosperma

El Yadini A, Elouafy Y, Amiri-Ardekani E, Shafiee M, Firouzi A, Sasani N, et al.

Molecules, 2023 Feb 10;28(4).
PMID: 36838696 DOI: 10.3390/molecules28041708

Retama monosperma L. (Boiss.) or Genista monosperma L. (Lam.), known locally as "R'tam", is a spontaneous and annual herb that belongs to the Fabaceae family. It is native to the Mediterranean regions, specifically in the desert areas and across the Middle Atlas in Morocco. This plant has been extensively used in folk medicine and it is rich in bioactive compounds, including polyphenols, flavonoids, and alkaloids. Current research efforts are focusing on the development of novel natural drugs as alternatives to various organic and non-organic chemical products from Retama monosperma. In addition, extract, and isolated compounds obtained from different parts of the chosen plant have been described to exhibit multiple biological and pharmacological properties such as antioxidant, anti-aging, anti-inflammatory, antihypertensive, anti-helminthic, disinfectant, diuretic, and hypoglycemic effects. The plant-derived extract also acts as an antimicrobial agent, which is highly efficient in the treatment of bacterial, viral, and fungal infections. Its antiproliferative effects are associated with some mechanisms, such as the inhibition of cell cycle arrest and apoptosis. In light of these assessments, we critically highlight the beneficial effects of the flowers, stems, seeds extracts, and isolated compounds from R. monosperma (L.) Boiss in human health care, industrial, and other applications, as well as the possible ways to be employed as a potential natural source for future drug discovery.
Fulltext Association between Physical Activity, Body Composition, and Metabolic Disorders in Middle-Aged Women of Ksar el Kebir (Morocco)

Harraqui K, Oudghiri DE, Mrabti HN, Hannoun Z, Lee LH, Assaggaf H, et al.

Int J Environ Res Public Health, 2023 Jan 18;20(3).
PMID: 36767104 DOI: 10.3390/ijerph20031739

This study aimed to examine the association between physical activity (PA), body composition, and metabolic disorders in a population of Moroccan women classified by menopausal status. This cross-sectional study comprised 373 peri- and postmenopausal women aged 45-64 years old. PA levels were assessed using the short version of the International Physical Activity Questionnaire (IPAQ-SF). Body composition and metabolic disorders were assessed by measurements of anthropometric and biological parameters: weight, body mass index (BMI), waist circumference (WC), hip circumference (HC), WC/HC ratio, percent body fat, systolic and diastolic blood pressure, fasting blood glucose, and serum lipids (total cholesterol (TC), triglycerides (TG), HDL-C, and LDL-C). Metabolic syndrome (MetS) was diagnosed according to the National Cholesterol Education Program Adult Treatment Panel III (NCEP-ATP III) criteria. Pearson correlations were used to test for associations. The mean total PA score of perimenopausal women was 1683.51 ± 805.36 MET-min/week, and of postmenopausal women was 1450.81 ± 780.67 MET-min/week. In all participants, peri- and postmenopausal women, PA was significantly and inversely associated with BMI, weight, percent body fat, HC, WC, and number of MetS components (p < 0.01), and with fasting blood glucose, TC, TG, and LDL-C (p < 0.05). The frequencies of metabolic disorders, obesity, abdominal obesity, type 2 diabetes, dyslipidemia, and MetS were significantly lower at moderate and intense levels of PA (p < 0.05), in also all participants. In middle-aged women, particularly those who are peri-menopausal, PA at moderate and intense levels is associated with more favorable body composition and less frequent metabolic disorders. However, in this particular study, PA does not appear to be associated with blood pressure and HDL-C concentrations. Future studies may be needed to further clarify these findings.
Fulltext Natural sources, biological effects, and pharmacological properties of cynaroside

Bouyahya A, Taha D, Benali T, Zengin G, El Omari N, El Hachlafi N, et al.

Biomed Pharmacother, 2023 May;161:114337.
PMID: 36812715 DOI: 10.1016/j.biopha.2023.114337

Cynaroside is a flavonoid, isolated from several species belonging to the Apiaceae, Poaceae, Lamiaceae, Solanaceae, Zingiberaceae, Compositae and other families and it can be extracted from seeds, roots, stems, leaves, barks, flowers, fruits, aerial parts, and the whole plant of these species. This paper discloses the current state of knowledge on the biological/pharmacological effects and mode of action to better understand the numerous health benefits of cynaroside. Several research works revealed that cynaroside could have beneficial effects on various human pathologies. Indeed, this flavonoid exerts antibacterial, antifungal, antileishmanial, antioxidant, hepatoprotective, antidiabetic, anti-inflammatory, and anticancer effects. Additionally, cynaroside exhibits its anticancer effects by blocking MET/AKT/mTOR axis by decreasing the phosphorylation level of AKT, mTOR, and P70S6K. For antibacterial activity, cynaroside reduces biofilm development of Pseudomonas aeruginosa and Staphylococcus aureus. Moreover, the incidence of mutations leading to ciprofloxacin resistance in Salmonella typhimurium was reduced after the treatment with cynaroside. In addition, cynaroside inhibited the production of reactive oxygen species (ROS), which reduced the damage to mitochondrial membrane potential caused by hydrogen peroxide (H2O2). It also enhanced the expression of the anti-apoptotic protein Bcl-2 and lowered that of the pro-apoptotic protein Bax. Cynaroside abrogated the up-regulation of c-Jun N-terminal kinase (JNK) and p53 protein expression triggered by H2O2. All these findings suggest that cynaroside could be used to prevent certain human diseases.
Enhanced Wound Healing with Rhodiola rosea Phytosomal Gel: Extraction, Formulation, and In vivo Evaluation

Kalusalingam A, Khan A, Kanakal MM, Abbas SA, Long CM, B T, et al.

Curr Pharm Des, 2025 Mar 20.
PMID: 40114578 DOI: 10.2174/0113816128359150250211053431

BACKGROUND: This study explores the formulation and effectiveness of a Rhodiola rosea phytosomal gel for enhancing wound healing.
OBJECT: The ethanolic extract of Rhodiola rosea roots, rich in bioactive compounds like alkaloids and flavonoids, was optimized into a phytosomal complex to improve absorption and dermal retention.
METHOD: Characterization through GC-MS revealed compounds, such as 2-Heptadecenal and Bicyclo[ 4.1.0]Heptane and 7-Pentyl. FTIR confirmed the successful encapsulation within the phospholipid bilayer, while SEM showed smooth, spherical particles.
RESULT: The Box-Behnken design optimized formulation parameters, achieving high yield (92.64%), small particle size (355 nm), and high entrapment efficiency (93.98%). In vitro release studies displayed a consistent release profile, aligning with Zero-order and Hixson-Crowell models. In vivo evaluation on Wistar rats showed that the phytosomal gel significantly enhanced wound healing, achieving 98.16% wound reduction by day 14, compared to 95.17% for R. rosea extract and 97.13% for standard treatment. Histopathological analysis demonstrated complete tissue regeneration and well-organized collagen fibers in the phytosomal gel group.
CONCLUSION: This research highlights the potential of Rhodiola rosea phytosomal gel as an effective wound healing therapy, with future studies suggested for extended stability tests and human skin permeation studies.
Baicalein as Promising Anticancer Agent: A Comprehensive Analysis on Molecular Mechanisms and Therapeutic Perspectives

Morshed AKMH, Paul S, Hossain A, Basak T, Hossain MS, Hasan MM, et al.

Cancers (Basel), 2023 Apr 03;15(7).
PMID: 37046789 DOI: 10.3390/cancers15072128

Despite significant therapeutic advancements for cancer, an atrocious global burden (for example, health and economic) and radio- and chemo-resistance limit their effectiveness and result in unfavorable health consequences. Natural compounds are generally considered safer than synthetic drugs, and their use in cancer treatment alone, or in combination with conventional therapies, is increasingly becoming accepted. Interesting outcomes from pre-clinical trials using Baicalein in combination with conventional medicines have been reported, and some of them have also undergone clinical trials in later stages. As a result, we investigated the prospects of Baicalein, a naturally occurring substance extracted from the stems of Scutellaria baicalensis Georgi and Oroxylum indicum Kurz, which targets a wide range of molecular changes that are involved in cancer development. In other words, this review is primarily driven by the findings from studies of Baicalein therapy in several cancer cell populations based on promising pre-clinical research. The modifications of numerous signal transduction mechanisms and transcriptional agents have been highlighted as the major players for Baicalein's anti-malignant properties at the micro level. These include AKT serine/threonine protein kinase B (AKT) as well as PI3K/Akt/mTOR, matrix metalloproteinases-2 & 9 (MMP-2 & 9), Wnt/-catenin, Poly(ADP-ribose) polymerase (PARP), Mitogen-activated protein kinase (MAPK), NF-κB, Caspase-3/8/9, Smad4, Notch 1/Hes, Signal transducer and activator of transcription 3 (STAT3), Nuclear factor erythroid 2-related factor 2 (Nrf2)/Kelch-like ECH-associated protein-1 (Keap 1), Adenosine monophosphate-activated protein kinase (AMPK), Src/Id1, ROS signaling, miR 183/ezrin, and Sonic hedgehog (Shh) signaling cascades. The promise of Baicalein as an anti-inflammatory to anti-apoptotic/anti-angiogenic/anti-metastatic medicinal element for treating various malignancies and its capability to inhibit malignant stem cells, evidence of synergistic effects, and design of nanomedicine-based drugs are altogether well supported by the data presented in this review study.