Pharmaceutical Components Research Articles

EFFECT OF CAFFEINATED AND DECAFFEINATED COFFEE ON BLOOD PRESSURE

The world's most popular stimulant, caffeine, accounts for 80% of all caffeine consumption. It is widely used as a component in pharmaceuticals due to its high antioxidant and nutrient content, including phenol and polyphenol. On the presence of caffeine drinks are categorised as caffeinated and decaffeinated. The present study was conducted to evaluate the effect of caffeinated and decaffeinated coffee on blood pressure among the young generation. This experimental study was conducted on 85 healthy individuals (both male and female, non hypertensive) between 18-28 years of age. Blood Pressure (BP) was measured by an automatic digital blood pressure monitor, before and after taking of coffee in 30, 60, and 90 minutes. Each participant ingested 100 mL of coffee prepared from 50 mg of caffeinated coffee in water. The consumption time of each individual was between 2- 4 minutes. It was noticed almost 65.7% participants were found normal while, a significant difference in 34.3% found in systolic blood pressure (SBP) and diastolic blood pressure (DBP) after the intake of caffeinated coffee at p-value (<0.001).An increase of4.4 mmHg and 5.02 mmHg was found in systolic blood pressure after 60, 90 minutes respectively from the normal that is <20mm Hg. While, a slight increase was noticed in DBP after taking caffeinated coffee. No significant difference were seen after the congestion of decaffeinated coffee among participants. It was concluded by the study that individual responses can vary. There was increase in BP after taking caffeinated coffee. There was no significant effect found after decaffeinated coffee. Some people might be more sensitive to caffeine and feel its effects more strongly, while others might not notice much difference. Additionally, any effects from this small amount of coffee are likely to wear off relatively quickly, within a few hours at most.

Integrative analysis of transcriptome and metabolome reveals the sesquiterpenoids and polyacetylenes biosynthesis regulation in Atractylodes lancea (Thunb.) DC.

Atractylodes lancea (Thunb.) is a perennial medicinal herb, with its dry rhizomes are rich in various sesquiterpenoids and polyacetylenes components (including atractylodin, atractylon and β-eudesmol). However, the contents of these compounds are various and germplasms specific, and the mechanisms of biosynthesis in A. lancea are still unknown. In this study, we identified the differentially expressed candidate genes and metabolites involved in the biosynthesis of sesquiterpenoids and polyacetylenes, and speculated the anabolic pathways of these pharmaceutical components by transcriptome and metabolomic analysis. In the sesquiterpenoids biosynthesis, a total of 28 differentially expressed genes (DEGs) and 6 differentially expressed metabolites (DEMs) were identified. The beta-Selinene is likely to play a role in the synthesis of atractylon and β-eudesmol. Additionally, the polyacetylenes biosynthesis showed the presence of 3 DEGs and 4 DEMs. Notably, some fatty acid desaturase (FAB2 and FAD2) significantly down-regulated in polyacetylenes biosynthesis. The gamma-Linolenic acid is likely involved in the biosynthesis of polyacetylenes and thus further synthesis of atractylodin. Overall, these studies have investigated the biosynthetic pathways of atractylodin, atractylon and β-eudesmol in A. lancea for the first time, and present potential new anchor points for further exploration of sesquiterpenoids and polyacetylenes compound biosynthesis pathways in A. lancea.

Divergent access to 5,6,7-perifused cycles

Nitrogen-containing heterocycles are the key components in many pharmaceuticals and functional materials. In this study, we report a transition metal-catalyzed high-order reaction sequence for synthesizing a structurally unique N-center 5,6,7-perifused cycle (NCPC). The key characteristics include the formation of a seven-membered ring by the 8π electrocyclization of various alkenes and aromatic heterocycles as π-components, in which metal carbene species are generated that further induce the cleavage of the α-C-H or -C-C bond. Specifically, the latter can react with various nucleophilic reagents containing -O, -S, -N, and -C. The stereo-controlled late-stage modification of some complicated pharmaceuticals indicates the versatility of this protocol.

A Simple UV Spectrophotometric Method Based on Continuous Wavelet Transform and Multivariate Calibration Model for the Concurrent Analysis of Three Water-Soluble Vitamins in Fertility Supplements.

Owing to the presence of overlapping spectra in pharmaceutical components, classical spectrophotometry is hard for concurrent determination. The advance of chemometrics along with UV-Vis spectrophotometry has contributed to solving this problem. In this study, a fast, easy, precise, accurate, low-cost, and eco-friendly spectrophotometric technique was introduced and validated for the simultaneous analysis of vitamin B6, vitamin B12, and vitamin C in fertility supplements for men and women using continuous wavelet transform (CWT) and partial least squares (PLS) techniques without using time-consuming extraction process and organic solvents. In the CWT method, the zero-crossing technique was applied to obtain the optimum points for plotting calibration curves for each component. The validation of both methods was evaluated by analyzing several mixtures with different concentrations. The efficiency of the proposed methods was also surveyed on commercial capsules. Wavelet families, including Symlet (sym2) at 230, Biorthogonal (bior1.3) at 378 nm, and Daubechies (db2) at 261, were considered for vitamins B6, B12, and C, respectively. The linear range was found to be 8-20, 8-20, and 10-25 μg/mL with the coefficient of determination (R2) equal to 0.9982, 0.9978, and 0.9701 for B6, B12, and C, respectively. Low limit of detection (LOD) (<0.09 μg/mL) and limit of quantification (LOQ) <0.9 μg/mL were achieved. The mean recovery values in synthetic mixtures were from 98.38 to 98.89% and from 99.83 to 99.99%, where root-mean-square error (RMSE) of not more than 0.4 and 0.05 using the CWT and PLS methods, respectively. The obtained results from the commercial capsules, applying the suggested techniques, were compared to those yielded by the high-performance liquid chromatography (HPLC) method using the analysis of variance (ANOVA) test. According to the results, there are no significant differences, and they were in good agreement. According to all the mentioned cases, the proposed approaches can replace the time-consuming and costly HPLC method in quality control laboratories. Green spectrophotometry coupling chemometrics methods were proposed. Simultaneous determination of three water-soluble vitamins in fertility supplements was done using these approaches. Rapidity, simplicity, low cost, and accuracy are the benefits of the proposed methods. A HPLC technique was used as a reference method to compare with the chemometrics methods.

Enantioselective Synthesis of 1-Aminoindanes via [3 + 2] Annulation of Aldimines with Alkenes by Scandium-Catalyzed C-H Activation.

Multisubstituted chiral 1-aminoindanes are important components in many pharmaceuticals and bioactive molecules. Therefore, the development of efficient and selective methods for the synthesis of chiral 1-aminoindanes is of great interest and importance. In principle, the asymmetric [3 + 2] annulation of aldimines with alkenes through C-H activation is the most atom-efficient and straightforward route for the construction of chiral 1-aminoindanes, but such a transformation has remained undeveloped to date probably due to the lack of suitable catalysts. Herein, we report for the first time the enantioselective [3 + 2] annulation of a wide range of aromatic aldimines and alkenes via ortho-C(sp2)-H activation by chiral half-sandwich scandium catalysts, which provides a straightforward route for the synthesis of multisubstituted chiral 1-aminoindanes. This protocol features 100% atom-efficiency, broad functional group compatibility, and high regio-, diastereo-, and enantioselectivity (up to >19:1 dr and 99:1 er). Remarkably, by fine-tuning the sterics of the chiral ligand around the catalyst metal center, the diastereodivergent asymmetric [3 + 2] annulation of aldimines and styrenes has been achieved with a high level of diastereo- and enantioselectivity, offering an efficient method for the synthesis of both the trans and cis diastereomers of a novel class of chiral 1-aminoindane derivatives containing two contiguous stereocenters from the same set of starting materials. Moreover, the asymmetric [3 + 2] annulation of aldimines with aliphatic α-olefins, norbornene, and 1,3-dienes has also been achieved.

Cost-effectiveness analysis of epidural morphine/ropivacaine treatment in patients with cancer pain.

Cancer pain is one of the main causes of human suffering, which can generate disabilities and compromise quality of life, giving rise to several psychosocial and economic consequences. This quantitative study sought to perform a cost-effectiveness pharmacoeconomic analysis to assess the impact of implanting epidural morphine associated with ropivacaine treatment in gastrointestinal cancer patients with pain that is difficult clinical control, compared with conventional oral treatment. The study population consisted of 24 patients with gastrointestinal neoplasia who underwent treatment for cancer pain that was difficult to clinically control. 12 patients each were recruited into the control and intervention groups, respectively. While patients in the control group were administered drug treatment orally, patients in the intervention group underwent a surgical procedure for subcutaneous implantation of a catheter that allowed epidural administration of morphine and ropivacaine. For pain assessment, the Visual Analogue Scale was applied. Data analysis had a descriptive character of costs, taking into account the costs for the year 2021. The study perspective was the Brazilian public healthcare provider, referred to as the Unified Health System (Sistema Único de-SUS in Portuguese). Costs were computed over the time horizon corresponding to the duration of treatment, from the first medical consultation (when the treatment was defined) to the end (end of treatment, disease progression, or death). Treatment duration was divided into three phases (first 60 days, support with palliative care, and end-of-life care). To assess the robustness of the economic analysis, sensitivity analyses were performed, considering the effectiveness of pain reduction on the Visual Analogue Scale, and a comparison of results using the median prices of pharmaceutical components used in the study. The mean age of patients was 59.3 years. The results from the cost-effectiveness analysis showed the epidural morphine/ropivacaine treatment to be more effective with regard to pain reduction on the pain scale, particularly for end-of-life care, when compared to the conventional oral treatment, however, at a significantly higher cost. From the accomplishment of this research, it was observed that the application of the pain assessment scale is a way to better interpret and understand the patient's pain, facilitating care planning and decision-making by health professionals, as well as monitoring the effectiveness of the proposed new treatment. To present a better cost-effectiveness ratio, a reduction in the cost of the new epidural technology or an increase in the value of the existing oral intervention would be required. However, the latter is not feasible and unlikely to occur. A value judgement to decide whether the incremental benefit associated with the use of the new intervention is worth the extra cost will have to be made by the healthcare provider. Interventions that can relieve cancer pain symptoms should be investigated continuously, in search of evidence to support clinical practice and promote better quality of life for patients.

Analysis of pharmaceutical supply of breast cancer patients

The aim: to conduct a clinical and economic analysis of the state of pharmaceutical support for patients with breast cancer in women. Materials and methods. During the research, data from the National List of Essential Medicines, the 14th State Formulary of Medicines, the Ukrainian clinical protocol, the clinical protocols of Great Britain and the United States of America for the treatment of breast cancer, and a depersonalized database of drug prescriptions were used. The research used such methods as clinical-economic, organizational-economic, mathematical-statistical, graphic, grouping and generalization. Research results. It was established that 46 schemes of schemes for the treatment of breast cancer are presented in Ukrainian and international clinical protocols (Great Britain, USA). In all three protocols, there were 5 regimens for the treatment of breast cancer, such as CMF (Cyclophosphamide, Methotrexat, Fluorouracil), AC (Doxorubicin, Cyclophosphamide), DC (Docetaxel, Cyclophosphamide), TC (Trastuzumab, Capecitabin), EC (Epirubicin, Cyclophosphamide). Analysis of the pharmaceutical component in the protocols for individual drugs showed that they included 23 drugs according to the INN, which belong to the group of antineoplastic drugs. The Ukrainian clinical protocol includes 17 drugs, the British protocol – 14 drugs, and the American one – 15 drugs. The frequency analysis of antineoplastic drugs included in the Ukrainian clinical protocol revealed the TOP-3 in terms of drug prescription frequency: L01A A01 Cyclophosphamide (Ki=0.037), L01C D02 Docetaxel (Ki=0.029), L01D B01 Doxorubicin (Ki=0.026). The largest number of prescribed drugs are vital drugs – 61.96 %, the smallest share – essential drugs – 2.17 %, and the share of non-essential drugs is 35.87 %. The ABC analysis made it possible to determine the group of the most expensive drugs in the treatment of breast cancer - these are antineoplastic and immunomodulating agents. The total expenses for this group amounted to UAH 772,459.96, which according to the US dollar exchange rate of the National Bank of Ukraine at the end of August 2022 was USD 21,122.77. According to the analysis of the matrix of the integrated ABC-VEN-frequency analysis, it was established that the largest number of prescriptions belonged to the group of less expensive and vital drugs (B/V) – 7 drugs (48.73 % of the total amount. At the same time, the largest amount of expenses is observed in for the A/V group – UAH 772,459.96 (52.83 % of all costs directed to the pharmaceutical support of patients). The results of the structural analysis of the group of the most expensive drugs showed that the highest costs were characteristic of L01CD02 Docetaxel (UAH 1166,531.31; 39.81 % of the total cost in the group), and the lowest – for L01DB01 Doxorubicin – UAH 63,694.14 (5.46 %, respectively). Conclusions. According to the results of the conducted research, it was established that the largest costs fall on the group of essential drugs (1047735.07 UAH, 71.65 % of all costs). This determines the need for further pharmacoeconomic calculations of breast cancer treatment to optimize the costs of antineoplastic drugs

Effects of moisture content and porosity on the thermal conductivity and volumetric specific heat capacity of pharmaceutical powders

Thermal conductivity and specific heat capacity are two important parameters for the drying process of pharmaceutical materials during methods such as wet granulation that can be observed in the overall tablet manufacturing process. In this study, a transient line heat source method was used for the first time to determine the thermal conductivity and volumetric specific heat capacity of common pharmaceutical components and binary mixtures, with moisture content ranging from 0 % to 30 % w.b and active ingredient loading between 0 % and 50 % by weight. A three-parameter least squares regression model relating the thermal properties to moisture content and porosity was evaluated at a 95 % confidence interval, with R2 values ranging from 0.832 to 0.997. Relationships were established between thermal conductivity, volumetric specific heat capacity, porosity, and moisture content for pharmaceutical ingredients including acetaminophen, microcrystalline cellulose, and lactose monohydrate.

Redox-responsive self-assembled podophyllotoxin twin drug nanoparticles for enhanced intracellular drug delivery

Podophyllotoxin (PPT) is an active natural pharmaceutical component with potent anticancer activity. However, due to its poor water solubility and serious side effects, its medical applications are limited. In this work, we synthesized a series of PPT dimers, which can be self-assembled into stable nanoparticles of 124–152 nm in aqueous solution and can significantly increase the solubility of PPT in aqueous solution. In addition, PPT dimer nanoparticles exhibited high drug loading capacity (>80%) and could store at 4 °C in aqueous state with good stability for at least 30 d. In vitro release studies showed that nanoparticles with disulfide bonds (SS NPs) can quickly release (about 96.5% drug released within 24 h) the conjugated drug in PBS buffer (pH = 7.4) in the presence of DTT. Cell endocytosis experiments showed that SS NPs enhanced cell uptake (18.56 times higher than PPT for Molm-13, 10.29 times for A2780S and 9.81 times for A2780T) and maintained antitumor effect against human ovarian tumor cells (A2780S and resistant A2780T) and human breast cancer cells (MCF-7). In addition, the endocytosis mechanism of SS NPs was revealed that these nanoparticles were mainly up-taken by macropinocytosis-mediated endocytosis. We believe that these PPT dimer-based nanoparticles will become an alternative formula for PPT, moreover the assembly behavior of PPT dimer can be extended to other therapeutic drugs.

On the Performance of a Ready-to-Use Electrospun Sulfonated Poly(Ether Ether Ketone) Membrane Adsorber.

Motivated by the need for efficient purification methods for the recovery of valuable resources, we developed a wire-electrospun membrane adsorber without the need for post-modification. The relationship between the fiber structure, functional-group density, and performance of electrospun sulfonated poly(ether ether ketone) (sPEEK) membrane adsorbers was explored. The sulfonate groups enable selective binding of lysozyme at neutral pH through electrostatic interactions. Our results show a dynamic lysozyme adsorption capacity of 59.3 mg/g at 10% breakthrough, which is independent of the flow velocity confirming dominant convective mass transport. Membrane adsorbers with three different fiber diameters (measured by SEM) were fabricated by altering the concentration of the polymer solution. The specific surface area as measured with BET and the dynamic adsorption capacity were minimally affected by variations in fiber diameter, offering membrane adsorbers with consistent performance. To study the effect of functional-group density, membrane adsorbers from sPEEK with different sulfonation degrees (52%, 62%, and 72%) were fabricated. Despite the increased functional-group density, the dynamic adsorption capacity did not increase accordingly. However, in all presented cases, at least a monolayer coverage was obtained, demonstrating ample functional groups available within the area occupied by a lysozyme molecule. Our study showcases a ready-to-use membrane adsorber for the recovery of positively charged molecules, using lysozyme as a model protein, with potential applications in removing heavy metals, dyes, and pharmaceutical components from process streams. Furthermore, this study highlights factors, such as fiber diameter and functional-group density, for optimizing the membrane adsorber's performance.

Filamentous fungi for pharmaceutical compounds degradation in the environment: A sustainable approach

Pharmaceutical compounds play an important role in enhancing the quality of human life. They substantially increase the life expectancy of humans and the well-being of livestock. The expansion in the global human population has increased the usage of pharmaceuticals in an enormous way. This has led to the emergence of pharmaceutical compounds as environmental pollutants because these components are continuously released to various water sources and terrestrial ecosystems. The pharmaceutical components are released during their synthesis, as waste from human and veterinary healthcare sectors, and dumping of drugs that are not used. Pharmaceutical components are known to persist in their potential even at lower concentrations and can create serious issues for ecosystems, especially aquatic systems. Various efforts are being made to remove or reduce the toxicity of pharmaceutical components in aquatic systems.Bioremediation using fungi is one of the most secure and sustainable ways of decontaminating polluted environments. With their strong morphology and diverse metabolic abilities, Fungi employ different methods including fungal enzymes to clear pollutants. Studies have proven that fungi and fungal enzymes can transform these pharmaceutical compounds into less toxic components. This review highlights the role of fungi in the bioremediation of pharmaceutical compounds.

Late-Stage C-H Functionalization of Azines.

Azines, such as pyridines, quinolines, pyrimidines, and pyridazines, are widespread components of pharmaceuticals. Their occurrence derives from a suite of physiochemical properties that match key criteria in drug design and is tunable by varying their substituents. Developments in synthetic chemistry, therefore, directly impact these efforts, and methods that can install various groups from azine C-H bonds are particularly valuable. Furthermore, there is a growing interest in late-stage functionalization (LSF) reactions that focus on advanced candidate compounds that are often complex structures with multiple heterocycles, functional groups, and reactive sites. Because of factors such as their electron-deficient nature and the effects of the Lewis basic N atom, azine C-H functionalization reactions are often distinct from their arene counterparts, and the application of these reactions in LSF contexts is difficult. However, there have been many significant advances in azine LSF reactions, and this review will describe this progress, much of which has occurred over the past decade. It is possible to categorize these reactions as radical addition processes, metal-catalyzed C-H activation reactions, and transformations occurring via dearomatized intermediates. Substantial variation in reaction design within each category indicates both the rich reactivity of these heterocycles and the creativity of the approaches involved.

Ethnobotany and Phytopharmacology of Avena sativa: A Qualitative Review

Among all cereals, oat is considered to be one of the goods consumed in functional grain, nutraceutical, and pharmaceutical components. The review article aims to explore plant profile, phytochemical constituents present in different parts, and potential therapeutic agent which prevents people from different diseases with their respective mechanism of action it also includes toxicity studies, dosage form, marketed formulation, and industrial application. The information on Avena sativa is collected from the different databases available in Science Direct, PubMed, Scopus, and Google Scholar to search for research papers for literature and data. Reviewed information suggests that the A. Sativa is a good source of a range of phytochemicals including lignans, saponin, anthocyanidins, and avenanthramides, which might be directly and/or indirectly linked with beneficial nutraceutical and/or pharmacological effect(s). The review states, that A. sativa is a promising candidate as a functional and/or non-functional food because of various phytoconstituents. The clinical report has described that the utilization of oats can provide several health benefits. However, systematic rational investigations for such indications and safety profiles are yet to be explored.

Microwave-assisted extraction of bioactive components from Angelica dahurica using the tailor-made natural deep eutectic solvents.

In the present study, a new, green, efficient, and sustainable microwave-assisted extraction method combined with a deep eutectic solvent was successfully established for the extraction of five important coumarins from Angelica dahurica, namely bergapten, oxypeucedanin, imperatorin, cnidilin, and isoimperatorin. Compared with the conventional extraction method, the extraction efficiency of this method was improved by 10.74%. With increasingly serious global environmental pollution, this green method will be a solution for mainstream sustainable development and lead to a stable improvement in fine industries such as food, medicine, and cosmetics. The findings of this study may provide valuable clues and a scientific basis for further research of A. dahurica and other pharmaceutical components.

Elucidating the Role of Noncovalent Interactions in Favipiravir, a Drug Active against Various Human RNA Viruses; a 1H-14N NQDR/Periodic DFT/QTAIM/RDS/3D Hirshfeld Surfaces Combined Study.

Favipiravir (6-fluoro-3-hydroxypyrazine-2-carboxamide, FPV), an active pharmaceutical component of the drug discovered and registered in March 2014 in Japan under the name Avigan, with an indication for pandemic influenza, has been studied. The study of this compound was prompted by the idea that effective processes of recognition and binding of FPV to the nucleic acid are affected predominantly by the propensity to form intra- and intermolecular interactions. Three nuclear quadrupole resonance experimental techniques, namely 1H-14N cross-relaxation, multiple frequency sweeps, and two-frequency irradiation, followed by solid-state computational modelling (density functional theory supplemented by the quantum theory of atoms in molecules, 3D Hirshfeld Surfaces, and reduced density gradient) approaches were applied. The complete NQR spectrum consisting of nine lines indicating the presence of three chemically inequivalent nitrogen sites in the FPV molecule was detected, and the assignment of lines to particular sites was performed. The description of the nearest vicinity of all three nitrogen atoms was used to characterize the nature of the intermolecular interactions from the perspective of the local single atoms and to draw some conclusions on the nature of the interactions required for effective recognition and binding. The propensity to form the electrostatic N-H···O, N-H···N, and C-H···O intermolecular hydrogen bonds competitive with two intramolecular hydrogen bonds, strong O-H···O and very weak N-H···N, closing the 5-member ring and stiffening the structure, as well as π···π and F···F dispersive interactions, were analysed in detail. The hypothesis regarding the similarity of the interaction pattern in the solid and the RNA template was verified. It was discovered that the -NH2 group in the crystal participates in intermolecular hydrogen bonds N-H···N and N-H···O, in the precatalytic state only in N-H···O, while in the active state in N-H···N and N-H···O hydrogen bonds, which is of importance to link FVP to the RNA template. Our study elucidates the binding modes of FVP (in crystal, precatalytic, and active forms) in detail and should guide the design of more potent analogues targeting SARS-CoV-2. Strong direct binding of FVP-RTP to both the active site and cofactor discovered by us suggests a possible alternative, allosteric mechanism of FVP action, which may explain the scattering of the results of clinical trials or the synergistic effect observed in combined treatment against SARS-CoV-2.

Current Understanding of Flavonoids in Cancer Therapy and Prevention.

Cancer is a major cause of death worldwide, with multiple pathophysiological manifestations. In particular, genetic abnormalities, inflammation, bad eating habits, radiation exposure, work stress, and toxin consumption have been linked to cancer disease development and progression. Recently, natural bioactive chemicals known as polyphenols found in plants were shown to have anticancer capabilities, destroying altered or malignant cells without harming normal cells. Flavonoids have demonstrated antioxidant, antiviral, anticancer, and anti-inflammatory effects. Flavonoid type, bioavailability, and possible method of action determine these biological actions. These low-cost pharmaceutical components have significant biological activities and are beneficial for several chronic disorders, including cancer. Recent research has focused primarily on isolating, synthesizing, and studying the effects of flavonoids on human health. Here we have attempted to summarize our current knowledge of flavonoids, focusing on their mode of action to better understand their effects on cancer.

Ginsenoside Rg3 Sensitizes Nasopharyngeal Carcinoma Cells to Radiation by Suppressing Epithelial Mesenchymal Transition.

Radioresistance restrains the therapeutic effect of nasopharyngeal carcinoma (NPC). Ginsenoside Rg3 (Rg3), an active pharmaceutical component extracted from ginseng, shows antitumor effects in various cancers. In this study, we aimed to determine whether Rg3 sensitized NPC cells to radiation and to explore the possible mechanisms. Our results revealed that Rg3 increased radiosensitivity in both HNE1 and CNE2 cell lines. Radiation-induced epithelial mesenchymal transition (EMT) in NPC cells and Rg3 blocked this effect. In addition, Rg3 attenuated radiation-induced epidermal growth factor receptor (EGFR) nuclear transport and DNA-dependent protein kinase expression. What's more, Rg3 significantly accelerated the apoptosis rates in irradiated NPC cells. In summary, our data suggested that Rg3 sensitized NPC cells to radiation and suppressed radiation-induced EMT. This effect is mediated through restrained EGFR nuclear translocation and increased cell apoptosis. Thus, Rg3 may be a potential radiation sensitizing agent for NPC.

Research Progress on the Mechanism of the Effective Components of Duzhong (Eucommiae Cortex) on Lumbar Disk Herniation

AbstractDuzhong (Eucommiae Cortex) is one of the most commonly used Chinese herb in the treatment of lumbar disk herniation (LDH). Both the single use of it and as a Chinese herbal compound have significant clinical efficacy. Its effective components including lignans, flavonoids, iridoid terpenes, polysaccharides, etc., participate in the treatment of LDH through multiple channels, which can effectively inhibit immune and inflammatory reactions, promote the repair of intervertebral disk bone tissues, protect neurological functions, enhance cell metabolism, regulate endocrine, etc. The signal pathways of Wnt/β-catenin, TNF, HL-1, MAPK, PI3K/AKT, and NF-κB may be also involved. The action mechanism of Duzhong (Eucommiae Cortex) on LDH is characterized by multiple paths, multiple targets, and multiple component cross-actions, but the direct effects of specific components of Duzhong (Eucommiae Cortex) on LDH pathological tissues have not been clarified in the existing studies. At present, the study on the efficacy of Chinese herbs has not yet included the chemical reactions among the pharmaceutical components and pharmaceutical processing, etc. Relevant experimental studies need to further extract the effective components through purification technology, analyze the target information between Duzhong (Eucommiae Cortex) and LDH through network pharmacology and biology, and strengthen the influence of different processing methods on the pharmaceutical effects of Chinese herbs to increase the choice of clinical medication. In the experimental study, the animal cell models were finely constructed, and the pathological targets of LDH were excavated, which was conducive to the development and application of new drugs.

Rapid Quantitative Simultaneous Determination of Vitamin A and Vitamin D in a Skin Ointment Pharmaceutical Formulation Based on Net Analyte Signal and Partial Least Squares using the UV Spectrophotometric Method

Objective: The aim of this study was to propose an easy, fast, and precise method, which can be satisfactorily applied to the simultaneous determination of the drugs in pharmaceutical dosage forms instead of the high-performance liquid chromatography (HPLC) method. Methods: Complicated and costly instruments, as well as spending a lot of time for analysis are the limitations of the chromatography method. Hence, UV spectrophotometric technique based on net analyte signal (NAS) and partial least squares (PLS) was proposed and validated for the simultaneous determination of vitamin A and vitamin D in binary mixtures and commercial skin ointment. The chromatographic technique was implemented to compare with the proposed approach for the simultaneous analysis of drugs. Results: The NAS method was able to determine vitamin A and vitamin D in the concentration range of 1–7 and 2-13 μg mL-1 at λmax=323 and λmax=261, respectively. The limit of detection (LOD) and limit of quantification (LOQ) related to the NAS method were found to be 0.092, 0.053 μg/mL and 0.214, 0.170 μg/mL for vitamin A and vitamin D, respectively. The root mean square error (RMSE) of the test series was 0.0607 and 0.0547 for vitamins A and D, respectively. Recoveries by the PLS method were found in the range of 99.98%-100.49% and 99.57%-100.88% for vitamins A and D, respectively. The results obtained from the NAS and PLS procedures were statistically compared with the reference method (HPLC) via analysis of variance (ANOVA) test, where no significant difference was observed. Conclusion: The spectrophotometry along with NAS and PLS methods are proper, rapid, and economic for the determination of pharmaceutical components in quality control laboratories.

Optimization of Ultrasound-Assisted Extraction in Limau Peels (Citrus amblycarpa), Antioxidant Activity and Its Potential as an Inhibitor for Xanthine Oxidase

Antioxidant content in limau peel (Citrus amblycarpa) is well recognized to be high. Free radicals can be neutralized by antioxidants, which can then be employed as natural active components in pharmaceuticals. One of them is an alternative xanthine oxidase (XO) inhibitor in lowering uric acid levels. Limau peel was extracted using the Ultrasound-Assisted Extraction method with ultrasonic waves showed optimum condition at amplitude of 45 in 50 minute and amplitude of 60 in 50 minute. The yield obtained was 9.07%. These results are obtained quickly without the use of solvents and excess energy. The results of phytochemical screening showed the presence of several secondary metabolites in limau peel extract, including Tannins, Phenolics, Glycoside Steroids, Flavonoids, and a small amount of Saponins. This study tested antioxidant activity using 3 different methods: the DPPH, CUPRAC, and FRAP methods. The antioxidant test results are shown in IC50 values with optimal gains of 33.40±0.01mg/L for DPPH, respectively; 21.38±0.04mg/L for CUPRAC; and 15.31±0.02mg/L for FRAP. Meanwhile, in testing the potential as a xanthine oxidase inhibitor, it was found that limau peel extract could reduce uric acid levels in vitro by 71.63±0.94%.