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1.
Heliyon ; 10(9): e29718, 2024 May 15.
Article En | MEDLINE | ID: mdl-38694079

Diabetes is a complex disease that affects a large percentage of the world's population, and it is associated with several risk factors. Self-management poses a significant challenge, but natural sources have shown great potential in providing effective glucose reducing solutions. Flavonoids, a class of bioactive substances found in different natural sources including medicinal plants, have emerged as promising candidates in this regard. Indeed, several flavonoids, including apigenin, arbutin, catechins, and cyanidin, have demonstrated remarkable anti-diabetic properties. The clinical effectiveness of these flavonoids is linked to their potential to decrease blood glucose concentration and increase insulin concentration. Thus, the regulation of certain metabolic pathways such as glycolysis and neoglycogenesis has also been demonstrated. In vitro and in vivo investigations revealed different mechanisms of action related to flavonoid compounds at subcellular, cellular, and molecular levels. The main actions reside in the activation of glycolytic signaling pathways and the inhibition of signaling that promotes glucose synthesis and storage. In this review, we highlight the clinical efficiency of natural flavonoids as well as the molecular mechanisms underlying this effectiveness.

2.
BMC Infect Dis ; 24(1): 484, 2024 May 10.
Article En | MEDLINE | ID: mdl-38730292

Thromboembolic (TE) complications [myocardial infarction (MI), stroke, deep vein thrombosis (DVT), and pulmonary embolism (PE)] are common causes of mortality in hospitalised COVID-19 patients. Therefore, this review was undertaken to explore the incidence of TE complications and mortality associated with TE complications in hospitalised COVID-19 patients from different studies. A literature search was performed using ScienceDirect and PubMed databases using the MeSH term search strategy of "COVID-19", "thromboembolic complication", "venous thromboembolism", "arterial thromboembolism", "deep vein thrombosis", "pulmonary embolism", "myocardial infarction", "stroke", and "mortality". There were 33 studies included in this review. Studies have revealed that COVID-19 patients tend to develop venous thromboembolism (PE:1.0-40.0% and DVT:0.4-84%) compared to arterial thromboembolism (stroke:0.5-15.2% and MI:0.8-8.7%). Lastly, the all-cause mortality of COVID-19 patients ranged from 4.8 to 63%, whereas the incidence of mortality associated with TE complications was between 5% and 48%. A wide range of incidences of TE complications and mortality associated with TE complications can be seen among hospitalized COVID-19 patients. Therefore, every patient should be assessed for the risk of thromboembolic complications and provided with an appropriate thromboprophylaxis management plan tailored to their individual needs.


COVID-19 , Hospitalization , Thromboembolism , Humans , COVID-19/complications , COVID-19/mortality , COVID-19/epidemiology , Thromboembolism/epidemiology , Thromboembolism/etiology , Thromboembolism/mortality , Hospitalization/statistics & numerical data , Pulmonary Embolism/epidemiology , Pulmonary Embolism/etiology , Pulmonary Embolism/mortality , SARS-CoV-2 , Incidence , Venous Thromboembolism/etiology , Venous Thromboembolism/epidemiology , Venous Thromboembolism/prevention & control , Stroke/epidemiology , Stroke/mortality , Myocardial Infarction/mortality , Myocardial Infarction/epidemiology , Myocardial Infarction/complications , Venous Thrombosis/epidemiology , Venous Thrombosis/etiology
3.
Support Care Cancer ; 32(6): 331, 2024 May 06.
Article En | MEDLINE | ID: mdl-38710920

AIM: We evaluated the efficacy and safety of Nuvastatic™ (C5OSEW5050ESA) in improving cancer-related fatigue (CRF) among cancer patients. METHODS: This multicenter randomized double-blind placebo-controlled phase 2 trial included 110 solid malignant tumor patients (stage II-IV) undergoing chemotherapy. They were randomly selected and provided oral Nuvastatic™ 1000 mg (N = 56) or placebo (N = 54) thrice daily for 9 weeks. The primary outcomes were fatigue (Brief Fatigue Inventory (BFI)) and Visual Analog Scale for Fatigue (VAS-F)) scores measured before and after intervention at baseline and weeks 3, 6, and 9. The secondary outcomes were mean group difference in the vitality subscale of the Medical Outcome Scale Short Form-36 (SF-36) and urinary F2-isoprostane concentration (an oxidative stress biomarker), Eastern Cooperative Oncology Group scores, adverse events, and biochemical and hematologic parameters. Analysis was performed by intention-to-treat (ITT). Primary and secondary outcomes were assessed by two-way repeated-measures analysis of variance (mixed ANOVA). RESULTS: The Nuvastatic™ group exhibited an overall decreased fatigue score compared with the placebo group. Compared with the placebo group, the Nuvastatic™ group significantly reduced BFI-fatigue (BFI fatigue score, F (1.4, 147) = 16.554, p < 0.001, partial η2 = 0.333). The Nuvastatic™ group significantly reduced VAS-F fatigue (F (2, 210) = 9.534, p < 0.001, partial η2 = 0.083), improved quality of life (QoL) (F (1.2, 127.48) = 34.07, p < 0.001, partial η2 = 0.243), and lowered urinary F2-IsoP concentrations (mean difference (95% CI) = 55.57 (24.84, 86.30)), t (55) = 3.624, p < 0.001, Cohen's d (95% CI) = 0.48 (0.20, 0.75)). Reported adverse events were vomiting (0.9%), fever (5.4%), and headache (2.7%). CONCLUSION: Nuvastatic™ is potentially an effective adjuvant for CRF management in solid tumor patients and worthy of further investigation in larger trials. TRIAL REGISTRATION: ClinicalTrial.gov ID: NCT04546607. Study registration date (first submitted): 11-05-2020.


Cinnamates , Depsides , Fatigue , Neoplasms , Rosmarinic Acid , Humans , Double-Blind Method , Fatigue/etiology , Fatigue/drug therapy , Female , Middle Aged , Male , Neoplasms/complications , Aged , Depsides/pharmacology , Depsides/administration & dosage , Depsides/therapeutic use , Adult , Cinnamates/administration & dosage , Cinnamates/therapeutic use , Cinnamates/pharmacology , Plant Extracts/administration & dosage
4.
Heliyon ; 10(8): e29490, 2024 Apr 30.
Article En | MEDLINE | ID: mdl-38655301

Diversity and homeostasis of gut bacterial composition is highly associated with the pathogenesis of insulin dysfunction and type 1 diabetes melittus (T1D), hence emerged in parallel with the activation of autoimmunity. We aimed to study the bioactive potential of essential oil from Zanthoxylum myriacanthum var. pubescens Huang (Maqian) through computational approaches. Twelve chemical constituents derived from Maqian essential oil were docked with selected proteins (i.e., 3pig, 1kho, 7dmq, 4m4d, 2z65, 4glp, and 3fxi) in which are involved in gut microbiota modulation in T1D. Subsequently, the prediction of bioavailability properties of the small molecules were evaluated. Among all chemical constituents, the post-docking interaction analysis demonstrated that α-phellandrene exhibits the strongest binding affinity and induces gut microbiota modulation with ß-fructofuranosidase from Bifidobacterium longum. The current result revealed the potential of 3-Carene and α-Pinene in inducing specific changes in gut microbiota downregulating Clostridium perfringens and quenching Leptotrichia shahii respectively. ß-Pinene possess exceptionally strong binding affinity that effectively disrupt the interaction between lipopolysaccharide and its cognate receptors, while α-Phellandrene was exhibited the uppermost binding affinity with TLR4/MD2 and could likely target TLR4 stimulating lipopolysaccharide. Our results are the first to report on the gut microbiota modulation effects of α-Phellandrene and ß-Phellandrene via actions on LPS binding to CD14 and the TLR4 co-receptor signaling. In conclusion, our findings based on computational approaches, small molecules from Maqian present as promising agents which could regulate inflammatory response and modulate gut microbiota in type 1 diabetes mellitus.

5.
J Appl Biomater Funct Mater ; 22: 22808000241236020, 2024.
Article En | MEDLINE | ID: mdl-38462785

OBJECTIVE: To investigate the Pinus halepensis extracts and determine its healing and antibacterial effects, and to evaluate the treatment of skin burns. METHODS: Aqueous and ethanolic extracts and topical based on Aleppo pine plant extracts were prepared. Thirty male and female Wistar rats were used to study the cutaneous toxicity of extracts from the bark of P. halepensis. The extracts' healing potential for burn wounds were also assessed by evaluating the clinical and macroscopic aspects of the wounds. The antibacterial activity of crude extracts of P. halepensis as well as its wound healing abilities was verified in this investigation. RESULTS: In animals with acute dermal toxicity, there were no signs of treatment-related toxicity or death. The extracts of these plants could be transformed into phytomedicines for the treatment of infected wounds. The results demonstrated that formulated ointments are successful in treating second-degree burns in rats and may be suitable for the short-term therapeutic treatment of second-degree burns. CONCLUSION: This study successfully answered our problem, regarding the efficacy of our extract for treating second-degree burns in rats. Further studies are needed to confirm these results by identifying the molecules responsible for these activities and examining their mechanism of action.


Burns , Pinus , Rats , Animals , Rats, Wistar , Wound Healing , Burns/drug therapy , Anti-Bacterial Agents/pharmacology , Skin/injuries
6.
Biomed Pharmacother ; 174: 116432, 2024 May.
Article En | MEDLINE | ID: mdl-38520868

Oxidative stress results from a persistent imbalance in oxidation levels that promotes oxidants, playing a crucial role in the early and sustained phases of DNA damage and genomic and epigenetic instability, both of which are intricately linked to the development of tumors. The molecular pathways contributing to carcinogenesis in this context, particularly those related to double-strand and single-strand breaks in DNA, serve as indicators of DNA damage due to oxidation in cancer cases, as well as factors contributing to epigenetic instability through ectopic expressions. Oxidative stress has been considered a therapeutic target for many years, and an increasing number of studies have highlighted the promising effectiveness of natural products in cancer treatment. In this regard, we present significant research on the therapeutic targeting of oxidative stress using natural molecules and underscore the essential role of oxidative stress in cancer. The consequences of stress, especially epigenetic instability, also offer significant therapeutic prospects. In this context, the use of natural epi-drugs capable of modulating and reorganizing the epigenetic network is beginning to emerge remarkably. In this review, we emphasize the close connections between oxidative stress, epigenetic instability, and tumor transformation, while highlighting the role of natural substances as antioxidants and epi-drugs in the anti-tumoral context.


Antioxidants , Cell Transformation, Neoplastic , Epigenesis, Genetic , Neoplasms , Oxidative Stress , Oxidative Stress/drug effects , Humans , Epigenesis, Genetic/drug effects , Antioxidants/pharmacology , Animals , Cell Transformation, Neoplastic/drug effects , Cell Transformation, Neoplastic/genetics , Cell Transformation, Neoplastic/metabolism , Neoplasms/drug therapy , Neoplasms/pathology , Neoplasms/genetics , Neoplasms/metabolism , Biological Products/pharmacology , DNA Damage/drug effects
7.
J Pharm Policy Pract ; 17(1): 2308617, 2024.
Article En | MEDLINE | ID: mdl-38420042

Background: The safety, side effects and efficacy profile of COVID-19 vaccines remain subjects of ongoing concern among the public in Malaysia. The aim of this study was to determine the types of adverse effects following immunisation with COVID-19 vaccines and the differences based on various types of COVID-19 vaccines to raise public awareness and reduce vaccine hesitancy among the public. Methods: A total of 901 Malaysian adults (≥18 years) who received various COVID-19 vaccines were selected to participate in our cross-sectional study through an online survey between December 2021 and January 2022. Results: A total of 814 (90.3%) of the participants reported ≥1 side effect following COVID-19 immunisation. Of these, the predominant symptoms were swelling at the injection site (n = 752, 83.5%), headache (n = 638, 70.8%), pain or soreness at the injection site (n = 628, 69.7%), fatigue or tiredness (n = 544, 60.4%), muscle weakness (n = 529, 58.7%) and diarrhea (n = 451, 50.1%). Recipients of the Pfizer-BioNTech (Comirnaty ®) vaccine reported the highest number of adverse effects (n = 355, 43.6%), followed by mixed COVID-19 vaccines (n = 254, 31.2%), the Oxford-AstraZeneca (ChAdOx1-®[recombinant]) vaccine (n = 113, 13.9%) and the Sinovac (CoronaVac®) vaccine (n = 90, 11.1%). The study showed that individuals who reported significantly more side effects were of elderly age, female gender and high educational level [P value < 0.05]. Mixed COVID-19 vaccine recipients also reported significantly more local and systemic symptoms after the first dose and third dose when compared with other single vaccine recipients. Conclusion: This study demonstrated the types of self-reported adverse effects following immunisation with single and mixed COVID-19 vaccines. These findings may provide the side effects of different COVID-19 vaccines with the hope of educating the public on the safety profiles of these vaccines and reducing vaccine hesitancy among the public.

8.
Article En | MEDLINE | ID: mdl-38357954

BACKGROUND: Seeds of plant Scaphium Affine are traditionally used by the healers of "India" for the treatment of piles. OBJECTIVE: The primary objective of the study was to assess the anti-hemorrhoidal potential of the ethanolic seed extract of Scaphium affine. METHODS: After the soxhlet extraction method, the seed extract from Scaphium affine was first submitted to phytochemical standardization and then GC-MS analysis. Rats were given Croton oil and Jatropha oil to develop hemorrhoids, and Scaphium affine seed extract (ESA) was administered orally for 5 days and 3 days, respectively, at doses of 1000 and 500 mg/kg. The Rectoanal coefficient (RAC) was calculated as an inflammatory marker. The hemorrhoidal tissues were also subjected to cytokine profiling, biochemical estimation and histopathology. RESULTS: ESA demonstrated the presence of flavonoids, saponins, phytosterols, phenols, and tannins. GCMS analysis elucidated the presence of hexadecanoic acid 2 hydroxy -1,3 propane diyl ester,9 Octadecanoic acid ethyl ester, Cyclohexane 1,4 di methyl cis, Farnesol isomer,1, E-11, Z-13 octa decatriene, Stigmasterol, N-(5 ethyl -1,3,4-thiadiazol-yl) benzamide, N, N Dinitro 1,3,5,7 tetraza bicyclo 93,3,1) as major phytoconstituents. The results depicted more potent anti-hemorrhoidal activity of ESA at 1000 mg/kg, p.o., which was evident through a decrease in RAC. A significant decline in the levels of IL-1ß, IL-6, and TNF-α expression was observed, along with the restoration of altered antioxidants and enzymes. Histopathological analysis confirmed the tissue recovery as it revealed minimal inflammation and decreased dilated blood vessels in treated animals. CONCLUSION: Based on the results it can be concluded that seeds of Scaphium affine showed significant anti-hemorrhoid agents which may be attributed to their anti-inflammatory and anti-oxidant potential due to the presence of certain phytoconstituents in it. The study also supports the traditional use of seeds of Scaphium affine for the first time in the treatment of hemorrhoids.

9.
Ann Med ; 56(1): 2271942, 2024 12.
Article En | MEDLINE | ID: mdl-38346353

AIM: The use of tobacco is responsible for many preventable diseases and deaths worldwide. Digital interventions have greatly improved patient health and clinical care and have proven to be effective for quitting smoking in the general population due to their flexibility and potential for personalization. However, there is limited evidence on the effectiveness of digital interventions for smoking cessation in Asian countries. METHODS: Three major databases - Web of Science (WOS), Scopus, and PubMed - for relevant studies published between 1 January 2010 and 12 February 2023 were searched for studies evaluating the effectiveness of digital intervention for smoking cessation in Asian countries. RESULTS: A total of 25 studies of varying designs were eligible for this study collectively involving a total of n = 22,005 participants from 9 countries. Among different digital tools for smoking cessation, the highest abstinence rate (70%) was reported with cognitive behavioural theory (CBT)-based smoking cessation intervention via Facebook followed by smartphone app (60%), WhatsApp (59.9%), and Pharmacist counselling with Quit US smartphone app (58.4%). However, WhatsApp was preferred over Facebook intervention due to lower rates of relapse. WeChat was responsible for 15.6% and 41.8% 7-day point prevalence abstinence. For telephone/text messaging abstinence rate ranged from 8-44.3% and quit rates from 6.3% to 16.8%. Whereas, no significant impact of media/multimedia messages and web-based learning on smoking cessation was observed in this study. CONCLUSION: Based on the study findings the use of digital tools can be considered an alternative and cost-effective smoking cessation intervention as compared to traditional smoking cessation interventions.


Smoking Cessation , Text Messaging , Humans , Smoking Cessation/psychology , Smoking/epidemiology , Counseling , Prevalence
10.
Heliyon ; 10(1): e23084, 2024 Jan 15.
Article En | MEDLINE | ID: mdl-38169772

Tetraclinis articulata is a known traditional medicinal plant used to manage various ailments, such as diabetes, rheumatism and infectious diseases. This study aims to determine the chemical constituents of T. articulata essential oil (EO) and to evaluate its in vitro antibacterial, anti-candidal, antioxidant, anti-inflammatory and dermatoprotective properties. In addition, a computational docking approach was used to predict the potential antioxidant, antibacterial, antifungal, anti-inflammatory, and cytotoxic properties of the identified compounds. The volatile oil obtained by hydrodistillation was characterized using gas chromatography-mass spectrometry (GC-MS). The antioxidant activity of T. articulata EO was investigated using three complementary assays: DPPH, ABTS and FRAP. Lipoxygenase (5-LOX) and tyrosinase enzymes were used to assess the anti-inflammatory and dermatoprotective effects of this oil. Moreover, disc-diffusion technique, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays were employed for the antimicrobial screening. The GC-MS analysis revealed that bornyl acetate (41.80 %), α-pinene (17.97 %) and camphor (15.97 %) are the major components of the studied EO. Moreover, T. articulata EO has exhibited promising antioxidant effect on FRAP, DPPH, and ABTS experiments. It also significantly inhibited 5-LOX (IC50 = 67.82 ± 0.03 µg/mL) and tyrosinase (IC50 = 211.93 ± 0.02 µg/mL). The results of MIC and MBC assays indicated that T. articulata EO is able to inhibit the growth of all tested bacteria (Gram + and Gram -) and Candida species. The ratio of tolerance level indicated that the tested oil was bactericidal against the Gram + bacteria and Candida species, whereas it has a bacteriostatic behavior against the Gram- bacteria. In light of these findings, T. articulata EO may be suggested as a potential pharmaceutical agent to prevent inflammation and skin problems and may serve as a natural antimicrobial and antioxidant alternative for sustainable application in food products.

11.
Biomed Pharmacother ; 170: 116070, 2024 Jan.
Article En | MEDLINE | ID: mdl-38163396

Two-dimensional (2D) nanomaterials have garnered enormous attention seemingly due to their unusual architecture and properties. Graphene and graphene oxide based 2D nanomaterials remained the most sought after for several years but the quest to design superior 2D nanomaterials which can find wider application gave rise to development of non-graphene 2D materials as well. Consequently, in addition to graphene based 2D nanomaterials, 2D nanostructures designed using macromolecules (such as DNAs, proteins, peptides and peptoids), transition metal dichalcogenides, transition-metal carbides and/or nitrides (MXene), black phosphorous, chitosan, hexagonal boron nitrides, and graphitic carbon nitride, and covalent organic frameworks have been developed. Interestingly, these 2D nanomaterials have found applications in diagnosis and treatment of various diseases including Alzheimer's disease (AD). Although AD is one of the most debilitating neurodegenerative conditions across the globe; unfortunately, there remains a paucity of effective diagnostic and/or therapeutic intervention for it till date. In this scenario, nanomaterial-based biosensors, or therapeutics especially 2D nanostructures are emerging to be promising in this regard. This review summarizes the diagnostic and therapeutic platforms developed for AD using 2D nanostructures. Collectively, it is worth mentioning that these 2D nanomaterials would seemingly provide an alternative and intriguing platform for biomedical interventions.


Alzheimer Disease , Biosensing Techniques , Graphite , Nanostructures , Humans , Graphite/chemistry , Alzheimer Disease/diagnosis , Alzheimer Disease/drug therapy , Nanostructures/therapeutic use , Nanostructures/chemistry , Biosensing Techniques/methods
12.
JMIR Med Educ ; 10: e47339, 2024 Jan 12.
Article En | MEDLINE | ID: mdl-38214967

BACKGROUND: Artificial Intelligence (AI) plays an important role in many fields, including medical education, practice, and research. Many medical educators started using ChatGPT at the end of 2022 for many purposes. OBJECTIVE: The aim of this study was to explore the potential uses, benefits, and risks of using ChatGPT in education modules on integrated pharmacotherapy of infectious disease. METHODS: A content analysis was conducted to investigate the applications of ChatGPT in education modules on integrated pharmacotherapy of infectious disease. Questions pertaining to curriculum development, syllabus design, lecture note preparation, and examination construction were posed during data collection. Three experienced professors rated the appropriateness and precision of the answers provided by ChatGPT. The consensus rating was considered. The professors also discussed the prospective applications, benefits, and risks of ChatGPT in this educational setting. RESULTS: ChatGPT demonstrated the ability to contribute to various aspects of curriculum design, with ratings ranging from 50% to 92% for appropriateness and accuracy. However, there were limitations and risks associated with its use, including incomplete syllabi, the absence of essential learning objectives, and the inability to design valid questionnaires and qualitative studies. It was suggested that educators use ChatGPT as a resource rather than relying primarily on its output. There are recommendations for effectively incorporating ChatGPT into the curriculum of the education modules on integrated pharmacotherapy of infectious disease. CONCLUSIONS: Medical and health sciences educators can use ChatGPT as a guide in many aspects related to the development of the curriculum of the education modules on integrated pharmacotherapy of infectious disease, syllabus design, lecture notes preparation, and examination preparation with caution.


Communicable Diseases , Educational Personnel , Humans , Artificial Intelligence , Educational Status , Curriculum , Communicable Diseases/drug therapy
13.
J Biomol Struct Dyn ; 42(5): 2550-2569, 2024 Mar.
Article En | MEDLINE | ID: mdl-37144753

Due to the high rates of drug development failure and the massive expenses associated with drug discovery, repurposing existing drugs has become more popular. As a result, we have used QSAR modelling on a large and varied dataset of 657 compounds in an effort to discover both explicit and subtle structural features requisite for ACE2 inhibitory activity, with the goal of identifying novel hit molecules. The QSAR modelling yielded a statistically robust QSAR model with high predictivity (R2tr=0.84, R2ex=0.79), previously undisclosed features, and novel mechanistic interpretations. The developed QSAR model predicted the ACE2 inhibitory activity (PIC50) of 1615 ZINC FDA compounds. This led to the detection of a PIC50 of 8.604 M for the hit molecule (ZINC000027990463). The hit molecule's docking score is -9.67 kcal/mol (RMSD 1.4). The hit molecule revealed 25 interactions with the residue ASP40, which defines the N and C termini of the ectodomain of ACE2. The HIT molecule conducted more than thirty contacts with water molecules and exhibited polar interaction with the ARG522 residue coupled with the second chloride ion, which is 10.4 nm away from the zinc ion. Both molecular docking and QSAR produced comparable findings. Moreover, MD simulation and MMGBSA studies verified docking analysis. The MD simulation showed that the hit molecule-ACE2 receptor complex is stable for 400 ns, suggesting that repurposed hit molecule 3 is a viable ACE2 inhibitor.


Angiotensin-Converting Enzyme 2 , Quantitative Structure-Activity Relationship , Angiotensin-Converting Enzyme 2/antagonists & inhibitors , Computer Simulation , Molecular Docking Simulation , Molecular Dynamics Simulation , Zinc
14.
Naunyn Schmiedebergs Arch Pharmacol ; 397(3): 1505-1524, 2024 03.
Article En | MEDLINE | ID: mdl-37755516

Saussurea costus (Falc.) Lipsch., commonly known as costus, is a perennial herb that has been traditionally used in various indigenous medicinal systems across Asia. Its historical prominence in traditional remedies underscores the need to explore its phytochemical composition, pharmacological properties, and potential therapeutic benefits. This review aims to provide a comprehensive overview of the available literature on the pharmacological properties, phytochemical constituents, ethnobotanical uses, and therapeutic potential of S. costus. An exhaustive search was performed across multiple electronic databases, including PubMed/MedLine, Google Scholar, Web of Science, Scopus, TRIP database, and Science Direct. Both experimental and clinical studies, as well as traditional ethnobotanical records, were considered for inclusion. The phytochemical analysis revealed that S. costus contains a plethora of bioactive compounds, including sesquiterpenes, flavonoids, and essential oils, which are responsible for its myriad of medicinal properties. The pharmacological studies have demonstrated its anti-inflammatory, anti-oxidant, anti-cancer, hepatoprotective, and immunomodulatory effects, among others. Ethnobotanical data showcased its extensive use in treating ailments like asthma, digestive disorders, and skin conditions. Some clinical trials also underscore its efficacy in certain health conditions, corroborating its traditional uses. S. costus possesses significant therapeutic potential, largely attributable to its rich phytochemical composition; the convergence of its traditional uses and modern pharmacological findings suggests promising avenues for future research, especially in drug development and understanding its mechanism of action in various ailments.


Saussurea , Sesquiterpenes , Saussurea/chemistry , Phytotherapy , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Extracts/chemistry , Phytochemicals/pharmacology , Phytochemicals/therapeutic use , Phytochemicals/analysis , Sesquiterpenes/pharmacology
15.
Drug Dev Ind Pharm ; 50(1): 36-44, 2024 Jan.
Article En | MEDLINE | ID: mdl-38149637

INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited. OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs. METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation. RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min. CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.


Excipients , Xylitol , Humans , Excipients/chemistry , Mirtazapine , Drug Compounding/methods , Solubility , Administration, Oral , Tablets/chemistry , Mannitol/chemistry
16.
Biomed Pharmacother ; 170: 115989, 2024 Jan.
Article En | MEDLINE | ID: mdl-38103309

Cyanobacteria and microalgae contain various phytochemicals, including bioactive components in the form of secondary metabolites, namely flavonoids, phenolic acids, terpenoids, and tannins, with remarkable anticancer effects. This review highlights the recent advances in bioactive compounds, with potential anticancer activity, produced by cyanobacteria and microalgae. Previous in vitro investigations showed that many of these bioactive compounds exhibit potent effects against different human cancer types, such as leukemia and breast cancers. Multiple mechanisms implicated in the antitumor effect of these compounds were elucidated, including their ability to target cellular, subcellular, and molecular checkpoints linked to cancer development and promotion. Recent findings have highlighted various mechanisms of action of bioactive compounds produced by cyanobacteria and microalgae, including induction of autophagy and apoptosis, inhibition of telomerase and protein kinases, as well as modulation of epigenetic modifications. In vivo investigations have demonstrated a potent anti-angiogenesis effect on solid tumors, as well as a reduction in tumor volume. Some of these compounds were examined in clinical investigations for certain types of cancers, making them potent candidates/scaffolds for antitumor drug development.


Antineoplastic Agents , Cyanobacteria , Microalgae , Neoplasms , Humans , Microalgae/chemistry , Cyanobacteria/metabolism , Biological Factors , Antineoplastic Agents/chemistry , Neoplasms/drug therapy
17.
Heliyon ; 9(11): e21222, 2023 Nov.
Article En | MEDLINE | ID: mdl-38053906

Lavandula stoechas, a Mediterranean plant, renowned in traditional medicine for its health benefits, is also arousing strong interest associated with its essential oils (EOs) with promising therapeutic properties. The aim of this study was to analyze the chemical composition of the plant, as well as to study its major activities, including antioxidant, anti-diabetic, dermatoprotective, anti-inflammatory, and antibacterial effects, focusing on its major molecules. Using the GC-MS method, the main compounds identified in L. stoechas EO (LSEO) were fenchone (31.81 %) and camphor (29.60 %), followed by terpineol (13.14 %) and menthone (8.96 %). To assess their antioxidant activity, three in vitro methods were used (DPPH, FRAP, and ABTS). The results revealed that LSEO exhibited the best antiradical property (54 ± 62 µg/mL) according to the DPPH test, while fenchone demonstrated the highest antioxidant capacity (87 ± 92 µg/mL) in the FRAP test, and camphor displayed the highest antioxidant capacity (96 ± 32 µg/mL) in the ABTS test. However, these results were lower than those obtained by Trolox used as a reference. In addition, study also explored the anti-diabetic potential of LSEO and its major compounds by evaluating their inhibitory activity towards two digestive enzymes, α-glucosidase and α-amylase. Camphor (76.92 ± 2.43 µg/mL) and fenchone (69.03 ± 2.31 µg/mL) exhibited the best inhibitory activities for α-amylase and α-glucosidase assays, respectively. Interestingly, all elements of the study exerted activities superior to those of acarbose, regardless of the test performed. In contrast, the evaluation of the dermatoprotective potential was carried out in vitro by targeting two enzymes involved in cutaneous processes, tyrosinase and elastase. In this light, fenchone (53.14 ± 3.06 µg/mL) and camphor (48.39 ± 1.92 µg/mL) were the most active against tyrosinase and elastase, respectively. It should be noted that the effect of both molecules, as well as that of LSEO, ranged between 53.14 ± 3.06 and 97.45 ± 5.22 µg/mL, which was significantly lower than the standard, quercetin (IC50 of 246.90 ± 2 0.54 µg/mL) against tyrosinase. Furthermore, the anti-inflammatory potential of these elements has been studied by evaluating their ability to inhibit lipooxygenase (LOX), a class of enzymes involved in the inflammatory process in the human body. As a result, the LSEO demonstrated a remarkable effect with an IC50 of 6.34 ± 1.29 µg/mL, which was almost comparable to the standard, quercetin (IC50 = 3.93 ± 0.45 µg/mL). Concerning the antibacterial potential, we carried out a quantitative analysis of the various products tested, revealing a bactericidal activity of the LSEO against the strain L. monocytogenes ATCC 13932 at a minimum effective concentration (MIC = CMB = 0.25). Overall, LSEOs offer significant potential as a source of natural antioxidants, and antidiabetic and anti-inflammatory agents, as well as dermatoprotective and antibacterial compounds. Its major molecules, fenchone and camphor, showed promising activity in these areas of study, making it a valuable candidate for future research and development in the field of natural medicine.

18.
Sci Rep ; 13(1): 22767, 2023 12 20.
Article En | MEDLINE | ID: mdl-38123687

Eight Moroccan avocado varieties were analyzed for their nutritional composition and physicochemical properties. The nutritional contents of the sample were determined through the evaluation of the moisture, oil, ash, protein, and carbohydrate contents, and energy value calculation. Additionally, macroelements (Ca, Mg, and Na) and microelements (Fe, Zn, Cu, and Mn) were determined in the mineral profile. Oils were examined also for their fatty acid, phytosterol, and tocopherol profiles. As a result of the study, the avocado presents significant differences between the eight studied varieties (p < 0.05), with regard to moisture content (57.88 g/100 g to 84.71 g/100 g), oil content (8.41 g/100 g to 57.88 g/100 g), ash (0.57 g/100 g to 1.37 g/100 g), protein content (5.7 g/100 g to 8.61 g/100 g), carbohydrate content (5.63 g/100 g to 14.61 g/100 g), and energy value (99.9 kcal/100 g to 316.8 kcal/100 g). Sodium (5783.01 mg/kg to 12,056.19 mg/kg) was the predominant macro-element in all varieties, followed by calcium (295.95 mg/kg to 531.67 mg/kg), and magnesium (246.29 mg/kg to 339.84 mg/kg). Copper (85.92 mg/kg to 112. 31 mg/kg) was the main microelement in all varieties, followed by iron (8.5 mg/kg to 20.32 mg/kg), and manganese (7.3 mg/kg to 18.45 mg/kg), while zinc (1.72 mg/kg to 5.66 mg/kg) was detected in small amounts. In addition, significant difference was observed in lipid profiles, according to the eight studied varieties (p < 0.05). Avocado oils were mainly composed of monounsaturated fatty acids (76.89 g/100 g to 84.7 g/100 g), with oleic acid (50.38 g/100 g to 71.49 g/100 g) standing out as particularly characteristic, while ß-sitosterol (l2365.58 mg/kg to 4559.27 mg/kg), and α-tocopherol (30.08 mg/kg to 182.94 mg/kg) were among its major phytosterols and tocopherols. All avocado varieties represented in this study can be consumed as a fruit as an excellent source of energy, minerals, fatty acids, phytosterols, and tocopherols. The regular consumption of this fruit provides the body with several essential nutrients.


Persea , Phytosterols , Persea/chemistry , Fatty Acids/chemistry , Tocopherols , Minerals , Carbohydrates , Oils
19.
J Pharm Policy Pract ; 16(1): 162, 2023 Nov 29.
Article En | MEDLINE | ID: mdl-38031133

BACKGROUND: This study aimed to assess the general public's perception of services provided by community pharmacies, their willingness to utilize these services, their satisfaction with and understanding of community pharmacists, and their views on dispensing separation and pharmacy medicines (P medicines). METHODS: An online cross-sectional study was conducted, in which questionnaires were distributed among the general public. A novel questionnaire was designed and validated specifically for this study. It was composed of six sections: demographics, pharmacy usage and service preferences, understanding and satisfaction with pharmacists, views on dispensing separation, private community pharmacies, and knowledge of P medicines. Statistical analyses such as one-way ANOVA, independent t test, and binary logistic regression were employed, with a p value of < 0.05 considered statistically significant. RESULTS: The study received 222 responses. The majority of the respondents were females within the 20-29-year-old age group (62.2%). Most respondents preferred to consult doctors for medical treatment, with their primary reason for visiting community pharmacies being to collect prescribed medicines. About 52.7% of respondents expressed their willingness to avail of screening services and treatment for minor illnesses at community pharmacies. A statistically significant difference was found among different age groups regarding their views on the dispensing separation system, with those aged 41-50 years demonstrating higher scores. However, the binary logistic regression analysis did not reveal any statistical significance when comparing the understanding of P medicines among respondents. CONCLUSIONS: In general, the public prefers to consult doctors for medical treatment and visit community pharmacies predominantly to collect prescriptions or purchase over-the-counter medications. Nonetheless, they are also open to utilizing services provided by community pharmacists, particularly screening services and treatment for minor illnesses.

20.
Clin Exp Vaccine Res ; 12(4): 265-290, 2023 Oct.
Article En | MEDLINE | ID: mdl-38025914

Rare but serious thrombotic incidents in relation to thrombocytopenia, termed vaccine-induced immune thrombotic thrombocytopenia (VITT), have been observed since the vaccine rollout, particularly among replication-defective adenoviral vector-based severe acute respiratory syndrome coronavirus 2 vaccine recipients. Herein, we comprehensively reviewed and summarized reported studies of VITT following the coronavirus disease 2019 (COVID-19) vaccination to determine its prevalence, clinical characteristics, as well as its management. A literature search up to October 1, 2021 using PubMed and SCOPUS identified a combined total of 720 articles. Following the PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guideline, after screening the titles and abstracts based on the eligibility criteria, the remaining 47 full-text articles were assessed for eligibility and 29 studies were included. Findings revealed that VITT cases are strongly related to viral vector-based vaccines, which are the AstraZeneca COVID-19 vaccine (95%) and the Janssen COVID-19 vaccine (4%), with much rarer reports involving messenger RNA-based vaccines such as the Moderna COVID-19 vaccine (0.2%) and the Pfizer COVID-19 vaccine (0.2%). The most severe manifestation of VITT is cerebral venous sinus thrombosis with 317 cases (70.4%) and the earliest primary symptom in the majority of cases is headache. Intravenous immunoglobulin and non-heparin anticoagulant are the main therapeutic options for managing immune responses and thrombosis, respectively. As there is emerging knowledge on and refinement of the published guidelines regarding VITT, this review may assist the medical communities in early VITT recognition, understanding the clinical presentations, diagnostic criteria as well as its management, offering a window of opportunity to VITT patients. Further larger sample size trials could further elucidate the link and safety profile.

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