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  1. Fulltext Bioactive substances of cyanobacteria and microalgae: Sources, metabolism, and anticancer mechanism insights
    Bouyahya A, Bakrim S, Chamkhi I, Taha D, El Omari N, El Mneyiy N, et al.
    Biomed Pharmacother, 2024 Jan;170:115989.
    PMID: 38103309 DOI: 10.1016/j.biopha.2023.115989
    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.
  2. Fulltext Cross-sectional Study on the Impact of Discount Pricing and Price Competition on Community Pharmacy Practice
    Mathews A, Ming LC, Che Rose FZ, Abbas SA
    Cureus, 2020 Aug 20;12(8):e9903.
    PMID: 32839684 DOI: 10.7759/cureus.9903
    Background Without stipulated legislation, a free pricing policy can lead to a disparity in prices among private healthcare setups. Competition is especially rampant among community pharmacies, especially in the Sabah state of Malaysia, where the recent years have witnessed the steady growth of pharmacy players from Peninsular Malaysia. Thus, this study aimed to examine the impact of price competition and discount pricing on the practice of community pharmacy in Sabah, Malaysia. Methods This was a cross-sectional study using an online questionnaire. Survey participants included community pharmacists practicing in Sabah. The validated and pilot-tested questionnaire consisted of three parts: background information of the pharmacy, attitudes and perception toward medicine prices, and practice of discount pricing. All required data were collected from community pharmacists practicing only in Sabah. Data were then analyzed by using descriptive, Chi-Square, and Kendall's tau-b tests. Results Of the 150 community pharmacists contacted, only 70 responded, providing a response rate of 47%. In terms of pharmacy type, 71% of the respondents were pharmacist-owned independent pharmacies, while 19% were pharmacy chains owned by community pharmacists. The remaining were pharmacies owned by non-pharmacists (10%). Sixty percent of the community pharmacies had been in existence for more than 10 years, with 12% in existence for less than two years, and 28% in existence for three to 10 years. More than 80% of the respondents stated that the business aspect of community pharmacy had overwhelmed the professional practice aspects and that community pharmacists have become providers of products instead of providers of care. In terms of professionalism, 87% also noted that they are being perceived as profiteering in the medicine business at the expense of patients. Conclusions The free market situation in Malaysia for medicine pricing has brought a detrimental consequence for community pharmacists with each one trying to undercut prices. Differing pricing mechanisms of medicines based on the quantity ordered contribute to the problem of discount pricing and price competition. Most community pharmacists, as indicated by this study, want the problem to be addressed.
  3. Developing a practice-based master in clinical pharmacy program at the Universiti Teknologi MARA, Malaysia
    Hadi MA, Ming LC, Leng LW, Shaharuddin S, Adam A
    Am J Pharm Educ, 2010 Mar 10;74(2):32d.
    PMID: 20414448
  4. Fulltext Flumazenil Pretreatment Reduces Mefenamic Acid-Induced Central Nervous System Toxicity in Mice
    Jarrar Q, Ayoub R, Jarrar Y, Aburass H, Goh KW, Ardianto C, et al.
    J Integr Neurosci, 2023 Jul 26;22(4):104.
    PMID: 37519168 DOI: 10.31083/j.jin2204104
    BACKGROUND: Mefenamic acid (MFA), a common analgesic, causes central nervous system (CNS) toxicity at high doses with a proposed activity on the Gamma-aminobutyric acid (GABA) system. However, it remains unknown whether flumazenil (FMZ), a GABA type A receptor (GABAAR) antagonist, can reverse MFA toxicity.

    METHODS: The behavioral and neurophysiological effects of MFA were investigated in mice with and without FMZ pre-treatment. The elevated zero maze (EZM) and marble burying tests were used to assess anxiety-like behaviors and burying activities, respectively. The standard bar test was used to evaluate catalepsy, while the actophotometer test was used to measure locomotor activity. Seizure intensity was scored, and fatalities were counted.

    RESULTS: Without FMZ pre-treatment, MFA induced behavioral and neurophysiological effects in a dose-dependent manner as follows: At a dose of 20 mg/kg, i.p, MFA-treated mice exhibited anxiety-like behaviors, which was determined by a significant increase in the time spent in the closed areas and a significant decrease in the number of entries to the open areas of the EZM apparatus. These mice also showed a significant decrease in the burying activity, manifested as a significant decrease in the number of buried marbles. At 40 mg/kg, i.p., MFA-treated mice showed catalepsy that was associated with a significant decrease in locomotor activity. At a dose of 80 mg/kg, i.p., mice developed fatal tonic-clonic seizures (seizure score = 4). Pre-treatment with FMZ (5 mg/kg, i.p.) significantly reversed the anxiety-like behaviors and restored marble-burying activity. Additionally, FMZ prevented catalepsy, significantly restored locomotor activity, reduced seizure intensity (seizure score = 0.3) and significantly reduced mortalities.

    CONCLUSIONS: The present study's findings indicate that activation of the GABAAR is involved in the CNS toxicity of MFA, and FMZ reverses MFA toxicity by interfering with this receptor.

  5. Effectiveness of digital tools for smoking cessation in Asian countries: a systematic review
    Goh KW, Ming LC, Al-Worafi YM, Tan CS, Hermansyah A, Rehman IU, et al.
    Ann Med, 2024 Dec;56(1):2271942.
    PMID: 38346353 DOI: 10.1080/07853890.2023.2271942
    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.

  6. Fulltext Positive global environmental impacts of the COVID-19 pandemic lockdown: a review
    Loh HC, Looi I, Ch'ng ASH, Goh KW, Ming LC, Ang KH
    GeoJournal, 2021 Jul 23.
    PMID: 34316088 DOI: 10.1007/s10708-021-10475-6
    Global environmental change is mainly due to human behaviours and is a major threat to sustainability. Despite all the health and economic consequences, the impact of the COVID-19 pandemic lockdown on environmental health warrants the scientific community's attention. Thus, this article examined and narratively reviewed the impact of several drastic measures taken on the macro environment and holistic planetary health. We note that the amount of pollution in the air, water, soil, and noise showed a significant decline during the pandemic. Global air quality improved due to lower anthropogenic emissions of air pollutants and atmospheric particles. Water ecosystems also demonstrated signs of recuperation in many countries. Less commercial fishing internationally resulted in the restoration of some aquatic life. Additionally, significant reduction of solid and water waste led to less soil pollution. Some places experienced cleaner beaches and ocean water while wildlife sightings in urban areas across the world occurred more often. Lastly, the COVID-19 pandemic lockdown also led to a worldwide decline in noise pollution. However, the beneficial environmental effects will not be permanent as the world gradually returns to its pre-pandemic status quo. Therefore, behavioural changes such as adopting a lifestyle that reduces carbon footprint are needed to make a positive impact on the environment. In addition, world leaders should consider the national policy changes necessary to ensure continuity of as many of the positive environmental impacts from the COVID-19 pandemic lockdown as possible. Those changes would also serve to lessen the likelihood of another zoonotic calamity.
  7. Molecular complexity of mammary glands development: a review of lactogenic differentiation in epithelial cells
    Jena MK, Khan FB, Ali SA, Abdullah A, Sharma AK, Yadav V, et al.
    Artif Cells Nanomed Biotechnol, 2023 Dec;51(1):491-508.
    PMID: 37694522 DOI: 10.1080/21691401.2023.2252872
    The mammary gland is a dynamic organ with various physiological processes like cellular proliferation, differentiation, and apoptosis during the pregnancy-lactation-involution cycle. It is essential to understand the molecular changes during the lactogenic differentiation of mammary epithelial cells (MECs, the milk-synthesizing cells). The MECs are organized as luminal milk-secreting cells and basal myoepithelial cells (responsible for milk ejection by contraction) that form the alveoli. The branching morphogenesis and lactogenic differentiation of the MECs prepare the gland for lactation. This process is governed by many molecular mediators including hormones, growth factors, cytokines, miRNAs, regulatory proteins, etc. Interestingly, various signalling pathways guide lactation and understanding these molecular transitions from pregnancy to lactation will help researchers design further research. Manipulation of genes responsible for milk synthesis and secretion will promote augmentation of milk yield in dairy animals. Identifying protein signatures of lactation will help develop strategies for persistent lactation and shortening the dry period in farm animals. The present review article discusses in details the physiological and molecular changes occurring during lactogenic differentiation of MECs and the associated hormones, regulatory proteins, miRNAs, and signalling pathways. An in-depth knowledge of the molecular events will aid in developing engineered cellular models for studies related to mammary gland diseases of humans and animals.
  8. Fulltext Strategies in fed-batch cultivation on the production performance of Lactobacillus salivarius I 24 viable cells
    Ming LC, Halim M, Rahim RA, Wan HY, Ariff AB
    Food Sci Biotechnol, 2016;25(5):1393-1398.
    PMID: 30263421 DOI: 10.1007/s10068-016-0217-1
    The potential use of fed-batch cultivation (FBC) for improvement of the production of Lactobacillus salivarius I 24 biomass for subsequent use as probiotics was studied using a 2-L stirredtank bioreactor. Three different constant feeding rates (0.1, 0.05, and 0.033 L/h) were applied in FBCs and their effect on carbon metabolism was evaluated. The carbon flux for cell built-up with reduction in lactic acid synthesis was observed in the fed-batch as compared to the batch cultivation mode. The viable cell number obtained in the constant FBC (CFBC) operated at a feeding rate of 0.05 L/h was 8 times higher (10.7×1010 CFU/mL) than that recorded in the batch cultivation. This gave the viable cell yield based on glucose consumed for CFBC of 26 times higher (11.3×1012 CFU/gGlucose) than the batch cultivation. This study demonstrated CFBC, which is simple with minimal use of process control equipment, has an industrial potential for improvement of probiotic production.
  9. Fulltext Multifaceted Pharmacological Potentials of Curcumin, Genistein, and Tanshinone IIA through Proteomic Approaches: An In-Depth Review
    Khan FB, Singh P, Jamous YF, Ali SA, Abdullah, Uddin S, et al.
    Cancers (Basel), 2022 Dec 30;15(1).
    PMID: 36612248 DOI: 10.3390/cancers15010249
    Phytochemicals possess various intriguing pharmacological properties against diverse pathological conditions. Extensive studies are on-going to understand the structural/functional properties of phytochemicals as well as the molecular mechanisms of their therapeutic function against various disease conditions. Phytochemicals such as curcumin (Cur), genistein (Gen), and tanshinone-IIA (Tan IIA) have multifaceted therapeutic potentials and various efforts are in progress to understand the molecular dynamics of their function with different tools and technologies. Cur is an active lipophilic polyphenol with pleiotropic function, and it has been shown to possess various intriguing properties including antioxidant, anti-inflammatory, anti-microbial, anticancer, and anti-genotoxic properties besides others beneficial properties. Similarly, Gen (an isoflavone) exhibits a wide range of vital functions including antioxidant, anti-inflammatory, pro-apoptotic, anti-proliferative, anti-angiogenic activities etc. In addition, Tan IIA, a lipophilic compound, possesses antioxidant, anti-angiogenic, anti-inflammatory, anticancer activities, and so on. Over the last few decades, the field of proteomics has garnered great momentum mainly attributed to the recent advancement in mass spectrometry (MS) techniques. It is envisaged that the proteomics technology has considerably contributed to the biomedical research endeavors lately. Interestingly, they have also been explored as a reliable approach to understand the molecular intricacies related to phytochemical-based therapeutic interventions. The present review provides an overview of the proteomics studies performed to unravel the underlying molecular intricacies of various phytochemicals such as Cur, Gen, and Tan IIA. This in-depth study will help the researchers in better understanding of the pharmacological potential of the phytochemicals at the proteomics level. Certainly, this review will be highly instrumental in catalyzing the translational shift from phytochemical-based biomedical research to clinical practice in the near future.
  10. Fulltext Illuminating the Molecular Intricacies of Exosomes and ncRNAs in Cardiovascular Diseases: Prospective Therapeutic and Biomarker Potential
    Khan FB, Uddin S, Elderdery AY, Goh KW, Ming LC, Ardianto C, et al.
    Cells, 2022 Nov 18;11(22).
    PMID: 36429092 DOI: 10.3390/cells11223664
    Cardiovascular diseases (CVDs) are one of the leading causes of death worldwide. Accumulating evidences have highlighted the importance of exosomes and non-coding RNAs (ncRNAs) in cardiac physiology and pathology. It is in general consensus that exosomes and ncRNAs play a crucial role in the maintenance of normal cellular function; and interestingly it is envisaged that their potential as prospective therapeutic candidates and biomarkers are increasing rapidly. Considering all these aspects, this review provides a comprehensive overview of the recent understanding of exosomes and ncRNAs in CVDs. We provide a great deal of discussion regarding their role in the cardiovascular system, together with providing a glimpse of ideas regarding strategies exploited to harness their potential as a therapeutic intervention and prospective biomarker against CVDs. Thus, it could be envisaged that a thorough understanding of the intricacies related to exosomes and ncRNA would seemingly allow their full exploration and may lead clinical settings to become a reality in near future.
  11. Fulltext 2D nanostructures: Potential in diagnosis and treatment of Alzheimer's disease
    Tufail S, Sherwani MA, Shamim Z, Abdullah, Goh KW, Alomary MN, et al.
    Biomed Pharmacother, 2024 Jan;170:116070.
    PMID: 38163396 DOI: 10.1016/j.biopha.2023.116070
    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.
  12. Fulltext Virtual Screening, Synthesis, and Biological Evaluation of Some Carbohydrazide Derivatives as Potential DPP-IV Inhibitors
    Jadhav PB, Jadhav SB, Zehravi M, Mubarak MS, Islam F, Jeandet P, et al.
    Molecules, 2022 Dec 24;28(1).
    PMID: 36615348 DOI: 10.3390/molecules28010149
    Dipeptidyl peptidase-4 (DPP-IV) inhibitors are known as safe and well-tolerated antidiabetic medicine. Therefore, the aim of the present work was to synthesize some carbohydrazide derivatives (1a-5d) as DPP-IV inhibitors. In addition, this work involves simulations using molecular docking, ADMET analysis, and Lipinski and Veber's guidelines. Wet-lab synthesis was used to make derivatives that met all requirements, and then FTIR, NMR, and mass spectrometry were used to confirm the structures and perform biological assays. In this context, in vitro enzymatic and in vivo antidiabetic activity evaluations were carried out. None of the molecules had broken the majority of the drug-likeness rules. Furthermore, these molecules were put through additional screening using molecular docking. In molecular docking experiments (PDB ID: 2P8S), many molecules displayed more potent interactions than native ligands, exhibiting more hydrogen bonds, especially those with chloro- or fluoro substitutions. Our findings indicated that compounds 5b and 4c have IC50 values of 28.13 and 34.94 µM, respectively, under in vitro enzymatic assays. On the 21st day of administration to animals, compound 5b exhibited a significant reduction in serum blood glucose level (157.33 ± 5.75 mg/dL) compared with the diabetic control (Sitagliptin), which showed 280.00 ± 13.29 mg/dL. The antihyperglycemic activity showed that the synthesized compounds have good hypoglycemic potential in fasting blood glucose in the type 2 diabetes animal model (T2DM). Taken all together, our findings indicate that the synthesized compounds exhibit excellent hypoglycemic potential and could be used as leads in developing novel antidiabetic agents.
  13. Gas Chromatography-Mass Spectrometry (GC-MS) Analysis of Scaphium Affine Seed Extract and Assessment of its Anti-Hemorrhoidal Efficacy
    Abbas SA, Khan A, Fatima M, Kalusalingam A, Kanakal MM, Inamdar SK, et al.
    Antiinflamm Antiallergy Agents Med Chem, 2024 Feb 14.
    PMID: 38357954 DOI: 10.2174/0118715230285370240131111539
    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-1β, 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.

  14. Investigation of Filler Effects on the Compounding of Freeze-dried Orodispersible Tablets Containing Annona muricata Extract
    Azman SEN, Abd Razak FS, Kamal WHBW, Zheng GK, Ming LC, Uddin AH, et al.
    Int J Pharm Compd, 2020 11 21;24(6):509-514.
    PMID: 33217741
    Orally disintegrating tablets are a solid dosage form that will disintegrate rapidly within 3 minutes upon contact with saliva. Fillers or diluents are excipients that are used to make up the volume of orally disintegrating tablets, and some might act as a disintegrant or binder that will affect the physical properties of orally disintegrating tablets. The objective of this study was to formulate and evaluate physical properties of orally disintegrating tablets containing Annona muricata leaves extract by a freeze-drying method using different fillers at different concentrations. In this study, fifteen formulations of orally disintegrating tablets were prepared by a freeze-drying method with different fillers such as starch, lactose, microcrystalline cellulose, StarLac, and CombiLac at 5%, 10%, and 15%. The orally disintegrating tablets were evaluated for hardness, thickness, weight variation, friability, and disintegration time test. The optimum formulation was chosen and incorporated with Annona muricata leaves extract. The results obtained in this work indicated that Formulation 3, with 15% starch, was the most optimum formulation due to the shortest disintegration time (21.08 seconds ± 4.24 seconds), and all the physical tests were within the acceptable range. The orally disintegrating tablets containing Annona muricata leaves extract possessed antioxidant activity and stable at least for 3 months under 60°C and 75% relative humidity.
  15. Comparison of Disintegrant-addition Methods on the Compounding of Orodispersible Tablets
    Mahesparan VA, Bin Abd Razak FS, Ming LC, Uddin AH, Sarker MZI, Bin LK
    Int J Pharm Compd, 2020 3 21;24(2):148-155.
    PMID: 32196477
    Orodispersible tablets disintegrate rapidly (within 3 minutes) in the oral cavity and release the medicament before swallowing. The mode of disintegrant addition might affect the properties of orodispersible tablets. The objective of this study was to formulate and evaluate orodispersible tablets by studying different modes of disintegration addition with varying concentrations of disintegrants. The wet granulation method was used to produce the orodispersible tablets. Two methods of disintegration addition were compared (i.e., intragranular, extragranular). Three disintegrants (i.e., cornstarch, sodium starch glycolate, crospovidone) were used at three levels (5%, 10%, and 15%) in the study. The formulations were tested for the powder flowability (angle of repose) and characterized physically (hardness, weight, thickness, friability, disintegration time). The mangosteen pericarp extract was used as a model active pharmaceutical ingredient to be incorporated into the optimum formulation. It was observed that the extragranular method produced granules with better flowability compared to that of the intragranular method. Crospovidone was found as the most efficient disintegrant among the three. The optimum formulation selected was one with the highest concentration of crospovidone (15%), which showed the fastest disintegration time. The mode of disintegrant addition into the orodispersible tablets formulation was found to show a marked difference in the disintegration, as well as other physical characteristics of the orodispersible tablets where the extragranular mode of addition showed better property, which caused the orodispersible tablets to disintegrate the fastest.
  16. Investigation of the Effects of Excipients in the Compounding of Amlodipine Besylate Orally Disintegrating Tablets
    Azmi NHS, Ming LC, Uddin ABMH, Sarker ZI, Bin LK
    Int J Pharm Compd, 2022 1 27;26(1):80-87.
    PMID: 35081048
    Oral drug delivery has been recognized as the most desirable drug administration method among other drug delivery routes due to its ease of administration, long shelf life, and low cost. Orally disintegrating tablets disintegrate within seconds in the mouth without the need of water for swallowing. This unique feature of orally disintegrating tablets is favorable to special populations such as geriatric and pediatric patients. Formulation optimization is significant to obtain the optimal combination of tablet constituents, as the tablet composition is influential on dosage-form characteristics. The objective of this study was to investigate the effect of different types of fillers and percentage on the physical properties of orally disintegrating tablets by using amlodipine as the model drug. Blank orally disintegrating tablets containing different fillers, namely, Sorbolac 400, Granulac 200, and CombiLac with different percentages, were prepared using the wet granulation method and were evaluated based on weight variation, hardness, thickness, friability, and disintegration time. Formulation 5 that consists of 25% Granulac 200 showed the optimal result among all formulations with the fastest disintegration time (96.17 s Å} 18.40) and sufficient tablet hardness (4.59 kg Å} 0.70). Hence, formulation 5 was selected as the optimal formulation and incorporated with amlodipine. From this study, it can be concluded that excipients have an essential role in determining the physical properties of orally disintegrating tablets.
  17. 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.
  18. 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.
  19. Fulltext Molecular mechanisms underlying the clinical efficacy of panobinostat involve Stochasticity of epigenetic signaling, sensitization to anticancer drugs, and induction of cellular cell death related to cellular stresses
    El Omari N, Bakrim S, Khalid A, Abdalla AN, Almalki WH, Lee LH, et al.
    Biomed Pharmacother, 2023 Aug;164:114886.
    PMID: 37224752 DOI: 10.1016/j.biopha.2023.114886
    Panobinostat, also known as Farydak®, LBH589, PNB, or panobinostat lactate, is a hydroxamic acid that has been approved by the Food and Drug Administration (FDA) for its anti-cancer properties. This orally bioavailable drug is classified as a non-selective histone deacetylase inhibitor (pan-HDACi) that inhibits class I, II, and IV HDACs at nanomolar levels due to its significant histone modifications and epigenetic mechanisms. A mismatch between histone acetyltransferases (HATs) and HDACs can negatively affect the regulation of the genes concerned, which in turn can contribute to tumorigenesis. Indeed, panobinostat inhibits HDACs, potentially leading to acetylated histone accumulation, re-establishing normal gene expression in cancer cells, and helping to drive multiple signaling pathways. These pathways include induction of histone acetylation and cytotoxicity for the majority of tested cancer cell lines, increased levels of p21 cell cycle proteins, enhanced amounts of pro-apoptotic factors (such as caspase-3/7 activity and cleaved poly (ADP-ribose) polymerase (PARP)) associated with decreased levels of anti-apoptotic factors [B-cell lymphoma 2 (Bcl-2) and B-cell lymphoma-extra-large (Bcl-XL)], as well as regulation of immune response [upregulated programmed death-ligand 1 (PD-L1) and interferon gamma receptor 1 (IFN-γR1) expression] and other events. The therapeutic outcome of panobinostat is therefore mediated by sub-pathways involving proteasome and/or aggresome degradation, endoplasmic reticulum, cell cycle arrest, promotion of extrinsic and intrinsic processes of apoptosis, tumor microenvironment remodeling, and angiogenesis inhibition. In this investigation, we aimed to pinpoint the precise molecular mechanism underlying panobinostat's HDAC inhibitory effect. A more thorough understanding of these mechanisms will greatly advance our knowledge of cancer cell aberrations and, as a result, provide an opportunity for the discovery of significant new therapeutic perspectives through cancer therapeutics.
  20. Fulltext Molecular mechanistic pathways underlying the anticancer therapeutic efficiency of romidepsin
    El Omari N, Lee LH, Bakrim S, Makeen HA, Alhazmi HA, Mohan S, et al.
    Biomed Pharmacother, 2023 Aug;164:114774.
    PMID: 37224749 DOI: 10.1016/j.biopha.2023.114774
    Romidepsin, also known as NSC630176, FR901228, FK-228, FR-901228, depsipeptide, or Istodax®, is a natural molecule produced by the Chromobacterium violaceum bacterium that has been approved for its anti-cancer effect. This compound is a selective histone deacetylase (HDAC) inhibitor, which modifies histones and epigenetic pathways. An imbalance between HDAC and histone acetyltransferase can lead to the down-regulation of regulatory genes, resulting in tumorigenesis. Inhibition of HDACs by romidepsin indirectly contributes to the anticancer therapeutic effect by causing the accumulation of acetylated histones, restoring normal gene expression in cancer cells, and promoting alternative pathways, including the immune response, p53/p21 signaling cascades, cleaved caspases, poly (ADP-ribose) polymerase (PARP), and other events. Secondary pathways mediate the therapeutic action of romidepsin by disrupting the endoplasmic reticulum and proteasome and/or aggresome, arresting the cell cycle, inducing intrinsic and extrinsic apoptosis, inhibiting angiogenesis, and modifying the tumor microenvironment. This review aimed to highlight the specific molecular mechanisms responsible for HDAC inhibition by romidepsin. A more detailed understanding of these mechanisms can significantly improve the understanding of cancer cell disorders and pave the way for new therapeutic approaches using targeted therapy.
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