Active Ingredients Research Articles

Assessment of basic pharmacokinetic parameters of dapagliflozin in TTS formulations in male minipigs

Given the extended time over which diabetes treatment is administered, the transdermal delivery system is anticipated to be a more suitable option for older individuals who may experience difficulty swallowing. The continuous delivery of dapagliflozin and more stable plasma levels are anticipated to reduce the incidence of side effects and the frequency of dosing. The objectives of the study were to determine the safety and plasma pharmacokinetics of dapagliflozin in male minipigs following application of the ointment and skin patch. In the initial phase of the study, the potential for transdermal permeation of dapagliflozin from ointment and transdermal patch to blood plasma of 15 male Göttingen minipigs was investigated. In the subsequent phase, the efficacy of utilising patches of varying strengths and sizes was assessed. The LC/MS method was employed to quantify the concentration of the active substance. The transportation of the studied API to the general circulation and accumulation in tissues were confirmed. The maximum drug concentration (122.99 ng/mL) in plasma was observed on the fourth day of application. The highest calculated Cmax was 131.91 ng/mL with a mean AUC0-last of 6620.7 ng h/mL. Following transdermal administration, dapagliflozin is excreted in the urine. The trend between urinary dapagliflozin 3-O-glucuronide levels and urinary glucose excretion was also observed. The transdermal patch has been demonstrated to be an effective drug delivery system for dapagliflozin.

Glycyrrhizic Acid Inhibits Hippocampal Neuron Apoptosis by Activating the PI3K/ AKT Signaling Pathway.

Glycyrrhizic acid (GA), one of the main active substances in Glycyrrhiza, has anti-inflammatory, anti-viral, and neuroprotective effects. GA can significantly reduce cerebral infarction size in middle cerebral artery occlusion (MCAO) rats and suppress inflammatory responses. However, the underlying mechanism by which GA protects the neuronal system remains poorly understood. Cell proliferation and viability were tested using CCK-8 and Edu assays. The effects of GA on apoptosis were detected using flow cytometry and Tunel assays. Western blotting was performed to assess protein expression. Behavioral experiments were conducted using the Morris water maze and rotation tests. Infarct size was observed using TTC staining. We report that GA protects neurons by inhibiting apoptosis, mainly through the PI3K/AKT pathway in oxygen-glucose deprivation/reoxygenation (OGD/R) and MCAO rat models. GA increases the viability and proliferation of oxygen- and glucose-deprived hippocampal neurons. Hippocampal neuron apoptosis decreased after GA treatment in vitro and in vivo. Furthermore, we determined that GA treatment increased the active state of PI3K and its downstream protein p-AKT, whereas when using a specific inhibitor of PI3K, Y294002, the levels of p-PI3K and p-AKT decreased. Finally, we showed that GA treatment improved spatial memory and motor coordination in MCAO rats, while TTC staining showed that GA decreased cerebral infarct size in MCAO rats. We reveal that GA protects hippocampal neurons by inhibiting their apoptosis, mainly through the PI3K/AKT signaling pathway.

Supramolecular cyclodextrin complexes of biologically active nitrogen heterocycles

The review is devoted to the rapidly developing field of modern supramolecular chemistry - cyclodextrin complexes of biologically active nitrogen heterocycles, such as piperidines, piperazines, morpholines and pyridines. Interest in cyclodextrin complexes is growing due to the search and construction of supramolecular assemblies for targeted drug delivery. The latter is achieved as a result of supramolecular self-assembly, based on the principles of molecular recognition, and is one of the areas of modern chemistry, leading to the creation of new materials with new properties. This review fully demonstrates the ongoing scientific and practical interest in the problem of encapsulation with cyclodextrins, including nanoencapsulation. Encapsulation with cyclodextrins provides a wide range of advantages: obtaining solid dosage forms from liquid ones, stabilizing and protecting active substances from the adverse effects of external factors, increasing solubility, increasing bioavailability, reducing toxicity, prolonging action, etc. The presented review includes recent advances in the field of supramolecular complexes of biologically active nitrogen heterocycles with cyclodextrins and concludes with a discussion and identification of future promising directions for research. The review presents the results of supramolecular self-assembly of biologically active azaheterocycles with cyclodextrins.

Anti-inflammatory effects of phytosphingosine-regulated cytokines and NF-kB and MAPK mechanism.

Phytosphingosine (PHS) is a major component of the skin barrier and a multifunctional physiologically active substance. This study aimed to investigate the types of cytokines regulated by PHS, their anti-skin inflammatory effects, and their anti-inflammatory mechanisms. RAW264.7 cells stimulated with Lipopolysaccharides (LPS) were treated with PHS to measure inflammatory factors such as nitric oxide (NO) and prostaglandin E2 (PGE2), and gene expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX2) were confirmed by q-PCR. Cytokines regulated by PHS against LPS-induced inflammation were found through cytokine array, and each factor was reconfirmed through ELISA. Western blot was performed to confirm anti-inflammatory mechanism of Iκbα and MAPK. To confirm anti-skin inflammatory efficacy, HaCaT cells stimulated with TNF-α/IFN-γ were treated with PHS, and TARC, IL-6, and IL-8 were detected by ELISA. PHS suppressed the gene expression of iNOS and COX2, which were increased by LPS, and suppressed NO and PGE2 production. Through cytokine array, it was confirmed that IL-6, IL-10, IL-27 p28/IL-30, IP-10, I-TAC, MCP-5, and TIMP-1 increased by LPS were decreased by PHS. PHS inhibited NF-κB signaling by inhibiting LPS-induced NF-κB nuclear migration and p-Iκbα-mediated Iκbα degradation, and inhibited p38, ERK, and JNK signaling pathways. PHS reduced the production of TARC, IL-6, and IL-8 increased by TNF-α/IFN-γ. These results indicate PHS has anti-inflammatory effects via the suppression of inflammatory factors and pro-inflammatory cytokines through the NF-κB and MAPK pathways. Moreover, these results may explain beneficial effects of PHS in the treatment of skin inflammatory conditions induced by TNF-α/IFN-γ.

Unveiling the Underlying Mechanisms Related to the Biological Activities of Cynometra cauliflora

Abstract: Cynometra cauliflora Linn. (C. cauliflora), a member of the Fabaceae family within the Cynometra genus, is an underrated medicinal plant in Malaysia. It features frog-like fruits and is known locally as Namnam. The plant grows in tropical regions and is used in the traditional treatment of various medical conditions. Previous studies have revealed a broad range of its pharmacological benefits, including antioxidant, anti-inflammatory, anti-diabetic, anti-lipase, anti-diarrheal, cytotoxic, anti-microbial, and anti-cholinesterase properties. The active constituents identified in C. cauliflora are thought to contribute to its diverse range of biological activities. Research shows that different parts of C. cauliflora contain phenolic compounds, tannins, saponins, and flavonoids. The leaves and bark also have cardiac glycosides, while the fruit is rich in flavonoids, triterpenoids, saponins, and tannins. Furthermore, ethanol extracts of its leaves were found to contain vitamin C and its major constituent, vitexin. In this review, the biological activities of C. cauliflora are explored and reviewed through various literature sources, aiming to highlight the mechanisms and compounds that underlie its potential as a source for natural therapies.

New Active Ingredients for Sustainable Modern Chemical Crop Protection in Agriculture.

Today, the agrochemical industry faces enormous challenges to ensure the sustainable supply of high-quality food, efficient water use, low environmental impact, and the growing world population. The shortage of agrochemicals due to consumer perception, changing needs of farmers and ever-changing regulatory requirements is higher than the number of active ingredients that are placed on the market. The introduction of halogen atoms into an active ingredient molecule offers the opportunity to optimize its physico-chemical properties such as molecular lipophilicity. As early as 2010, around four-fifths of modern agrochemicals on the market contained halogen atoms. In addition, it becomes clear that modern agrochemicals have increasingly complex molecular structures with one or more stereogenic centers in the molecule. Today, almost half of modern agrochemicals are chiral molecules (herbicides, insecticides/acaricides/nematicides ≪ fungicides) and most of them consist of mixtures such as racemic mixtures of enantiomers, followed by mixtures of diastereomers and mixtures of pure enantiomers. Therefore, it is important that halogen-containing substituents or stereogenic centers are considered in the structural optimization of the active ingredients to ultimately develop sustainable agrochemicals in terms of efficacy, ecotoxicology, ease of use and cost-effectiveness.

Assessment of the Farmers’ Knowledge on Pesticide Usage and Classification of the Types of Pesticides Used in the Farms along Thiba River Catchment Area, Mwea Irrigation Scheme, Kirinyaga County, Kenya

The aim of the study was to assess the farmers’ knowledge on the safe use of pesticides, to identify the types and classify pesticides used to control pests and diseases in the catchment area using structured questionnaire, face to face interview, and focus group discussion. This was done in February and May, 2021 representing the dry and wet seasons respectively. The farmers applied 12 different pesticides, under different trade names and active ingredient. World Health Organization class Type II of the pesticides were used by 50 %, class III and IV by 25% of the farmers respectively. The WHO, Type II pesticides are considered to be toxic when manufacturers’ specifications are not adhered to and Type III are slightly toxic while IV are not toxic. Chlorpyrifos was the highest used pesticide by 72 % of the farmers followed by Lambda-cyhalothrin at 60 % while the least was Copper hydroxide by 40 %.

Study and selection of optimal rheological characteristics of piracetam gel compositions for intranasal use

Background. One of the important areas of pharmaceutical research is the creation of new, as well as improvement of existing, in-demand dosage forms, using already known drugs as active substances. Current issues are the development of drugs that activate the integrative properties and functions of the brain, as well as increase the body’s resistance to aggressive influences. Nootropics, namely piracetam and its analogues, are successfully used in neurological, psychiatric and drug treatment practice. At the same time, the intranasal route of administration is attractive for combined and longterm therapy of these diseases. when developing new intranasal compositions, the issues of choosing the optimal combination of excipients that allow the dosage form to be easily distributed in the nasal cavity must be resolved. The selection of optimal compositions based on consistency properties is possible on the basis of rheological research data, which allows not only to predict the properties of the dosage form being developed, but also to select the required composition and ratio of components. In addition, an important indicator of the quality of soft dosage forms that affects consumer properties is their stability during transportation and storage, as well as such an indicator as spreadability.Aim. Selection of the optimal composition of the gel with piracetam based on rheological characteristics and predicting the thermal and colloidal stability of the gel structure.Materials and methods. Carboxymethyl cellulose, chitosan and carbopol were chosen as the gel base. The rheological characteristics of the samples were studied by rotational viscometry on a Fungilab Premium viscometer (Spain). Data were obtained and collected using Fungilab Data Boss software; additional data processing was carried out using Microsoft Excel.Results. The gelling agent was selected and its rheological characteristics were determined.Conclusion. The optimal composition of excipients piracetam gel was selected taking into account the basic rheological parameters.

Pharmaceutical Standardization and Comparative Study of <i>Varunadi Kvatha Churna</i> as <i>Varunadi Ghana Vati</i>/Tablet and <i>Varunadi Pravahi Kvatha</i>

Background: In Ayurveda, there are many types of potent dosage forms available with their different specifications, anupan, preparation procedure and shelf life. The preparation of medicines of herbal drug origin is generally included in the Bhaishajya Kalpana section. In Bhaishajya Kalpana there are five basic dosage forms necessary to prepare formulations from herbal origin drugs i.e. Swarasa, Kalka, Kvatha, Hima and Phanta. These five basic formulations are potent dosage forms which can moulded into different finished formulations. Aim: The objectives of this study were to prepare and standardise the Varunadi Kvatha Churna as Varunadi Ghana Vati/Tablet and Varunadi Pravahi Kvatha with a comparative study. Methods: Firstly, kvatha churna was prepared as per the master formula. The kvatha churna was then used in two different ways i.e. firstly it was used to prepare Varunadi Ghana Vati (Tablet) without using any additives as it acts as a self-binder. On the other hand, Pravahi kvatha was prepared which is a self-generated alcohol formulation, in which dhataki pushpa, gudda and babool are added as a fermentation initiator and additives. Results: Physicochemical parameters do not show significant variation. According to the TLC profile, the Ghana Vati has six spots i.e. having much more active constituents than the Pravahi kvatha having two spots. Therefore, according to the parameters, it might be stated that the Pravahi kvatha has much more stability than the Ghana Vati. But as far as palatability and activity are concerned Ghana Vati is comparatively better than Pravahi kvatha Conclusion: Converting Varunadi Kvatha Churna into Varunadi Ghana Vati, Varunadi Pravahi Kvatha provides several benefits related to ease of use, dosage precision, and patient preference. Hence based on observation we stated that the Varunadi Ghana Vati has a better choice of dosage form as compared to Varunadi Pravahi Kvatha, although it has better stability.

The attrition, physical and insecticidal durability of two dual active ingredient nets (Interceptor® G2 and Royal Guard®) in Benin, West Africa: results from a durability study embedded in a cluster randomised controlled trial.

Studies evaluating the attrition, physical and insecticidal durability of dual active ingredient (AI) insecticide-treated nets (ITNs) are essential for makingprogrammatic decisions regarding their deployment. We performed a prospective study embedded in a cluster randomised controlled trial (cRCT) to evaluate the attrition, fabric integrity and insecticidal durability of Interceptor® G2 (alpha-cypermethrin-chlorfenapyr) and Royal Guard® (alpha-cypermethrin-pyriproxyfen), compared to Interceptor® (alpha-cypermethrin) in Benin. A total of 2428 study nets in 1093 randomly selected households in five clusters per arm of the cRCT were monitored for ITN attrition and fabric integrity every 6-12months post-distribution. Householders were further surveyed to investigate non-study net use and their preference for ITN fabric types used in the study nets. A second cohort of 120 nets per ITN type were withdrawn every 12months and assessed for chemical content and insecticidal activity in laboratory bioassays. Alpha-cypermethrin bioefficacy was investigated using the susceptible Anopheles gambiae Kisumu strain, and chlorfenapyr and pyriproxyfen bioefficacy were investigated using the pyrethroid-resistant Anopheles coluzzii Akron strain. Net pieces were tested in WHO cone bioassays and tunnel tests for alpha-cypermethrin and in tunnel tests for chlorfenapyr; pyriproxyfen activity was assessed in cone bioassays as the reduction in fertility of blood-fed survivors using ovary dissection. Bioefficacy was expressed as the proportion of ITNs passing predetermined WHO criteria, namely knock-down ≥ 95% or 24/72h mortality ≥ 80% or reduction in fertility ≥ 50%. Overall ITN survivorship was 52% at 24months and fell to 15% at 36months. Median ITN survival time was lower with Royal Guard® relative to Interceptor® [1.6 vs 2.3years; hazard ratio (HR) 1.49, 95% confidence interval (CI) 1.36-1.66; p < 0.001] and Interceptor® G2 (1.6 vs 2.1years; HR 1.33, 95% CI 1.20-1.47; p < 0.001). Householders overwhelmingly preferred polyester nets over polyethylene nets (96%), and more Royal Guard® nets were replaced with spare polyester nets from previous campaigns. All Royal Guard® nets passed efficacy criteria for alpha-cypermethrin at all time points (100%) while ITN pass rates after 24months had fallen to < 40% for pyriproxyfen and chlorfenapyr. The chemical content analysis showed a higher loss rate of the non-pyrethroid insecticides relative to the pyrethroids in each dual ingredient AI ITN; 74% vs 47% for Royal Guard® and 85% vs 63% for Interceptor® G2 at 36months. The median ITN survival time for Interceptor® G2 (2.1years) and Royal Guard® (1.6years) in Benin is substantially lower than 3years. Royal Guard® nets were discarded more quickly by householders, partly due to their low preference for polyethylene nets. The insecticidal activity of the non-pyrethroid insecticides in both dual AI ITNs was short-lived compared to alpha-cypermethrin. The results corroborate the findings from the cRCT conducted in Benin.

Determination of an Anti-Parasitic Active Pharmaceutical Ingredient in Wastewater Effluents Using Capillary Zone Electrophoresis.

Ireland has a successful pharmaceutical industry with over 100 pharmaceutical manufacturing sites across the island. Although this success has many benefits, the irreversible effects emissions from pharmaceutical manufacturing can have on the environment are a major drawback. Although known pollutants are regularly monitored with limits set out by the Environmental Protection Agency, one significant pollutant has been overlooked: pharmaceutical pollution. Detecting these pollutants and ensuring they are at a safe concentration for the environment is of utmost importance. In recent years, capillary electrophoresis is being recognised as a suitable alternative to high-performance liquid chromatography due to its many benefits such as faster analysis, water-based buffers and smaller sample volumes. In this paper, a capillary zone electrophoresis (CZE) method with a preconcentration step of solid-phase extraction was developed for an anti-parasitic active pharmaceutical ingredient (API) called ZB23. The API was successfully detected in a wastewater sample in less than 10min using the CZE parameters of 25mM borate buffer with a pH of 10.5, 15% MeOH, 10kV voltage, 25mbar for 5s injection size, an Lt of 40cm, an Ld of 31.5cm and a detection wavelength of 214nm.

Intoxicação por &lt;i&gt;Palicourea marcgravii&lt;/i&gt; em bovinos no Brasil

Palicourea marcgravii is considered the most important toxic plant that causes sudden death in cattle in Brazil, due to its extensive national distribution, high toxicity, good palatability and cumulative effect, being responsible for deaths and economic losses in Brazilian livestock every year. Its active toxic principle is monofluoroacetic acid which inhibits the Krebs cycle, interrupting the metabolism of carbohydrates, fats and proteins. There´s not treatment for the poisoning due to its superacute progression, and prevention is based on the construction of fences around forested areas, cutting access to the plants.

Organ-protective effects of the alternative renin-angiotensin system and prospects for therapeutic treatment. Review

The article is devoted to review the data regarding the identification of biochemical and functional features of the components of the renin‑angiotensin system using the tools of bibliometric analysis of scientific literature. A modern interpretation by the dividing of the multifunctional complex into two systems, namely the classical renin‑angiotensin system and alternative renin‑angiotensin system, in accordance with the definition of biological effects, is given. The enzymatic cascade involved in the production and metabolism of peptides in both classical and non‑classical pathways of renin‑angiotensin systems is shown from the point of view of the evolution of scientific concepts. The triggering role of components of the classical renin‑angiotensin system in pathophysiological processes with transformation into cardiovascular diseases and metabolic dysfunction has been proven. The history of the creation of pharmacological drugs for the correction of the classic renin‑angiotensin system is presented. In view of the achievement of recent years, the revision of the alternative renin‑angiotensin system is emphasized due to the discovery of the counter‑regulatory action of the angiotensin‑converting enzyme 2, angiotensin‑(1—7), the Mas receptor in relation to their correction of metabolic processes, regulation of blood pressure, and the presence of anti‑fibrotic, anti‑inflammatory and antioxidant properties. The positive effect of the components of the non‑classical renin‑angiotensin system on the protection of the cardiovascular system and kidney is presented based on the results of experimental studies on animals. Pharmacokinetic and pharmacodynamics characteristics of recombinant angiotensin‑converting enzyme 2 in experiments on healthy volunteers are highlighted. The potential protective effects of angiotensin‑converting enzyme 2 and angiotensin‑(1—7) concerning cardiometabolic risk are presented. The available data indicate the need for further comprehensive scientific investigations of the components of alternative renin‑angiotensin system to create a new class of pharmacological agents with their implementation in medical practice.

Bergenin, the main active ingredient of Bergenia purpurascens, attenuates Th17 cell differentiation by downregulating fatty acid synthesis.

Bergenin is the main active ingredient of Bergenia purpurascens, a medicinal plant which has long been used to treat a variety of Th17 cell-related diseases in China, such as allergic airway inflammation and colitis. This study aimed to uncover the underlying mechanisms by which bergenin impedes Th17 cell response in view of cellular metabolism. Invitro, bergenin treatment reduced the frequency of Th17 cells generated from naïve CD4+ T cells of mice. Mechanistically, bergenin preferentially restrained fatty acid synthesis (FAS) but not other metabolic pathways in differentiating Th17 cells, and exogenous addition of either palmitic acid (PA) or oleic acid (OA) and combination with acetyl-CoA carboxylase 1 (ACC1) activator citric acid dampened the inhibition of bergenin on Th17 cell differentiation. Bergenin inhibited FAS through downregulating the expression of SREBP1 via restriction of histone H3K27 acetylation in the SREBP1 promoter, and SREBP1 overexpression weakened the inhibition of bergenin on Th17 differentiation. Furthermore, bergenin was shown to directly interact with SIRT1 and result in activation of SIRT1. Either combination with SIRT1 inhibitor EX527 or point mutation plasmid of SIRT1 diminished the inhibitory effect of bergenin on FAS and Th17 cell differentiation. Finally, the inhibitory effect of bergenin on Th17 cell response and SIRT1 dependence were verified in mice with dextran sulfate sodium-induced colitis. In short, bergenin repressed Th17 cell response by downregulating FAS via activation of SIRT1, which might find therapeutic use in Th17 cell-related diseases.

From biological potency absorbed components to artificial intelligence mining: A review of analytical strategies for the discovery and validation of quality marker in traditional Chinese medicine in the past decade

Quality control of Traditional Chinese Medicine (TCM) is fundamental to ensuring its clinical efficacy, with TCM formulas being the primary form used in clinical practice. Current quality control methods for TCM formulas often rely on pharmacopoeial standards for individual medicinal materials, typically encompassing only characteristic or partial active ingredients. These methods fail to fully reflect the clinical efficacy of TCM formulas. Consequently, exploring the multiple efficacious components in TCM formulas and establishing the correlation between multi-component content and efficacy has become an urgent issue in the modern quality assessment of TCM formulas. The quality marker (Q-marker) has emerged as a crucial standard in this field, achieving notable success in recent years. This paper reviews recent progress in the development of the Q-marker system in TCM by highlighting strategies based on the correlation between efficacy and constituents, using analytical techniques to investigate the material basis and efficacy of TCM. However, the aforementioned methods inevitably involve human selection factors. With the widespread application of artificial intelligence (AI) learning algorithms, it is now possible to develop a modern quality evaluation method for the multi-component “efficacy-quality” correlation in TCM formulas. This approach leverages AI techniques to explore novel and quantifiable methods for scientific and rational quality control in TCM formulas. In this paper, important future directions and questions in this field are also discussed.

Bioinformatics-based drug repositioning and prediction of the main active ingredients and potential mechanisms of action for the efficacy of Dan-Lou tablet

Drug repositioning is gaining attention as a method for developing new drugs due to its low cost, short cycle time, and high success rate. One important approach is to explore new uses for already marketed drugs. In this study, we utilized the strategy of drug repositioning, focusing on the Dan-Lou tablet. We predicted the efficacy of Dan-Lou tablet against non-small cell lung cancer based on gene expression similarity and verified it by in vitro experiments. Next, we performed further analysis and validation using network pharmacology, molecular docking and molecular dynamics. Based on the results, it was concluded that Dan-Lou tablet mainly acted through nine compounds, Quercetin, Luteolin, Scoparone, Isorhamnetin, Eugenol, Genistein, Coumestrol, Hederagenin, Succinic Acid, and mainly targeted CCL2, FEN1, TPI1, RMI2 by six pathways. This discovery not only provides a new idea for the development of Dan-Lou tablet but also provides useful predictive information for clinical treatment. The method we adopted has great development prospects as a way to predict the efficacy of new drugs and their main mechanisms of action, and it has a positive impact on the research and development of new drugs using drug repositioning and the modernization of traditional Chinese medicine.

Preparation of a nanoemulsion containing active ingredients of cannabis extract and its application for glioblastoma: in vitro and in vivo studies

Recently, the anti-tumor effects of cannabis extract on various cancers have attracted the attention of researchers. Here, we report a nanoemulsion (NE) composition designed to enhance the delivery of two active components in cannabis extracts (∆9-Tetrahydrocannabinol (THC) and Cannabidiol (CBD)) in an animal model of glioblastoma. The efficacy of the NE containing the two drugs (NED) was compared with the bulk drugs and carrier (NE without the drugs) using the C6 tumor model in rats. Hemocompatibility factors (RBC, MCV, MCH, MCHC, RDW, PPP, PT and PTT) were studied to determine the potential in vivo toxicity of NED. The optimized NED with mean ± SD diameter 29 ± 6 nm was obtained. It was shown that by administering the drugs in the form of NED, the hemocompatibility increased. Cytotoxicity studies indicated that the NE without the active components (i.e. mixture of surfactants and oil) was the most cytotoxic group, while the bulk group had no toxicity. From the in vivo MRI and survival studies, the NED group had maximum efficacy (with ~4 times smaller tumor volume on day 7 of treatment, compared with the control. Also, survival time of the control, bulk drug, NE and NED were 9, 4, 12.5 and 51 days, respectively) with no important adverse effects. In conclusion, the NE containing cannabis extract could be introduced as an effective treatment in reducing brain glioblastoma tumor progression.Graphical abstract

Is fluoride the best we've got? The most common toothpaste active ingredients and their influence on caries and oral health: A brief review of the literature

Aim of the study Toothpaste is a paste or gel to be used with a toothbrush to maintain and improve oral health and aesthetics. Nowadays there is a great variety of ingredients that might have different effects on caries development or oral health in general. Society continues to seek ways to replace fluoride or include more natural ingredients in everyday hygiene products. The aim of our study is to present current knowledge of various ingredients in toothpastes regarding their influence on teeth and intraoral soft tissues and the possibility of replacing fluoride with other substances. Material and methods Our review is based on the analysis of materials collected in„Pubmed”, „Google Scholar” and other scientific articles using keywords: „toothpaste”, „fluoride”, „ingredients”, “hydroxyapatite”, „chlorhexidine”, “triclosan”, “propolis”, “aloe vera”, “charcoal”, “oleanolic acid”, “SLS”, “xylitol” Conclusions Despite numerous studies, there is space for further research in finding substances that might improve toothpastes with or without extracting fluoride from them. Fluoride has the most proven effectiveness in caries prevention, with fluorosis as its most damaging side effect, while hydroxyapatite shows promising results. Although, there are many substances that might be useful in oral health care products.

RP-HPLC Method for Simultaneous Quantification of Withanolides in &lt;i&gt;Withania somnifera&lt;/i&gt;

Background: Withanolides are the primary bioactive components of Withania somnifera (L.) Dunal. Among them, withanolide A, and 12-deoxy-withastramonolide are the herb’s most physiologically active ingredients. The steroidal lactones are isomers, which makes them difficult to separate. Aim: In the current research, a simple, precise, accurate, and decent RP-HPLC method has been developed, optimised and validated for simultaneous quantification and separation. Methods: Resolution was conducted on Gemini, Phenominex C18 (250mm X 4.6mm, 5 μ) column at 40oC utilising binary mobile phases of acetonitrile and ammonium acetate (10 mM) in gradient mode with 1.0 mL/min flow rate and observed at 230 nm. The total run time was twenty-five minutes. The procedure complied with ICH guidelines, covering the limit of detection, specificity, linearity, quantification, precision, accuracy, and robustness. Results: The standard curves of both relevant analytes displayed a linear pattern with regression values &gt; 0.999 in the 1–10 μg/mL range. For both herbal markers, 1 μg/mL was the lowest limit of quantification. The method’s accuracy was 100.38-100.93 % and 99.13-100.75 % for with withanolide A, and 12-deoxy-withastramonolide respectively. The precision of within and between days was found in the tolerable limit of &gt;2% for both herbal markers. Conclusion: The suggested method worked well for simultaneously analyzing the extracted samples and identifying withanolides.

SUITABLE INSECTICIDE FOR INTEGRATED PEST MANAGEMENT

The article presents the results of testing the oxadiazine insecticide Avaunt with the active substance indoxacarb against the cotton bollworm on cotton and the mulberry moth on mulberries. In all experiments, high efficiency against caterpillars of all ages was obtained, which greatly distinguishes it from other preparations - larvicides. Depending on the objects, the consumption rates of the preparation can be in the range from 0.3 to 0.45 l / ha. The preparation is practically non-toxic for entomophages - trichogramma, bracon and lacewing, which is especially valuable in integrated plant protection programs. KEYWORDS: Cotton, tomato, insecticide, avaunt, cotton bollworm, mulberry moth, entomophages, efficiency.