Journal of Applied Pharmaceutical Science (JAPS)
Permanent URI for this collection
Editor: Dr. Khalid Akhter Ansari
ISSN: 2231-3354; (Print)
Frequency: 12 issues a year
Language: Englishh
An Official Publication of Open Science Publishers
Open Access Peer-reviewed journal
Web site: https://www.japsonline.com/
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Item Antioxidative constituents of Mitragyna diversifolia plant extract and their protective effect on H2O2-induced oxidative stress in L6 myotubes(Open Science Publishers LLP, 2025-04) Hama, I; Vonghirundecha, P; Wungsintaweekul, B; Boonsut, R; Limsuwanchote, S; Wungsintaweekul, J.This study aimed to evaluate the antioxidative constituents of Mitragyna diversifolia (Wall. ex G. Don) Havil. (MD). Total phenolic, total condensed tannin, and total flavonoid contents were determined. Antioxidant activities were assessed using colorimetric assays. The results indicated that the leaf crude extract (LCE) had the highest total phenolic, total condensed tannin, and total flavonoid contents compared to the extracts from branches, stem barks, and fruits. The antioxidative capacity of LCE exhibited IC50 values of 459.19 ± 9.08 ?g/ml for 2,2-diphenyl-1-picrylhydrazyl assay and 150.93 ± 7.59 ?g/ml for lipid peroxidation assay, with an ferric ion reducing antioxidant power value of 279.88 ± 2.54 ?M gallic acid equivalent/g extract. After fractionating the LCE through the Toyopearl® HW-40 column, the enriched polyphenolic fraction (Fr 5) was obtained. The chemical profiles of Fr 5 using high-performance thin-layer chromatography and liquid chromatography-electrospray ionization tandem mass spectrometry were constructed. All fractions were further evaluated for their protective effect on H2O2-induced oxidative stress in L6 myotubes cell line. The protective effect was found in cells treated with 25–100 ?g/ml of Fr 5. The present study concluded that the enriched polyphenolic fraction of MD has antioxidative potential and reduces oxidative stress in L6 myotubes.Item Immunostimulatory effects of Physalis angulata L fruit extract: An in vitro and in vivo studies(Open Science Publishers LLP, 2025-04) Riski, R; Adnyana, IK; Nugraha, YP; Rachmawati, H.Physalis angulata L fruit extract is a promising natural substance with immunomodulatory properties. Therefore, this study aimed to characterize and investigate the immunostimulatory effect of P. angulata L fruit extract using hematological parameters and nitric oxide (NO) production. Fruit extract was characterized through standardization, LC-ESI-MS analysis, and determination of total phenolic content. In vivo immunostimulatory effect tests were conducted on Wistar rats using hematological parameters. Meanwhile, an in vitro test was performed on RAW 264.7 cells through cell viability and NO assays. LC-ESI-MS analysis showed 16 secondary metabolite compounds in P. angulata L fruit extract, and the total phenolic content was 2.895 mg/g gallic acid. Additionally, an in vivo immunostimulatory effect test identified that a 300 mg/70 kg BW dose of fruit extract increased the levels of leukocytes, lymphocytes, monocytes, and granulocytes in male Wistar rats. In vitro test results showed that cell viability induced by P. angulata L fruit extract averaged above 100% to a concentration of 500 ppm. Furthermore, NO production in cells administered with extract was higher compared to other treatments. In conclusion, P. angulata L fruit extract could enhance the immune system, suggesting the potential for development as a natural immunostimulant.Item Development and validation of an LC-MS/MS method for pharmacokinetic assessment of tucatinib in rat plasma(Open Science Publishers LLP, 2025-04) Ramarao, BV; Kamalakaran, AS.Tucatinib, a selective HER2 tyrosine kinase inhibitor demonstrating unique survival benefits for HER2-positive breast cancer patients, can be precisely measured in rat plasma using a validated LC-MS/MS method. To ensure reliable quantification, the method incorporates Imatinib as an internal standard (IS). This allows for the accurate measurement of Tucatinib concentrations over a wide linear range, spanning from 0.05 to 1000 ng/ml. Protein precipitation is employed for sample preparation. This involves adding 2:1 acetonitrile (200 ?l) to rat plasma (100 ?l) to extract both Tucatinib and the IS. The combination of a Kinetex C18 column and a gradient mobile phase system achieves rapid and clean separation of Tucatinib and the IS in only 1.5 minutes. For separation, two mobile phases: A (water with 0.1% formic acid) and B (a 50:50 mix of acetonitrile and methanol, both with 0.1% formic acid) were used. This approach facilitated the sensitive detection of both Tucatinib and the IS using a specific method named positive electrospray ionization (ESI) in multiple reaction monitoring (MRM) mode. ESI-MRM enhances the selectivity of the analysis, ensuring we only measure the desired compounds. The method achieves a low limit of quantification (LLOQ) of 0.05 ng/ml, indicating its high sensitivity for detecting Tucatinib. Excellent linearity was observed for the standard curve (r² > 0.9997) across a broad concentration range of 0.05 to 1000 ng/ml. This signifies a strong, positive relationship between Tucatinib concentration and the instrument›s response. Furthermore, the method adheres to the established criteria set by the Food and Drug Administration for both precision and accuracy, assessed within and between days (intra- and inter-day). To ensure the method’s robustness, stability studies evaluated Tucatinib and the IS under various conditions, including bench-top stability, auto-sampler compatibility, long-term storage, and freeze-thaw cycles. This successful validation paves the way for the method’s reliable application in pharmacokinetic studies.Item Bioanalytical method validation of rifapentine and its metabolite in human plasma using the LC-MS/MS method, as well as its application to a pharmacokinetics study(Open Science Publishers LLP, 2025-04) Parghale, R; Inapakolla, R; Tikka, VDR; Suvvaru, RK; Date, P; Gawade, V; Anil, A; Jagdale, SC.A highly sensitive and specific LC-MS/MS technique was developed. It is validated for quantifying rifapentine and 25-desacetyl rifapentine in K2EDTA human plasma. The concentration ranges are 60.061 ng/ml to 8008.134 ng/ml for Rifapentine and 30.000 ng/ml to 4000.015 ng/ml for 25-desacetyl rifapentine. The separation of analytes were achieved using reverse phase chromatography employing a Supelco discovery C18 column (10 cm × 4.6 mm, 5 ?m particle size). Detection was performed via electro spray ionization in positive ion mode [M+H]+. A triple quadrupole mass spectrometer, with multiple reaction monitoring of specific ions for each analyte and their respective deuterated internal standards (IS) were used. Retention times for rifapentine and 25-desacetyl rifapentine were 2.45 minutes and 1.77 minutes, respectively. The retention time for the IS rifapentine D9 and 25-desacetyl rifapentine D8 were 2.30 minutes and 1.68 minutes, respectively. The total run time of the method was 8.00 minutes. No interfering peaks or matrix effects were noticed during validation, confirming the reliability of the results. The validation report encompasses standard curves, quality control sample recovery, stability of experiments, and meeting stringent criteria for sensitivity, reproducibility, and accuracy. This method has been effectively used in a rifapentine bioequivalency study with healthy adult Asian male volunteers, highlighting its suitability for pharmacokinetic investigations.Item Antioxidant potential of melanin pigment from marine sponge-associated actinomycete Micromonospora sp.(Open Science Publishers LLP, 2025-04) Aqlinia, M; Astuti, RI; Prastya, ME; Wahyudi, AT.Melanin pigment is a dark-colored natural biopolymer produced by microbes, such as actinomycetes. Melanin has various potential bioactivities, including antioxidant activity. This study aimed to determine the antioxidant and photoprotective properties of melanin extracted from the marine sponge-associated actinomycete Micromonospora fulva HV6. Antioxidant properties were measured by spectrometric techniques using 2,2?-diphenyl-1-picrylhydrazyl (DPPH) and 2,2?-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods, and photoprotective properties were evaluated by measuring the sun protection factor (SPF). The IC50 values exhibited potent antioxidant activity of melanin in reducing DPPH and ABTS in vitro at concentrations of 31.55 ± 0.60 ?g/ml and 63.07 ± 3.29 ?g/ ml, respectively. At the cellular level, 240 ?g/ml melanin improved the viability of Schizosaccharomyces pombe under severe H2O2-induced stress better than L-ascorbic acid did, indicating its potential to prolong the longevity of yeast cells. Melanin also increased mitochondrial activity and induced oxidative stress tolerance, likely through mitochondrial adaptive reactive oxygen species signaling, similar to the response induced by calorie restriction. Melanin exhibited photoprotective properties with an SPF value of 20.78. In summary, the melanin pigment extracted from M. fulva HV6 showed potential as a natural antioxidant from a rare actinomycete group for medical and pharmacological applications.Item LC-MS/MS profiling and in silico molecular docking analysis of water-soluble bioactive compounds from Pleurotus pulmonarius as potential immunomodulators on monocyte immune response(Open Science Publishers LLP, 2025-04) Arromsava, A; Chuchawankul, S; Amornsupak, K.Pleurotus pulmonarius is an affordable edible fungus extensively utilized in food and traditional medicine. This study aims to comprehensively profile the water-soluble bioactive compounds in P. pulmonarius and identify those responsible for modulating monocyte immune response. The crude extract, prepared through hot water extraction, was analyzed for its biological activities using untargeted LC/MS-MS analysis and molecular docking. The potential compound-targeted proteins in monocytes were investigated and further identified using the MCODE algorithm. The pharmacokinetic properties and the biological activity of tentative compounds were studied using absorption, distribution, metabolism, excretion, and toxicity (ADMET) and PASS analysis. The findings revealed that 164 chromatographic peaks were detected in ESI-positive mode, and 36 bioactive compounds were proposed. The top seven candidate compounds found abundantly in the mushroom were selected, including diacylglycerol, phosphatidylethanolamine, phosphatidylinositol, glutathione, quercetin 3-(6-O-acetyl-beta-glucoside), dihydroresveratrol, and aspartic acid. Notably, glutathione, quercetin, and dihydroresveratrol demonstrated promising potential proinflammatory inhibitors, with their binding affinities surpassing those of known inhibitors (?2.32 kcal/ mol for glutathione; ?6.76 kcal/mol for quercetin and ?5.02 to ?7.02 kcal/mol for dihydroresveratrol). Additionally, dihydroresveratrol showed promise as an immunomodulatory agent due to its favorable absorption, distribution, and safety profile. These findings highlight the potential of P. Pulmonarius, particularly dihydroresveratrol as a natural alternative immunomodulator for addressing monocyte-related inflammation.Item Knowledge, attitude, and practice of doctors and nurses about the disposal of expired and unused medicines in Dhaka city(Open Science Publishers LLP, 2025-04) Shakib, FF; Ratul, T; Uddin, MB.Improper medicine disposal practice has become a major concern in South Asian countries. Many healthcare professionals are not aware of safe medicine disposal practices. This survey study aimed to assess the knowledge, attitude, and practice (KAP) of unused and expired medicines among doctors and nurses in Dhaka City. A questionnaire-based, cross-sectional survey was conducted among 150 respondents. Respondents were classified into two categories: doctors = 100, and nurses = 50. Data collection was done using a pre-validated, structured questionnaire. Collected data were added to the MS Excel spreadsheet and analyzed by Statistical Package for Social Science version 23.0. Two-thirds of the nurses kept expired medicines in their houses as they did not want to waste them whereas 50% of doctors had expired medicines. Remarkably, 42.86% of nurses responded to immune system deficiencies resulting from improper medicine disposal, while it figured 28.16% among doctors. Alarmingly, 95.46% of nurses disposed of medicines via flush in the toilet/basin or dump in the dustbin, and 69.79% of doctors followed similar practices. 27.43% of doctors and 13.85% of nurses recommended reducing the number of medicines from prescription. It has been suggested that health policymakers work together with healthcare professionals and general people by launching public awareness campaigns.Item Assessments of anti-breast cancer activity and profiling of active compounds using LC-MS/MS from the Indonesian Agelas nakamurai(Open Science Publishers LLP, 2025-04) Murniasih, T; Hadi, TA; Ahmadi, P; Sari, M; Bustanussalam, B; Hadisaputri, YE; Putra, MY; Rahmawati, SI; Indriani, DW.Breast cancer is now one of the leading causes of death in women worldwide. Finding a cure is, therefore, critical for women’s health. Marine sponge-derived drugs have gained interest in breast cancer treatment. The development of marine natural products into cancer therapy includes several stages. It starts with the screening using the cytotoxic test method, a preclinical trial using the animal mode, clinical trial phases I and II. In this study, we focus on the basic cytotoxic test to find the new source of anti-breast cancer compounds derived from Agelas nakamurai to know the potential for further investigation to become lead compounds. However, the anti-breast cancer potential of the Indonesian marine sponge A. nakamurai has never been studied. This study aimed to evaluate the anti-breast cancer potential of extract and fraction of A. nakamurai against epithelial human breast cancer cells (MDA-MB-231 and MCF-7 cells line) and to preliminary profile the known active compounds. The maceration using methanol was used for extraction and followed by partitioning with varied solvents [ethyl acetate (EtOAc), butanol, and water]. Fractionation was done using normal phase open column chromatography, and the liquid chromatography mass spectrometry/mass spectrometry (LC-MS/MS) was used for analyzing compounds. MDA-MB-231, MCF-7, and HEK-293 cell lines were used for biological activities. The chromatographic separation of the EtOAc fraction led to the F7 subfraction which strongly inhibits proliferation against the MDA-MD-231 (IC50: 10.677 ?g/mL), MCF-7 (IC50: 15.154 ?g/mL), and HEK-293 cells line. The LC-MS/MS data of active fraction F7 contained agelasin-D and ageloxime-D. This study reported that fraction 7 of A. nakamurai showed strong activity against MDA-MB-231, MCF-7, and HEK-293 cell lines. Further analysis will be carried out to know the mechanisms of action of active compounds.Item Development of a quality by design based hybrid RP-HPLC method for Glimepiride: Bioanalytical and industrial applications(Open Science Publishers LLP, 2025-04) Kumar, A; Dhiman, C; Kumar, M; Kannappan, N; Kumar, D; Chourasia, MK; Narayan, KP.In this study, we present a hybrid analytical method for the quantification of glimepiride (GLP) from blood plasma and pharmaceutical formulations. Shimadzu HPLC (Model SIL 20 AC HT), a photodiode array detector, and a Phenomenex C18 column (150 × 4.6 mm, 4 ?m) were used for method development. A further quality by design (QbD) surface optimization model was applied, and the best-optimized method with chromatographic conditions, such as an injection volume of 15 ?l, a column oven temperature of 40°C, a sample cooler temperature of 15°C ± 1°C, a run time of 5 minutes, and a flow rate of 0.8 ml/minute with a mobile phase composition (acetate buffer: acetonitrile, 40:60 ratio), was identified. Finally, the method was validated, and GLP was quantified from various pharmaceutical dosage forms and blood plasma. The results were observed in subsequent laboratories in diluent media and mouse plasma with limits of detection of 0.066 ?g/ml and 0.193 ?g/ml, respectively, followed by limits of quantification of 0.199 ?g/ml and 0.583 ?g/ml, respectively. Subsequently, linearity (r2) was observed at 0.999 for both samples. The ?max was 228 ± 2 nm, and the retention time (RT) was 2.8 ± 0.28 minutes. The plasma matrix effect was calculated to be 81.9%. The research findings revealed that the proposed analytical method could be used for both analytical and bioanalytical applications at the industrial scale.Item Harnessing the potential of TiO2 nanoparticles from marine macroalgae Ulva lactuca for antibacterial, anti-inflammatory, and cytotoxic properties(Open Science Publishers LLP, 2025-04) Mariyam, MSA; Subbarayan, RR; Dhanraj, G.The present investigation explores the green synthesis of titanium dioxide nanoparticles (NPs) using an aqueous extract of Ulva lactuca, a medicinally important marine macroalgae. Characterization of UL-TiO2NPs showed an intense peak at 371 nm. Fourier transform-infrared spectroscopy analysis showed the presence of functional groups such as hydroxyls, carbonyls, methylene, aliphatic and aromatic hydrocarbons, amines, and ethers. X-ray diffraction confirmed the crystalline nature of the biosynthesized UL-TiO2NPs with sizes in the range of 20 and 50 nm. Scanning electron microscope analysis emphasized the morphology of TiO2NPs to be spherical-shaped with minimal clustering. Antibacterial activity indicated profound inhibitory zones against clinical isolates (12–19 mm) rather than against microbial type culture collection bacterial pathogens (9–14 mm). The anti-inflammatory activity of the UL-TiO2NPs was affirmed by a remarkable reduction (22%–78%) of protein denaturation. Anticancer activity of UL-TiO2NPs against oral oral carcinoma cell line carcinoma cells showed a notable reduction in viability of cells (94.31%–17.4%) with respect to an increase in concentrations and recorded an IC50 value of 28.74 ?g/ml. Thus, the distinct properties of biologically synthesized titanium dioxide NPs imply that they could be efficiently utilized as a nano-antibiotic coating on the surface of healthcare devices and as a drug carrier in anticancer studies.Item Effect of Eleutherine americana (aubl.) Merr ethanol extracts against high lipid profile and arterial stiffness in high-fat high-cholesterol diet-induced rats(Open Science Publishers LLP, 2025-04) Putra, HM; Istiqomah, AN; Hasimun, P; Aplilianti, N; Aligita, W.Comprehensive studies have been carried out on Dayak onion (Eleutherine americana (aubl.) Merr) and its effects on cardiovascular health, specifically on dyslipidemia. However, its effect in relation to arterial stiffness has not been well-studied. This study aims to assess the impact of ethanol extracts of E. americana on high cholesterol levels and arterial stiffness in an animal model with dyslipidemia generated by a high-fat high-cholesterol (HFC) diet. Daily dosages of E. americana at 25, 50, and 100 mg/kg body weight (BW) were administered to the rats for 60 days and their lipid profile, arterial stiffness, heart rate (HR), and histopathology were measured and compared to rats receiving no treatment (negative control) and simvastatin at 1.8 mg/kg BW (positive control). The results indicated that an HFC diet increases the likelihood of cardiovascular issues by raising lipid levels and encouraging the progression of atherosclerosis. This then leads to an increase in arterial stiffness and HR. The ethanol extract of E. americana successfully prevented the rise in lipid profiles and the progression of atherosclerosis, hence preventing HR from increasing and arterial stiffness. The highest effective dosage of E. americana was 100 mg/kg BW, with 50 mg/kg BW yielding similar performance to 1.8 mg/kg BW of simvastatin.Item The potential of citral isomers from lemongrass (Cymbopogon citratus) essential oil as WAT browning agents in obesity by activating AMPK and PPAR?: An in silico approach(Open Science Publishers LLP, 2025-04) Mashitah, MW; Widodo, N; Permatasari, N; Rudijanto, A.Obesity is characterized by abnormal fat accumulation in the white adipose tissue (WAT), posing a significant health risk. Enhancing energy expenditure through WAT browning using dietary components and natural extracts is a promising therapeutic strategy for obesity management. This study explored the efficacy of citral isomers from Cymbopogon citratus (lemongrass) essential oil as agents for WAT browning by activating primarily the proliferator- activated receptor gamma (PPAR?) and AMPK, utilizing an in silico approach. Essentials oil were extracted from lemongrass leaves and stalks via steam-hydro distillation, and the citral isomer content was analyzed through gas chromatography-mass spectrophotometry. Molecular docking was performed using AutoDock Vina, and molecular dynamics simulations were conducted using YASARA. Five citral isomers were identified: geranial, neral, geranial diethyl acetal (GDA), isogeranial, and isoneral isomers. This study identified GDA and neral as the most effective AMPK agonists, acting by directly activating their allosteric sites. Additionally, GDA, isoneral, and neral demonstrate PPAR? agonist properties by stabilising the protein’s active site. In conclusion, citral isomers in lemongrass essential oil hold the potential to act as WAT browning agents in obesity management through the activation of AMPK and PPAR?. Future in vitro and in vivo studies are required to validate these findings.Item Central composite design aided optimization and validation of developed an eco-friendly HPLC method for the quantification of Lenalidomide loaded mesoporous silica nanoparticles(Open Science Publishers LLP, 2025-01) Gupta, A; Rachana, SP; Moorkoth, S; Das, N.Lenalidomide (LND) was encapsulated within mesoporous silica nanoparticles (MSNs), and we developed an reverse-phase (RP)-HPLC analytical method to quantitate the LND content in the formulation. Through a multivariate Central composite design (CCD), we systematically optimized key chromatographic parameters, including the flow rate, sample injection volume, and organic phase ratio. We evaluated the responses of retention time, peak area, and theoretical plate. Our enhanced chromatographic approach employed a Spherisorb ODS C18 column. To investigate the suitableness of the mobile phase for isocratic elution, we adhered to International Conference on Harmonisation Q2(R1) standards. Suggesting the optimality of a methanol and ammonium acetate buffer combination (pH 5.5, adjusted with 1% v/v glacial acetic acid and ammonia solution). This validated RP-HPLC analytical method exhibited specificity for LND even in the presence of the matrix of MSNs. The fabricated MSNs were confirmed by evaluating the surface morphology of the formulation. We successfully applied the developed RP-HPLC method to quantify the amount of LND entrapped and to determine the drug loaded in the MSNs formulation. The % EE for LND in MSNs was found to be 76.66% and % DL for LND in MSNs was found to be 1 4.00%, respectively. The novelty of the Design of expert -based method development is that it reduces the number of trials, thereby reducing solvent wastage and is environmentally friendly, scoring eight green, six yellow, and one red.Item Aqueous root extract of Salacia oblonga ameliorates experimental diabetes by upregulation of PDX1 expression and alpha-to-beta cell trans-differentiation(Open Science Publishers LLP, 2025-04) Anbumani, SK; Shankaranarayanan, A; Thomson, JER; Sadayan, S; Subramanian, M.The global rise in diabetes has spurred interest in plant-based treatments. The plant Salacia oblonga exhibits antidiabetic activity by inhibiting alpha-glucosidase and stimulating insulin secretion. The transcription factor pancreatic and duodenal homeobox 1 (PDX1) is vital for beta cell stimulation, neogenesis, and insulin secretion. This study evaluated the impact of Salacia oblonga on insulin and glucagon secretion and PDX1 expression. Streptozotocin- induced male Wistar albino diabetic rats received glibenclamide (2 mg/kg) and aqueous extract of S. oblonga root (200 mg/kg) orally for 8 weeks. Fasting blood glucose, insulin, glucagon, lipid profiles, and renal markers, were analyzed. Histopathology, immunohistochemistry, and PDX1 protein and gene expression in the pancreas were also assessed. Salacia oblonga significantly reduced fasting blood glucose and enhanced insulin and glucagon secretion in diabetic rats. Histopathology and immunohistochemistry confirmed recovery from streptozotocin-induced damage and increased numbers of beta and alpha cells. Quantitative polymerase chain reaction and western blot analyses showed upregulation of PDX1 expression. Increased alpha cell mass and glucagon and insulin expression indicated alpha-to-beta cell trans-differentiation. Salacia oblonga root extract exhibited antidiabetic properties by upregulating PDX1 expression and promoting alpha-to-beta cell trans-differentiation. It also corrected fat and protein metabolism disturbances, highlighting its potential in preventing diabetic complications and making it a promising candidate for further diabetes research.Item Dietary fiber-based floating in situ gels for improved gastric delivery of roselle extract(Open Science Publishers LLP, 2025-04) Pumjan, S; Praparatana, R; Issarachot, O; Wiwattanapatapee, R.Dietary fiber-based, in situ gelling systems of roselle extract were formulated to prolong the release of anthocyanin in the stomach. The formulations comprised sodium alginate as a gel-forming polymer (0.5%–1% w/v), and a release rate-controlling polymer (0.25% w/v) selected from hydroxyethyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, or konjac glucomannan (KGM). Sodium bicarbonate was included as a flotation agent to generate CO2. The formulations showed fast floatation in less than 5 seconds following contact with simulated gastric fluid and stayed afloat for over 8 hours, releasing more than 80% of the anthocyanin content. An increase of sodium alginate concentration resulted in an increment of the gel strength. The optimized formulation containing KGM provided sustained drug release and higher gel strength than other polymers. It also displayed antioxidant activity as evidenced by radical scavenging effects on 2,2-diphenyl-1-picrylhydrazyl. Anti-inflammatory behavior was demonstrated by inhibition of lipopolysaccharide-activated nitric oxide production in RAW264.7 murine macrophage cells, while cytotoxic activity was measured against human gastric carcinoma cells. These results indicate that in situ gelling systems based on dietary fiber derivatives offer potential as a gastroretentive carrier for improving the systemic bioavailability of anthocyanin and for the local treatment of gastric diseases.Item Evaluation of anticancer activity of Annona muricata leaf targeting FGFR3 and EGFR receptors against bladder and lung cancer(Open Science Publishers LLP, 2025-04) Suhail, P; Venkatachalam, VV; Balasubramanian, T; Murali, R; Renganathan, ABL.The amplification of tyrosine kinase receptors, specifically fibroblast growth factor receptors and epidermal growth factor receptors, is primarily observed in various cancers, including bladder and lung cancer. This study aimed to identify the phytochemical components of Annona muricata leaves and evaluate their anticancer potential. The study used Q-TOF LC/MS analysis to identify phytochemical components and conducted molecular docking studies to predict the binding action of quinic acid. The largest peak was found at a retention time of 10.12 (stephabyssine), followed by 9.97 (procyanidin B2) and 11.83 (quinic acid) minutes, revealing the presence of many phytochemicals. In molecular docking studies, quinic acid was found to interact with the catalytic residues of LEU 478, ALA 557, LYS 476, and ALA 559 with hydrogen bonds, indicating hydrophobic interaction with some amino acids in the hydrophobic pockets of fibroblast-growth factor receptors 3 protein with a docking score of ?9.94 Kcal/mol. It also interacts with the catalytic residues of ASP 831, THR 830, and THR 766 of the epidermal growth factor receptors proteins with a docking score of ?9.103 Kcal/mol. The assessment of anticancer activity was conducted through the measurement of mitochondrial dehydrogenase activity (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay). The IC50 for MCF-7, T47D, HCT-15, and PC-3 were found to be 76.64 ± 2.56, 142.43 ± 1.86, 42.68 ± 2.89, and 152.16 ± 3.21 ?g/ml, respectively. The findings were corroborated by the observed morphological alterations, including membrane blebbing, cell detachment, and rounded cell morphology in comparison to parental cells. The phytochemical analysis, including in vitro and in silico studies, identified significant constituents and key mechanisms of quinic acid as a potential anticancer agent derived from A. muricata leaves.Item Impact of Artocarpus lakoocha heartwood extract and Oxyresveratrol on cholesterol digestion and absorption in Caco-2 cell cultures(Open Science Publishers LLP, 2025-04) Trisat, K; Limpeanchob, N.Cardiovascular diseases are the leading causes of death globally, with hypercholesterolemia being a major contributing factor. While lifestyle changes and dietary modifications are recommended for individuals with moderately high cholesterol, there is growing interest in natural alternatives to help manage blood cholesterol levels. Oxyresveratrol has shown promising antihyperlipidemic properties in animal studies. However, the mechanisms underlying these effects are not fully understood. This study focuses on the direct effects of oxyresveratrol and Puag-Haad, an aqueous extract from the heartwood of Artocarpus lakoocha, on lipid and cholesterol processing in the intestinal tract. The study assessed the inhibitory effects on pancreatic lipase, solubility of cholesterol in lipid micelles, bile acid binding, and absorption of cholesterol into differentiated Caco-2 cells. The results showed that both oxyresveratrol and Puag-Haad exhibited a dose-dependent inhibition of pancreatic lipase. Both compounds also effectively inhibited cholesterol solubility in lipid micelles. Puag-Haad in particular bound to bile acids with higher potency than the standard bile acid binder, cholestyramine. In addition, oxyresveratrol and Puag-Haad inhibited cholesterol uptake into Caco-2 intestinal cells, with efficacy comparable to the cholesterol absorption inhibitor ezetimibe. These findings indicate that oxyresveratrol and Puag-Haad interfere with multiple processes involved in lipid digestion and absorption, making them promising candidates for further development as natural antihyperlipidemic agents.Item Development of tablet formulations containing genistein solid dispersion optimized using Box-Behnken design for enhanced solubility(Open Science Publishers LLP, 2025-04) Phanapithakkun, S; Yusakul, G; Sitthisak, C; Plyduang, T.Genistein, a bioactive isoflavone, offers therapeutic potential but is hindered by poor water solubility, limiting its oral bioavailability. This study aimed to enhance genistein’s solubility by developing solid dispersion (SD) and formulating them into tablets. The SDs were prepared using the solvent evaporation method with polyethylene glycol 4000, poloxamer 407, and crospovidone (XPVP) as carriers. A Box-Behnken design optimized the formulation, yielding a significant increase in solubility to 181.12 ?g/ml, closely matching the predicted value. Characterization studies, including differential scanning calorimetry, attenuated total reflectance-Fourier transform infrared spectroscopy, and powder X-ray diffraction, confirmed the conversion of genistein from a crystalline to an amorphous state without interaction with carriers, contributing to improved solubility and dissolution profile. The optimized genistein-SD was further developed into tablets, demonstrating effective drug release. Genistein-SD tablets containing XPVP showed faster disintegration and higher genistein release than those with sodium starch glycolate. Stability testing under long-term and accelerated storage conditions confirmed the retention of genistein content (?96.61%) over 3 months in both the optimized genistein-SD and genistein-SD tablets. These tablets offer a promising genistein oral delivery approach, supporting further pharmaceutical development.Item QbD assisted RP-HPLC method for determination of Pyridoxine and Doxylamine in pharmaceutical formulation using central composite design(Open Science Publishers LLP, 2025-04) Challa, GN; Kunda, DR; Mustaq, SJH; Marni, N; Ketha, S; Gorle, U; Jakkula, S; Babu Koppisetty, BR.The quality by design enabled the development of cost-effective, simple, precise, and rapid RP-HPLC techniques for determining Pyridoxine (PRD) and Doxylamine (DXA) in the tablet dosage form. Systematic method optimization was performed through central composite design by altering the flow rate and composition of the organic phase in the mobile phase as the critical method parameters for evaluating the necessary analytical attributes, namely the tailing factor, theoretical plate count, and resolution. The optimal separation was achieved on a column with C18 in nature and dimensions of (250 mm length × 4.6 mm id × 5 ?m particle size) composed of a blend of acetate buffer and acetonitrile in a volumetric composition of 35:65, at a flow rate of 1.0 ml/minute. Detection was carried out at 254 nm. The PRD and DXA have retention times of 3.053 and 4.357 minutes, respectively. The developed method was useful for the determination of bulk drugs and formulations.Item Utilizing secretomes as a novel molecular-based therapy for Parkinson’s disease: A scoping review(Open Science Publishers LLP, 2025-04) Hutabarat, EAJ; Suroto, S; Soetrisno, S; Mirawati, DK; Pamungkasari, EP; Wasita, B.Parkinson’s disease (PD) is a neurodegenerative disorder that affects multiple body systems and results in a variety of motor and non-motor symptoms. Recent research has highlighted the importance of secretome, a diverse array of bioactive molecules produced by mesenchymal stem cells (MSCs). This study explores the progress and potential benefits of secretome use in treating PD. A scoping review was conducted following the Preferred Reporting Items for Scoping Reviews protocol, utilizing journals from PubMed Central, ScienceDirect, and Scopus databases with no time restrictions. The findings suggest that secretome shows promise in developing new therapies for PD, particularly due to its superior antioxidant, neuroprotective, and neurodifferentiation effects on dopaminergic neurons compared to MSCs. These effects have been linked to notable improvements in motor, behavioral, and morphological changes. However, for secretome therapy to be effectively implemented in human patients with PD, factors such as production stages, release mechanisms, and administration routes require further investigation.