Journal of Advanced Pharmaceutical Technology & Research最新文献

Triple-negative breast cancer (TNBC) is one of the most common types of serious breast cancer. Due to the absence of therapeutic hormone receptors, TNBC treatment generally involves chemotherapy which results in various side effects and resistance development. Herbal compounds, including α-mangostin, have shown potential anticancer effects against TNBC. However, rigorous screening is needed to uncover its mechanisms and characteristics. The aim of this study was to understand the molecular mechanism of α-mangostin against TNBC and its possible limitations. The study design used is an in si lico study. The study involved database mining and compound characteristic analysis. Network pharmacology and molecular docking were also done to explore potential target and molecular mechanisms against TNBC. There was no statistical analysis conducted as this study relies on predefined algorithms and simulation models. Instead, a parameter threshold was used for each analysis to ensure its reliability. Prediction of Activity Spectra for Substances prediction and Gene Ontology-Kyoto Encyclopedia of Genes and Genomes enrichment predicted potential anticancer effects of α-mangostin through the regulation of enzyme activity and apoptotic pathway. Compound property predictions showed α-mangostin to have promising drug-likeness with sufficient bioavailability and low biodegradability. However, α-mangostin still has some potential limitations in water solubility and toxicity risks. Through network pharmacology, 75 potential target proteins of α-mangostin in TNBC cases were found. The top three most significant of which (AKT1, CTNNB1, and HSPAA91) were proven to bind with α-mangostin through molecular docking. Study results suggested α-mangostin to have a promising anticancer and chemopreventive activity with great drug-likeness and pharmacokinetic properties. It was revealed that α-mangostin can bind to key components in TNBC-related pathways, including AKT1, CTNNB1, and HSP90AA1 proteins. However, further experimental studies may be needed to verify its effectiveness as well as possible solubility and toxicity limitations.

Under a hidden waterfall in the interior of the tropical rainforest of East Kalimantan, a new medicinal plant that produces essential oil (EO) was found with the name Strobilanthes kalimantanensis. The aim was to investigate the botanical and evaluate the pharmacognostic characteristics of S. kalimantanensis leaves from East Kalimantan, Indonesia. Pharmacognostic studies can provide recommendations for establishing quality control standards or guidelines for cultivating, harvesting, and processing S. kalimantanensi s to ensure the consistent and reliable quality of medicinal products. Characteristic methods of S. kalimantanensis leaves include botanical macroscopic, fluorescence, physicochemical, and phytochemical evaluation. The plant characteristics of this plant are similar to S. kunthia and S. reptans but can be differentiated in the leaves and flowers. Fluorescence assay with sodium hydroxide 5% shows unique characteristics of secondary metabolites based on their ability to form dark green with black precipitate in Ultraviolet 365 nm. The physicochemical characteristics showed yield, water content, water-soluble, ethanol soluble, total ash value, and acid-insoluble ash. Phytochemicals showed the presence of alkaloids, polyphenols, terpenoids, and EO containing 23% trans-anethole. This evaluation report details the chemical composition, identity, and safety of S. kalimantanensis leaves.

Lime (Citrus aurantifolia) juice was reported to contain ascorbic acid (AA) and flavonoids, which has bioactivity as antioxidants. To develop an antioxidant product, improving its stability is necessary due to the perishable characteristics of compounds in lime. Therefore, the formulation of polyelectrolyte microparticles using chitosan and alginate was conducted to overcome the weaknesses. This study aims to evaluate the effect of various chitosan, alginate, and lime juice powder (LJP) concentrations on the physical characteristics and antioxidant activity of LJP encapsulated in chitosan-alginate microparticles (CALM). Microparticles with various concentrations of chitosan and alginate were prepared by ionic gelation method using CaCl₂ as a crosslinker. The microparticles were evaluated for its physical properties and its antioxidant activity using 2-2-diphenyl-1-picrylhydrazyl reagent. A one-way ANOVA test and Tukey's honest significant difference post hoc were used to determine the effect of LJP amount on the antioxidant activity. The highest AA content in CALM was 0.14 mg/100 mg, with a % encapsulation efficiency of 18.38% ± 0.02%. Antioxidant activity tests revealed that LJP possessed the strong antioxidant activity with an IC₅₀ value of 32.59 μg/mL, whereas IC₅₀ values of the microparticles ranged from 24.79 ± 0.03 μg/mL to 39.96 ± 0.07 μg/mL. During storage, the IC₅₀ of LJP decreased from 32.59 ± 0.13 μg/mL to 65.53 ± 0.03 μg/mL, whereas the IC₅₀ of microparticles remained stable. This study concluded that the chitosan-alginate polyelectrolyte microparticle formulation can improve and protect LJP's antioxidant activity.

A topical antimicrobial ointment was developed from the fruit extract of Oroxylum indicum and was evaluated for its antibacterial and wound-healing effects and acute toxicity in animal models. O. indicum fruit and seed extracts exhibited antibacterial activities against clinically isolated bacteria and showed in vitro antioxidant activities. To develop a topical antimicrobial ointment from the fruit extract of O. indicum and evaluate for its antibacterial and wound-healing effects. O. indicum fruit extract ointment was prepared and qualitatively controlled. Acute toxicity of the extract was evaluated in the animal model. Antibacterial effects and healing effects of the ointment to the dog wound were investigated. The results are expressed as mean ± standard deviation. The ointment exhibited in vitro antibacterial effects. A single daily application of the ointment to a dog's wound exhibited a wound-healing effect with complete epithelialization within 7 days while the wound was completely healed with the removal of the scabs, the size was decreased to 14% of the original size within 12 days. The ointment was found no acute toxicity in the animal model. O. indicum ointment promoted in vitro antibacterial activity and wound-healing effect in dogs with no acute toxicity.

Benign prostatic hyperplasia (BPH) is a chronic disorder that inflicts severe symptoms on middle-aged men. The current study compared the effects of tadalafil and tamsulosin on urological parameters after 3 and 6 months of therapy. A retrospective case-control study was conducted, in which 100 patients with moderately severe BPH were divided into two groups based on their treatment: 50 patients were given tamsulosin 0.4 mg/day and group 50 patients were administered tadalafil 5 mg daily. All patients continued therapy for approximately 6 months, and their urological parameters were assessed at baseline and after 3 and 6 months. There was no significant difference in the overall effect on the International Prostate Symptom Score at the end of the study using two-way ANOVA analysis (P = 0.448). The intercourse number was significantly improved by tadalafil compared to tamsulosin (P < 0.001). The prostatic-specific antigen, postvoiding residual, and prostatic volumes were not significantly different between tadalafil and tamsulosin (P = 0.198, 0.163, and 0.183, respectively). In conclusion, tadalafil, 5 mg once daily, appears to have similar efficacy to tamsulosin, with significant improvement in the patient's erectile function. Tadalafil can be used for 6 months for moderate-to-severe lower urinary tract symptoms.

Hesperidin is a citrus bioflavonoid and has numerous pharmacological actions. Hesperidin's effect on testicular dysfunction has not been well researched. Hence, the present study is aims to investigate the effect of hesperidin on aluminium chloride (AlCl₃)-induced testicular dysfunction in rats. Both vitamin C (200 mg/kg) and hesperidin (50, 100, and 200 mg/kg) were administered orally for 21 days. At the end of the study, the blood samples were obtained from all animals for investigation of biochemical and hematological parameters. Then, bilateral orchiectomy was carried out to remove testicles from the animals, and sperm was collected and examined under a microscope. Finally, organs such as the liver, kidney, and testicles were also collected and utilized for histopathological analysis. Part of the liver sample was used for determination of antioxidant enzymes such as reduced glutathione (GSH) and catalase (CAT) levels. The rats administered with AlCl₃ showed elevated levels of biochemical and hematological parameters and a reduction in levels of sperm count, sperm motility, and oxidative stress parameters, whereas the rats administered with vitamin C/hesperidin (200 and 400 mg/kg) were able to ameliorate AlCl₃-induced testicular dysfunction by attenuating AlCl₃-induced changes in biochemical and hematological parameters, sperm motility, sperm count, and oxidative stress. Both vitamin C and hesperidin had significant ameliorative effects against AlCl₃-induced testicular dysfunction.

Antioxidants are compounds that can inhibit excessive free radical reactions in the body. Excessive free radicals can cause system imbalances in the body which can trigger oxidative stress and cause serious illness. The limitations of antioxidants in the body can be overcome by consuming safe natural additional antioxidants that can be obtained from natural products. Isolating compounds of Allium ascalonicum leaves as antioxidant and antiradical agents in inhibiting excessive free radicals by in vitro and in silico. The extracted compounds were purified by column chromatography. The compounds obtained were then characterized using ultraviolet, infrared, NMR, and mass spectrometry. Determination of antioxidant activity was carried out by in vitro using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the non-enzymatic superoxide dismutase (SOD) methods. The in silico study used the density functional theory (DFT) calculation method with global descriptive parameters (GDP), donor acceptor map (DAM), and frontier molecular orbitals (FMO) analysis. Three compounds have been isolated, of which compound 1 is a new compound. In the DPPH method, compound 1 has more strong antioxidant activity than others, as well as in the non-enzymatic SOD method. Whereas, in the DFT calculation shows that compound 1 has the best reactivity and stability between other compounds and was categorized as the best antiradical. Compound 1 has the highest antioxidant activity compared to the other compounds by in vitro both the DPPH and non-enzymatic SOD methods. In silico, compound 1 has the potential as the best antiradical.

Indonesia is the second country with the highest number of tuberculosis (TB) cases in the world and the first in Southeast Asia, according to WHO Global Report 2020. Quercetin has been tried as an alternative therapy and was found effective. This study aims to optimize quercetin pulmospheres using combination polymers and study its characteristics as an inhalation delivery system. Combination polymers provide the advantages of safe, mucoadhesive, and compact pulmospheres. Pulmospheres were made as formula F1, F2, and F3 (polymer ratios of 1:1, 1:2, and 1:3), respectively. Pulmospheres were made with quercetin 0.2%, alginate-carrageenan (total concentration of 1.8%), and CaCl₂ 0.5 M. Characterization of particle size, morphology, moisture content (MC), yield, drug loading, and entrapment efficiency (EE) were conducted. The yield range was from 83.89 to 86.30% ± 4.59%. MC range was from 4.23 to 5.12% ± 0.05%. Particle size was <3 µm (between 2.19 and 2.76 ± 0.149 µm), spherical shape and smooth surface. EE range was 60.69% ± 4.45% to 77.86% ± 1.74% and the drug loading range was 1.66-2.09% ± 0.15%. F2 formula with a polymer ratio of 1:2 was the best quercetin pulmospheres. Potential pulmospheres will then be recommended for in vitro release and in vivo study.

Rosemary leaf extract, a well-known medicinal plant, can induce neurotrophin gene expression and proliferation in stem cells. Human adipose-derived stem cells (hASCs) with high proliferation and differentiation capacity are easily accessible and can be extracted with the least damage. This study evaluated the effect of rosemary extract (RE) on neurotrophin gene expression at 48 h postinduction in hASCs. hASCs were isolated from healthy female donors, aged 28-35 years, who had undergone abdominal liposuction. Passage-4 stem cells were cultured and treated with different doses of RE (from 30 to 70 µg/ml) containing 40% carnosic acid for 48 h. Reverse transcription-polymerase chain reaction was used to check the expression of neurotrophin genes. The expression of NTF3, NTF4, and nerve growth factor genes in cells treated with 40-60 µg/ml and the expression of GDNF in cells treated with 50-70 µg/ml of RE for 48 h showed a significant increase compared to cells cultured in serum-containing medium. However, different doses of RE showed no effect on brain-derived neurotrophic factor gene expression in the treated cells. RE (50, 60 µg/ml) leads to an increase of neurotrophin gene expression in hASCs as compared to routine cell culture. Hence, this protocol can be used to prepare ideal cell sources for cell therapy.

Candida species are the primary cause of candidiasis, a common yeast infection, with Candida albicans being the most prevalent pathogen. These infections often infiltrate the body through cutaneous and vaginal routes. Given the potential severity of some Candida infections, particularly invasive cases, there is a critical need for effective antifungal treatments. Controlled drug delivery strategies have been developed to achieve optimal release kinetics and precise targeting of active agents, especially in fungal infection therapeutics. Consequently, significant attention has been focused on exploring and utilizing bioadhesive polymers to enhance the performance of drug delivery systems for antifungal medications. Bioadhesive drug delivery systems aim to sustain the release of therapeutic agents, reducing the need for frequent dosing. This article provides a comprehensive review of scientific investigations into the use of antifungal drugs within bioadhesive drug delivery systems for treating candidiasis, locally and systemically. The evaluation covers the efficacy of these systems against candidiasis, factors affecting prolonged contact at the application site, and the underlying mechanisms of drug delivery.