Journal of Applied Pharmaceutical Science (JAPS)

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https://imsear.searo.who.int/handle/123456789/149611

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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Anti-psoriatic evaluation of aloe emodin-loaded topical hydrogel in an imiquimod-induced human plaque-type psoriasis in BALB/c mice
(Open Science Publishers LLP, 2024-09) Pandey, A; Srivastava, N; Dubey, RC; Dhaneshwar, S; Shukla, AK
Aloe emodin, an anthraquinone derivative, mainly obtained from Aloe vera, possesses an extensive spectrum of pharmacological properties, including anti-proliferative, anticancer, wound healing, analgesic, anti-inflammatory, antibacterial, and antiviral properties. The objective of the present study was to prepare aloe emodin-loaded topical hydrogel formulations for managing plaque-type psoriasis. Different proportions of carbopol 940, chitosan, and hydroxyl propyl methyl cellulose K15M (HPMC K15M) were used as gelling agents. The prepared hydrogels were characterized for pH, viscosity, rheological behavior, spreadability, extrudability, swelling index, drug content, and accelerated stability. Based on physicochemical and in vitro permeation studies, PHGL1 containing aloe emodin (1%) and carbopol 940 (1%) was selected. The acute dermal toxicity study was also conducted as per the OECD guidelines 402. The mechanism of drug release followed Korsemeyer–Peppa’s model. The optimized batch showed a pH range from 6.867 ± 0.015 to 6.91 ± 0.254, drug content 94.6% ± 0.686% w/w of the active principle when studied in triplicate for drug content analysis, the measured viscosity of the formulation was 31402.33 ± 149.0783 mPaS exhibiting a shear thinning system along with thixotropic behavior at 25°C, and sustained drug release of 78% in 8 hours. An ex vivo permeation study demonstrated that 203.73 ?g/ml/cm 2 drug permeated through skin in 24 hours. Application of aloe emodin-loaded topical hydrogel to psoriatic skin resulted in a reduction of epidermal thickness, scaling, and ear thickness. The key inflammatory marker tissue necrosis factor (TNF-?) also showed a significant decrease. Compared with the marketed formulation, the test formulation showed no significant difference in the percentage reduction in ear thickness. No acute dermal toxicity was observed at the initial dose of 200 mg. The outcome suggests the promising potential of aloe emodin-loaded hydrogel in improving plaque-like psoriasis without dermal toxicity. Further studies are warranted to establish its efficacy in the management of psoriasis.
The impact of COVID-19 pandemic on treatment adherence, access to care, and disease control in diabetic patients in Jordan, an online survey
(Open Science Publishers LLP, 2024-09) Al-Taani, GM; Muflih, SM; Alsharedeh, R; Karasneh, R; Al-Azzam, SI.
This study aimed to assess the impact of the COVID-19 pandemic on treatment adherence, access to care, and disease control in diabetic patients. An online survey design was utilized to collect data from a convenient sample of diabetic patients in Jordan. The developed survey collected data on sociodemographic characteristics, COVID-19 impact on access to care in diabetic patients, COVID-19 impact on diabetic patients’ adherence to their medications, and patients’ level of knowledge of COVID-19 impact on their health. Nearly three-quarters of the participants reported that they avoided going to the physician for regular non-emergent visits during the outbreak, and 69.5% stated that their access to insulin, other diabetic medications, and supplies was not affected by the pandemic situation. The majority of patients reported that COVID-19 did not affect their adherence to their medications. Almost 42% reported that COVID-19 has negatively affected their physical activity level and their healthy lifestyle habits, while 60% stated that it did not affect their diet. Additionally, 56.6% reported that they have noticed less control in their blood glucose readings. The findings may reflect that the patients high adherence rate to their medications and that they avoided going to the doctor’s clinic to avoid contracting the virus.
The prediction of pH-dependent interaction using micro-dissolution approach in bio-relevant media: Insights from model drug study of lapatinib
(Open Science Publishers LLP, 2024-06) Rajpurohit, AUS; Patil, PH; Desai, M; Jagadisht, PC.
Understanding the impact of dynamic alterations in gastrointestinal fluid properties and intestinal dissolution of poorly soluble drugs, such as lapatinib, is crucial for predicting drug absorption in vivo. The current study employs a micro-dissolution pH shift model to forecast the dynamic dissolution of lapatinib in buffer and bio-relevant media by application of analytical design of experiments. The utilization of a Box-Behnken design has resulted in a robust analytical method. According to an in vitro micro-dissolving pH shift experiment in United States Pharmacopeia buffers, lapatinib displays a typical weak base pH-dependent solubility, with 15% drug release at pH 1.2 and dropping to 2% at pH 6.5 buffers. In contrast, the solubility of the compound was initially measured to be 0.0127 mg/ ml in fasted state-simulated gastric fluid; however, pH alterations by the addition of fasted state-simulated intestinal fluid 6.5 resulted in a significant increase to 0.0291 mg/ml. The in vitro pH-effect risk for dissolution experiment in biorelevant media is 0.80, suggesting that the existence of salts in fasted state-simulated intestinal fluid results in the formation of a macroaggregate that is accountable for improved solubility of lapatinib. Thus, using a bio-relevant buffer in a pH shift model may improve this in vitro technique’s predictive ability and aid weakly drug advancement in the intestinal environment.
Investigation of the antibacterial activity of synthesized hydroxyapatite Sr-doped nanocomposite
(Open Science Publishers LLP, 2024-09) Jamarun, N; Afriskaa, LN; Welliaa, DV; Prasejatia, A; Amirullaha, TY; Wulandaria; Trycahyania, NA.
Hydroxyapatite is a mineral compound with a composition resembling the components found in human teeth and bones. Hydroxyapatite possesses osteoconductive, bioactive, and biocompatible characteristics. Nevertheless, hydroxyapatite has limitations, particularly its limited antibacterial activity. Therefore, this research uses the sol-gel method to synthesize and characterize strontium hydroxyapatite doped composites (HAp-Sr doped composites). The calcium precursor used in this research comes from the green mussel shells (Perna viridis); the main component is CaCO3 , which will later be converted into CaO compounds. HAp Sr-doped composites were synthesized by varying the concentration of Sr metal (5%, 10%, and 20% w/w), which aimed to determine its good antibacterial ability. The X-ray fluorescence analysis reveals that green mussel shells contain 97.261% calcium oxide (CaO). The X-ray diffraction analysis reveals that the pattern observed at an angle of 2? corresponds to the hydroxyapatite standard from ICDD (No.96-101-1243), which possesses a hexagonal structure. The Fourier transform infrared spectroscopy spectra reveal the presence of PO4 3? groups in the sample at wave numbers 528 cm?1, 604 cm?1, 945 cm?1, and 1,018 cm?1. The antibacterial activity of the HAp-Sr doped composite was evaluated against Staphylococcus aureus and Escherichia coli bacteria. The results indicated that the 5% HAp-Sr doped composite exhibited antibacterial activity. Therefore, it can potentially be utilized in bone grafts and implants.
Evaluation of Lakadong turmeric derived curcumin nanogel against resistant biofilms: In-silico, antibacterial and antibiofilm analysis
(Open Science Publishers LLP, 2024-09) Sarma, SK; Dutta, U; Das, BK; Bharali, A; Laloo, D; Kalita, JM; Sahu, BP
The emergence of drug resistance can lead to increased mortality and morbidity as treatment efficacy declines, and there is an urgent need to explore novel antibacterial compounds with enhanced effectiveness against drugresistant bacteria, particularly resistant biofilms. Curcumin, with its antimicrobial activity, can be a potential safe agent; however, studies on its efficacy against resistant biofilm are limited. This study, therefore, aims to explore the potential of curcumin and/or its novel derivatives against a spectrum of resistant biofilm-related pathogens, including bacteria, fungi, and human pathogens. Another study objective is to investigate the effectiveness of the high-yielding Lakadong turmeric (LKD)-derived curcumin for its antibacterial effects and the ability to inhibit biofilm formation in Gram-positive and Gram-negative bacteria using in-vitro assays. A molecular docking study was used to select the most potential binding interaction between the selected protein structure and ligand molecule for the potential efficacy of curcumin against resistant biofilms. Lakadong-derived curcumin-loaded nano gels (LKD-Cur Nanogel) were prepared and tested for antibacterial (zone-inhibition) and biofilm formation (scanning confocal microscope) activity against Staphylococcus aureus and Pseudomonas aeruginosa. Furthermore, Curcumin derivatives were studied in-silico for potential effectiveness against a spectrum of resistant biofilms. The in-silico results showed that curcumin and/or its novel derivatives exhibited high selectivity toward a range of targeted proteins compared to curcumin. Moreover, LKD-Cur Nanogel exhibited significant anti-bacterial activity with an increased mean zone of inhibition compared to positive control. The biofilm formation assay illustrated that LKD-Cur Nanogel effectively disrupted established bacterial biofilms (both for P. aeruginosa and S. aureus) grown on microtiter plates at a concentration of 1,000 µg/ml compared to the control. Therefore, it can be concluded that curcumin and/or its newly modified derivatives could hold promising antibacterial activity targeting diverse biofilm-associated pathogens based on the in-silico and in-vitro study. Moreover, it can be concluded that LKD-derived curcumin nanogels have good antibacterial and antibiofilm efficacy.
Public awareness towards antibiotics use, misuse and resistance in Saudi community: A cross-sectional population survey
(Open Science Publishers LLP, 2024-09) Bdair, IA; Bdair, OA; Maribbay, GML; Elzehiri, D; Hassan, ES; Tolentino, AD; Emara, MM; Ali, EK; Abdelmeged, RM; Fadul, MO.
Antibiotics (ABs) resistance is a worldwide health issue. However, there is a lack of awareness toward the proper use of ABs. This study was designed to assess the awareness of antibiotic usage and antibiotic resistance (ABR) among the public. A population-based survey was executed from September to November 2023. A validated questionnaire was administered to 600 participants. Data were analyzed through Statistical Package for the Social Sciences version 25. Multivariate regression was administered to identify associated factors with awareness. The results revealed a high prevalence of ABs consumption. The public knowledge of ABs was suboptimal where (50.2%) of the participants had sufficient knowledge. Moreover, it is worth highlighting that respondents hold a generally positive attitude (72.3%) and satisfactory practice (69.7%). Participants who are older, male, educated, married, and employed typically have significantly higher mean scores in knowledge, attitude, and practice. Public awareness about proper antibiotic usage and ABR is a vital public health concern. Considering the current study’s findings, ongoing educational activities should emphasize the importance of improving the public’s judicious use of ABs, which may help curb the spread of ABR. Educational campaigns to improve health literacy regarding dispensing, purchasing, prescribing, and using ABs are recommended particularly for the target groups.
An in-silico approach for the identification of natural compounds as potential BACE1 inhibitors for the treatment of Alzheimer disease
(Open Science Publishers LLP, 2024-09) Lodha, T; Birangal, S; Pai, A; Prabhu, S; Nayak, S; Francis, T; Kumar, L; Verma, R
BACE-1 is a transmembrane protein occurring in the endoplasmic reticulum that is responsible for generation of beta amyloid (A?) by cleavage of amyloid precursor protein (APP). Deposition and aggregation of A? in the brain results in the onset of Alzheimer’s disease (AD). The process of drug discovery in this area is sluggish and most of the developed molecules fail due to toxicity. Research related to phytochemicals has taken pace in drug discovery process due to associated low toxicity comparatively. The development of low toxicity BACE-1 inhibitors has proven to be a promising treatment strategy for AD. In the current study, in-silico drug repurposing techniques were employed to identify small natural molecules from the ZINC database as potential BACE-1 inhibitors. Molecular docking studies (both rigid and flexible) were conducted via high-throughput virtual screening, standard-precision and extra precision mode and protein ligand interactions were observed. Top compounds were undertaken for molecular mechanics with generalized Born and surface area solvation (MMGBSA) calculations and absorption distribution metabolism elimination properties analysis. ZINC000014945921, ZINC000150351431, and ZINC000069488328 were selected as leads and these compounds with the co-crystallized ligand were subjected to molecular dynamic simulations. The final findings of this study suggested that ZINC000150351431 and ZINC000069488328 can be considered as potential leads in the development of drugs for therapeutic use for AD.
Oleuropein ameliorates hyperlipidemia, oxidative stress, inflammatory and liver dysfunction biomarkers, in streptozotocin-induced diabetic rats
(Open Science Publishers LLP, 2024-09) Mohamed, NA; Hussein, MM; Ahmed, OM; Al-Jameel, SS; Al-Muzafar, HM; Amin, KA; Abdou, HM
Diabetes mellitus (DM) is a serious threat factor for chronic liver disorders and the development of nonalcoholic steatohepatitis into cirrhosis. However, numerous pharmacological actions of olive polyphenol have been discovered, with oleuropein being a primary phenolic substance found in olive leaves, olive oil, and olive fruit (Olea europaea). Our goal is to identify the impacts of oleuropein on lipid measurements, oxidative stress, serum leptin, adiponectin levels, inflammatory status, and hepatic dysfunctions in a male rat model with streptozotocin (STZ)-induced DM. Oleuropein was orally administered to diabetic rats at a 5 mg/kg bw/day dose for 15 days. Diabetic rats treated with oleuropein demonstrated improved hepatic function test results (ALT, AST, alkaline phosphatase, and bilirubin), while activity of the low liver glucose-6-phosphate dehydrogenase (G6PDH) increased. Moreover, serum triacylglycerol, very low-density lipoprotein, low-density lipoprotein, and total cholesterol (TC) were considerably reduced, while high-density lipoprotein increased markedly. In addition, serum antioxidative enzymes such as glutathione peroxidase, catalase, glutathione-S-transferase, and superoxide dismutase increased, as well as glutathione levels. Lipid peroxidation levels were lower than those in the STZ control group. Treating diabetic rats with oleuropein not only resulted in decreased serum leptin and increased adiponectin levels but also had a substantial inhibitory effect on the elevated COX-2 and TNF-? mRNA expression levels in the livers of the STZ group. In conclusion, oleuropein has shown promising results in mitigating hyperlipidemia, oxidative stress, inflammation, and hepatic dysfunction biomarkers in diabetic rats.
Network pharmacology approach to investigate the molecular mechanism of DLBS2411 (Cinnamomum burmannii) as a gastritis treatment
(Open Science Publishers LLP, 2024-09) Rustan, J; Yulandi, A; Tjandrawinata, RR
DLBS2411, a bioactive fraction of Cinnamomum burmannii, has been proven to exhibit its anti-ulcer properties through preclinical and clinical studies. However, the bioactive compounds, protein targets, and underlying molecular pathways are still poorly known. Therefore, network pharmacology was used in this study to understand the molecular mechanisms of DLBS2411 in treating gastritis. There were three stages in this investigation. First, the DLBS2411 compounds and targeted proteins associated with DLBS2411 and gastritis were gathered and examined. The subsequent stage involved constructing and analyzing the protein–protein interaction network. Then, molecular docking was employed to confirm the interaction between substances and proteins. This study found that most DLBS2411 compounds, including p-cymene, copaene, and cinnamaldehyde, were apparent in their effects on gastritis. These substances impacted several important target proteins, including PTGS1, PTGS2, 15-hydroxyprostaglandin dehydrogenase, NOS2, and ATPase H+/K+ transporting subunit alpha, which were associated with the mucosal protector and proton-pump inhibitor modes of action, consistent with earlier in vitro and in vivo studies. In addition, the molecular docking study revealed that the ligand-receptor binding activity had a good vina score, indicating stable ligand-protein complexes. Thus, it can be concluded that the proton pump inhibitor and mucosal protector were the key molecular pathways utilized by DLBS2411 to treat gastritis.
Pharmacoeconomic research of medicines used for allergic rhinitis in children
(Open Science Publishers LLP, 2024-09) Suyunov, N; Umurzakhova, G; Blatov, R; Yegizbayeva, S; Abdullaeva, M; Zhakipbekov, K
Allergic rhinitis (AR) is a common global disease, affecting approximately 2%–25% of children and 1%–40% of adults. Recent studies have shown an increasing prevalence, especially in low-income countries. Although not fatal, AR significantly impairs patients’ quality of life and is linked to bronchial asthma (BA) development. This research aimed to study the regional distribution of AR in children, analyze various medicine preparations used for treatment, and identify effective and affordable options through pharmaco-economic methods. Data from the Ministry of Healthcare of the Republic of Uzbekistan, Hospital No. 2 of the Tashkent Medical Academy, and wholesale medicine costs were analyzed. The study demonstrated the effectiveness and cost efficiency of budesonide medicines for treating AR in children with BA, resulting in significant cost savings during the first treatment session.
Purification and characterization of a novel zinc chelating peptides from Holothuria scabra and its ex vivo absorption activity in the small intestine
(Open Science Publishers LLP, 2024-09) Syahputra, G; Sandhiutami, NMD; Hariyatun, H; Hapsari, Y; Gustini, N; Sari, M; Siwi, OGR; Putra, MY; Fadilah, F; Louisa, M.
Zinc supplements currently marketed in Indonesia are second-generation zinc supplements, which must be improved for the effectiveness caused by their low absorption rate and side effects on the gastrointestinal tract. Third- generation zinc supplements are currently being investigated to improve the effectiveness of the previous generation of supplements. The present study aimed to discover a new alternative source of zinc-chelating peptide (ZCP) from Holothuria scabra. In addition, the research investigates the ZCP characteristics and absorption abilities in an ex vivo evaluation using the everted gut sac model method. The results obtained were six zinc peptides: Asp-Asp-Ala- Phe-Gln-Ala-Phe-Cys; Thr-Asp-Asn-Leu; Leu-Gly-Cys; Pro-Gly-Thr; Ser-Cys; and Pro-Tyr. The characterization showed that the resulting peptides comprised two to eight amino acids with molecular weights between 208 and 915 Da. The highest zinc binding capacity of the peptides was 92.11 mg/100 g at 30 kDa for molecular weight. Fourier- transform infrared spectra indicate that zinc ions (Zn 2+ ) bind to carboxyl groups and interact with nitrogen atoms in amino acids and amides. The scanning electron microscope-energy dispersion spectroscopy results stated that, topographically and morphologically, ZCP has a different surface with peptides with Zn composition in the sample. Furthermore, we evaluated the peptide fractions for ex vivo absorption in the small intestine using the everted gut sac method. We found that zinc-binding peptides transported and enhanced zinc absorption in the duodenum segment at 60 minutes, resulting in a 40% increase in absorption rate. The potency of ZCPs from H. scabra as an alternative to third-generation zinc supplements with higher absorption than previous-generation supplements.
The combination of fraction A3 of Cyrtostachys renda Blume with doxorubicin improved cytotoxicity against T47D cell line through cell cycle arrest and apoptotic induction
(Open Science Publishers LLP, 2024-09) Syamsurizal, S; Utami, DT.
Currently, natural products of herb medicinal plants are widely reported as a supplement to cancer chemotherapy. The cytotoxic effect of a dichloromethane (DCM) extract of Cyrtostachys renda root and its flow cytometric profile against a human breast cancer cell line (T47D) were investigated in this study. The 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromid assay was used to assess the combined cytotoxic effects of fraction A3 C. renda root and doxorubicin. The combination index (CI) criteria was used to analyze the synergistic effect of fraction A3 and doxorubicin. The cell cycle and apoptosis profiles were completed using flow cytometric labeling with propidium iodide/RNase and Annexin V. Cell morphological changes were observed using an inverted microscope. Single cytotoxicity fraction A3 of DCM extract was effective against T47D cells with an IC 50 value of 43.03 ?g/ml. Fraction A3 and doxorubicin at half of IC 50 combined had a strong synergistic effect on T47D cells with a CI of 0.2. The cell cycle analysis results showed that this combination caused cell cycle arrest in the G1 and S phases. This observation is consistent with the results of single fraction A3 and doxorubicin treatments, which resulted in cell cycle arrests in the G1 and S phases, respectively. The result of single fraction A3 treatment, combined with doxorubicin for 24 hours, can also induce apoptosis against T47D cells. When the control and treatment groups were compared, the test cell shape altered.
Ethnomedical uses of Cananga odorata (Lam.) Hook. f. and Thomson in indigenous traditional medicine among Indonesia ethnic groups
(Open Science Publishers LLP, 2024-09) Nuning, Rahmawati; Ika, Yanti M Sholikhah; Rohmat, Mujahid; Yuli, Widiyastuti; Agung, Endro Nugroho; Abdul, Rohman
Cananga odorata, commonly known as ylang-ylang, is an evergreen perennial tropical tree belonging to the Annonaceae family, which is traditionally and scientifically reported to have various pharmacological activities. This indigenous medicine study was carried out to document the traditional usage of C. odorata for medicinal reasons by Indonesian ethnic groups. This is one of numerous initiatives aimed at preserving indigenous knowledge and medical practices maintained by the community. Data were acquired during 2015 and 2017 through in-depth interviews with selected traditional healers from each ethnic group throughout 34 Indonesian provinces, who were chosen using a purposive sampling approach based on inclusion criteria. The information gathered includes the demographic data of healers, medicinal plants used, potions, and their applications for health purposes. Following the completion of the interview with the informant, specimens of medicinal plants were collected. Data quantification was accomplished by examining the value of plant parts and doing a simple ranking analysis for multihealth purposes. This study revealed 42 traditional applications of C. odorata by 36 traditional healers from 28 ethnic groups in 16 provinces to overcome 18 diseases. Cananga odorata was primarily obtained from the woodland instead of the house garden and other environments. Skin disease was identified as the most prevalent indication of C. odorata, in agreement with the most commonly employed administration method, the external route. Leaves became the foremost prominent plant part utilized by healers. This study emphasized the significant role of traditional healers in healing various illnesses with C. odorata and the variations in C. odorata ethnomedical usage as a traditional remedy in Indonesia. Nonetheless, cultivating initiatives should be started as more than 60% of identified C. odorata has yet to be grown. The study’s findings are likely to benefit various stakeholders, serve as baseline data for further studies on the efficacy and safety of C. odorata, and contribute to efforts for developing health products that employ C. odorata.
An evaluation of Sargassum cinctum anticancer properties utilizing in vitro testing and molecular docking, with assistance from GC-HRMS and FTIR
(Open Science Publishers LLP, 2024-09) Salunke, M; Mane, P; Kumbhar, S; Balaji, Wakure B
Cancer is characterised by unregulated, uncontrollable cell development, which is a continuous abnormality in cellular behavior. This frequently results in the aggressive invasion, metastasis, and dispersal of malignant cells throughout different organs. Breast cancer is one of the most common types of cancer that is prevalent worldwide. In particular, it comes in second place after lung cancer in terms of cancer-related mortality among women. The current work concentrated on identifying bioactive components in ethanolic extracts of Sargassum cinctum by gas chromatography high-resolution mass spectroscopy (GC-HRMS) and Fourier-transformed infrared (FTIR) analysis. Following GC-HRMS and FT-IR studies, anticancer activity and molecular docking are carried out on the ethanolic extract of S. cinctum. Different bioactive compounds, including phenols, alcohols, amines, aldehydes, ketone esters, carboxylic acids, alkenes, and alkanes, are detected by the GC-HRMS and FT-IR analyses. Sargassum cinctum ethanolic extract exhibits strong anti-cancer properties. The IC50 value of the MCF 7 cell line and A549 cell line is 134.50 and 161.02 µg/ml, respectively. Asn923, Phe1047, Lys868, and Asp1046 from vascular endothelial growth factor receptor (VEGFR) and Met623, Asp690, and Lys567 from anexelekto (AXL) kinase are among the residues that may have contributed to the anti-cancer benefit observed in this study. Using in-silico approach, it was determined that the medications that target the VEGFR2 and AXL kinase receptors had anticancer properties. This is the first-hand evaluation of the bioactive elements of S. cinctum extracts that have anticancer potential, as far as we aware. Recent study proved value of in silico analyses in the search for new drugs and the capacity of marine compounds to produce distinctive bioactives with considerable biological activity.
Endophytic fungi from medicinal plant Garcinia cowa Roxb. ex Choisy and their antibacterial activity
(Open Science Publishers LLP, 2024-09) Handayani, D; Muslim, RI; Syafni, N; Artasasta, MA; Riga, R
Endophytic fungi grow inside plant tissues and produce biologically active substances without harming the host plant. Endophytic fungi isolated from the roots, barks, and leaves of Garcinia cowa Roxb. ex Choisy, an ethnomedicinal plant commonly used in West Sumatera, Indonesia, are the focus of this research, which aims to evaluate their antibacterial activity. Traditional medicine has made extensive use of this plant’s various parts. In total, 14 endophytic fungal isolates were obtained from plant fragments of G. cowa that had undergone surface sterilization. After four to six weeks of cultivation in rice medium, the fungus isolate was extracted with ethyl acetate (EtOAc). Each EtOAc extract of fungus was tested for antimicrobial activity using Kirby–Bauer diffusion against Staphylococcus aureus, Escherichia coli, Methicillin Resistant S. aureus, and Candida albicans. The measurement results of the inhibition zone indicate that the GCA3 isolate of endophytic fungi exhibited significant inhibitory diameters and demonstrated potential as an antibacterial agent. The GCA3 strain showed an inhibition diameter zone of 15.05 ± 0.51 mm against S. aureus, 14.68 ± 0.5 mm against E. coli, and 13.48 ± 0.15 mm against MRSA. None of the fungi extracts can inhibit the growth of C. albicans. The fungus GCA3 has been determined to be identical to Penicillium citrinum through macroscopic, microscopic, and molecular identification methods. The findings indicate that endophytic fungi from the Garcinia plant can generate antibacterial compounds. Hence, additional investigation is required to separate these bioactive compounds.
Safety profile assessment of standardized root extract of Potentilla fulgens in Wistar rats: Acute and sub-acute dermal toxicity study
(Open Science Publishers LLP, 2024-09) Kumar, S; Nikam, YP; Baruah, S; Kushari, S; Ghose, S; Prasad, SK; Das, A; Banu, ZW; Kalita, J; Laloo, D
Potentilla fulgens Wall (Rosaceae), a well-known medicinal plant native to Asian regions has a rich history of traditional use for treating skin, gastrointestinal tract, and various metabolic disorders. Research has addressed that the plant is applied topically to treat conditions such as wounds, ulcers, and other skin ailments. Surprisingly, no prior investigation has explored the dermal toxicity of this plant. Therefore, the study was set to conduct the acute and subacute toxicity assessments on the ethyl acetate (EAPF) and methanol (MEPF) extracts of P. fulgenson Wistar rats. In the acute dermal toxicity study, rats received a single dose and were monitored for 14 days, while in the sub-acute study; they received a daily dose for 28 days. 2,000 and 5,000 mg/kg were tested by applying them to the shaved dorsal skin. Throughout the experiments, changes in physical appearance, behavior, and histological alterations were monitored. The results unequivocally revealed no abnormal physical or physiological changes, behavioral deviations, or mortality in any of the rats in both acute and sub-acute dermal toxicity assessments. Furthermore, there were no statistically significant differences (nsp > 0.05) in body weight, kidney, liver, spleen weights, hematological parameters, or blood biochemistry values between the treatment and control groups. These findings were further substantiated by the normal macroscopic and microscopic characteristics of the rats’ skin, kidneys, liver, and spleen. In conclusion, our study affirms that the application of EAPF and MEPF to the skin does not induce acute or subacute skin irritation nor elicit systemic toxic responses in rats.
Contriving a novel multi-epitope subunit vaccine from Plasmodium falciparum vaccine candidates against malaria
(Open Science Publishers LLP, 2024-09) Mamudu, CO; Iheagwam, FN; Okafor, EO; Dokunmu, TM; Ogunlana, OO
In this study, immunoinformatics strategies were used to design a subunit vaccine against malaria from immunogenic regions of three Plasmodium falciparum surface antigens; liver stage antigen 3-C (V750-K1433), merozoite surface antigen 180 truncate-4 (A805-P1093), and merozoite surface protein 10 region 1 (D29-N188). A multi-epitope subunit vaccine construct (VC) was designed from immunodominant B- and T-cell epitopes followed by structure prediction, evaluation, and validation. Toll-like receptors (TLRs) 2 and 4 were docked with the VC. Their complexes’ molecular dynamics, immune stimulation, codon optimization, and in silico cloning of the VC were simulated. The VC is a 49.2 kDa antigenic and nonallergenic protein, comprised of 26% ?-helix, 7% ?-strand, 66% coil. The immune simulation test showed that the vaccine could provoke adaptive immune responses, and molecular docking tests showed that it interacts strongly with TLR-2 (?945.1 kcal/mol) and TLR-4 (?919.8 kcal/mol) to form complexes of high stability that hardly deform. The guanine-cytosine content and codon adaptation index of the VC were 42.94 and 0.99 after codon optimization. Escherichia coli pET-28a(+) was identified as the best vector for optimal gene expression. In conclusion, the study reveals that the VC shows promising results in neutralizing falciparum malaria.
Development of an LC-MS/MS technique and its validation for the determination of infigratinib in human K2EDTA plasma; Pharmacokinetics in healthy rabbits
(Open Science Publishers LLP, 2024-09) Anusha, K; Sowjanya, G
A precise and linear liquid chromatography tandem mass spectrometry technique was developed for the estimation of infigratinib in human K2EDTA plasma. Chromatographic isolation of infigratinib and dasatinib was attained on orosil, 3 µm, C18, 150 × 4.6 mm stationary phase with a 0.8 ml/minute movable phase flow rate. The method was rectilinear in a concentration range of 1–1,640 ng/ml. Validation showed an r2 = 0.9997 and an equation of y = 0.0015x ? 0.0063. The average accuracies of back-assessed concentrations for all quality controls (QCs) were between 96.34 and 100.76. At medium QC, high-QC, and low-QC concentrations, infigratinib had 98.14%, 96.36%, and 97.21% mean recoveries, respectively. Retention time %CV findings were ?0.62 for the analyte and dasatinib, respectively. The developed method was successfully applied to the pharmacokinetic studies of infigratinib in healthy rabbits. The Cmax, Tmax, andT1/2, of the infigratinib tablets were 87.25 ± 1.43 ng/ml, 6.0 ± 0.03 hours, and 15.24 ± 0.53 hours, respectively. AUC0–? infinity for infigratinib tablets was 291.74 ± 3.67 ng h/ml. The developed method was successfully validated and can be utilized for the assessment of infigratinib in biological matrices at industries, forensic laboratories, QC laboratories, and bioavailability studies.
New bisnorsesquiterpene from Glottiphyllum linguiforme and its antimicrobial, cytotoxic, and antioxidant activities
(Open Science Publishers LLP, 2024-06) Ahmed, HS; Amir, DE; Muhaisen, HMH; Sebak, M; Abdelghany, TM; Elmaidomy, AH; Amin, E; Owis, AI; Orabi, MAA; Afifi, N.
Natural product research is a cornerstone in the drug discovery process. Many inspiring chemical moieties with new skeletons and potent biological activity are commonly reported from natural sources. Chromatographic examination of the alcoholic extract of Glottiphyllum linguiforme aerial furnished four compounds, including ?-sitosterol (1), ?-sitosterol-3-O-?-D-glucopyranoside (2), and 1,1? biuracil (3), and a new compound, tectoionyl A 3-O-sodium sulfate (4). The new structure was elucidated using high-resolution mass and intensive 1D and 2D NMR spectroscopic analyses. Quantitative analysis of G. linguiforme extract revealed considerable contents of total phenolic and total flavonoid. A DPPH antioxidant assay indicated moderate activity (0.026 mg acid equivalent antioxidant capacity/g dry extract). Antimicrobial activity testing of the pure compounds indicated noticeable antibacterial activity of compound 2 against Escherichia coli, Salmonella enterica, and Pseudomonas aeruginosa. In addition, compounds 1–4 displayed mild cytotoxic effects against human breast adenocarcinoma (MCF7) and hepatocellular carcinoma (HepG2) cell lines, and the normal (Vero) cells at the tested concentration (100 ?g/ml), as compared to the standard cytotoxic drug, doxorubicin. This study is the first to estimate phenolics and flavonoid contents, discover constituents by phytochemical isolation, and examine cytotoxicity and antimicrobial properties of G. linguiforme. The unusual nitrogenous compound 1,1?-biuracil (3) and the sulfate derivative (4) may evidence chemotaxonomic importance.
Citric acid-glycerol-based NADES for microwave-assisted extraction enhances the polyphenols level of Eleutherine bulbosa mill. Urb. Bulbs
(Open Science Publishers LLP, 2024-09) Ahmad, I; Shakti, SOP; Prabowo, WC; Hikmawan, BD; Arifuddin, M; Angelina, M; Prastya, ME; Okselni, T; Alwi, RS; Sadikin, R; Iswahyudi, I; Febrina, L; Herman, H; Junaidin, J; Faisal, M; Samsul, E; Ibrahim, A; Mun’im, A
Natural deep eutectic solvent combined with Microwave-assisted extraction (MAE) is considered as a potential green substitute for conventional extraction methods because of its selectivity and shorter extraction time. Eleutherine bulbosa Mill Urb. (E. bulbosa) bulbs, is renowned for having a high concentration of bioactive substances, primarily phenolics compounds with various therapeutic characteristics. This study aims to increase the level of total phenolics content (TPC) in E. bulbosa bulbs extract by applying a citric acid-glycerol (CA-Gly)-MAE and to optimize its extraction conditions using response surface methodology-based box-behnken design. In this study, we extracted dried samples under various conditions including microwave irradiation time and power, solid–liquid, sample-solvent ratio, and CA-Gly ratio. The measurements of TPC value were done spectrophotometrically and gallic acid was used as standard reference. The recommended optimum conditions were at 50% microwave power for 15 minutes, ratio of 1:14 g/ml, and CA-Gly ratio of 1:1 g/g, resulting in a predicted TPC value of 74.749 ± 3.716 mg GAE/g DW extract. Confirmation experiments were conducted using the recommended optimal extraction parameters, and the obtained TPC value was 84.653 ± 0.918 mg GAE/g DW extract. Our result demonstrates the potential of the CA-Gly-MAE for obtaining a higher yield of polyphenols from E. bulbosa bulbs.

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