ABSTRACT
German chamomile (Matricaria chamomilla L.) is an essential oil- containing medicinal plant used worldwide. The aim of this study was to gain knowledge of the phytochemical composition and the analgesic and soporific activity of Matricaria chamomilla L. (German chamomile) flower extract and its amino acid preparations, to predict the mechanisms of their effects by molecular docking and to develop aqueous printing gels and novel 3D-printed oral dosage forms for the flower extracts. In total, 22 polyphenolic compounds and 14 amino acids were identified and quantified in the M. chamomilla extracts. In vivo animal studies with rodents showed that the oral administration of such extracts revealed the potential for treating of sleep disorders and diseases accompanied by pain. Amino acids were found to potentiate these effects. Glycine enhanced the analgesic activity the most, while lysine and ß-alanine improved the soporific activity. The molecular docking analysis revealed a high probability of γ-aminobutyric acid type A (GABAA) and N-methyl-D-aspartate (NMDA) receptor antagonism and 5-lipoxygenase (LOX-5) inhibition by the extracts. A polyethylene oxide (PEO)-based gel composition with the M. chamomilla extracts was proposed for preparing a novel 3D-printed dosage form for oral administration. These 3D-printed extract preparations can be used, for example, in dietary supplement applications.
Subject(s)
Amino Acids , Flowers , Matricaria , Molecular Docking Simulation , Phytochemicals , Plant Extracts , Printing, Three-Dimensional , Plant Extracts/chemistry , Plant Extracts/pharmacology , Animals , Matricaria/chemistry , Amino Acids/chemistry , Flowers/chemistry , Phytochemicals/chemistry , Phytochemicals/pharmacology , Rats , Analgesics/chemistry , Analgesics/pharmacology , Male , MiceABSTRACT
The pharmaceutical industry usually utilizes either hydrophobic or hydrophilic substances extracted from raw plant materials to prepare a final product. However, the waste products from the plant material still contain biologically active components with the opposite solubility. The aim of this study was to enhance the comprehensive usability of plant materials by developing a new no-waste extraction method for eucalypt leaves and by investigating the phytochemical and pharmacological properties of eucalypt extracts and their 3D-printed dosage forms. The present extraction method enabled us to prepare both hydrophobic soft extracts and hydrophilic (aqueous) dry extracts. We identified a total of 28 terpenes in the hydrophobic soft extract. In the hydrophilic dry extract, a total of 57 substances were identified, and 26 of them were successfully isolated. The eucalypt extracts studied showed significant antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Candida albicans, Corynebacterium diphtheriae gravis, and Corynebacterium diphtheriae mitis. The anti-inflammatory activity of the dry extract was studied using a formalin-induced-edema model in mice. The maximum anti-exudative effect of the dry extract was 61.5% at a dose of 20 mg/kg. Composite gels of polyethylene oxide (PEO) and eucalypt extract were developed, and the key process parameters for semi-solid extrusion (SSE) 3D printing of such gels were verified. The SSE 3D-printed preparations of novel synergistically acting eucalypt extracts could have uses in antimicrobial and anti-inflammatory medicinal applications.
ABSTRACT
Pineapple weed (Matricaria discoidea DC.) is a widespread plant in Europe and North America. In ethnomedicine, it is well-known for its anti-inflammatory and spasmolytic activities. The aim of this research was to develop novel methods of M. discoidea processing to obtain essential oil and dry extracts and to investigate their phytochemical compositions. Moreover, the molecular docking of the main substances and the in vivo studies on their soporific and analgesic activities were conducted. The essential oil and two dry extracts from M. discoidea were prepared. A total of 16 phenolic compounds (seven flavonoids, seven hydroxycinnamic acids, and two phenolic acids) in the dry extracts were identified by means of UPLC-MS/MS. In the essential oil, nine main terpenoids were identified by gas chromatography (GC). It was shown that phenolic extraction from the herb was successful when using 70% ethanol in a triple extraction method and at a ratio of 1:14-1:16. The in vivo studies with rodents demonstrated the analgesic activity of the M. discoidea extracts and improvements in the sleep of animals. The dry extracts of M. discoidea did not show any toxicity. The molecular docking analysis showed a high probability of COX-1,2 inhibition and NMDA receptor antagonism by the extracts.
Subject(s)
Matricaria , Oils, Volatile , Animals , Molecular Docking Simulation , Plant Extracts/pharmacology , Plant Extracts/chemistry , Chromatography, Liquid , Tandem Mass Spectrometry , Analgesics/pharmacology , Analgesics/chemistry , Phytochemicals/pharmacology , Phytochemicals/chemistry , Oils, Volatile/pharmacology , Ethanol , Phenols/pharmacology , Antioxidants/chemistryABSTRACT
Galenic preparations of German chamomile are used to treat mild skin diseases, inflammation, and spasms, and they have also been reported to have anxiolytic and sedative effects. The medicinal use of chamomile is well known in ethnomedicine. After obtaining its galenic preparations, there is lots of waste left, so it is expedient to develop waste-free technologies. The aims of this study were to gain knowledge of the ethnomedical status of chamomile in the past and present, develop methods for preparing essential oils and dry extracts from German chamomile flowers using complex processing, reveal the phytochemical composition of such extracts, and verify the analgesic and soporific activity of the extracts. Two methods for the complex processing of German chamomile flowers were developed, which allowed us to obtain the essential oil and dry extracts of the tincture and aqueous extracts as byproducts. A total of 22 phenolic compounds (7 hydroxycinnamic acids, 13 flavonoids, and 2 phenolic acids) were found in the dry extracts by using UPLC-MS/MS. In total, nine main terpenoids were identified in the chamomile oil, which is of the bisabolol chemotype. During the production of chamomile tincture, a raw material-extractant ratio of 1:14-1:16 and triple extraction are recommended for its highest yield. In in vivo studies with mice and rats, the extracts showed analgesic activity and improvements in sleep. The highest sedative and analgesic effects in rodents were found with the dry extract prepared by using a 70% aqueous ethanol solution for extraction at a dose of 50 mg/kg. The developed methods for the complex processing of German chamomile flowers are advisable for implementation into the pharmaceutical industry to reduce the volume of waste during the production of its essential oil and tincture, and to obtain new products.
ABSTRACT
Anxiety disorders are highly prevalent worldwide and can affect people of all ages, genders and backgrounds. Much efforts and resources have been directed at finding new anxiolytic agents and drug delivery systems (DDSs) especially for cancer patients to enhance targeted drug delivery, reduce drug adverse effects, and provide an analgesic effect. The aim of this study was (1) to design and develop novel nanofiber-based DDSs intended for the oral administration of new 1,2,3-triazolo-1,4-benzodiazepines derivatives, (2) to investigate the physical solid-state properties of such drug-loaded nanofibers, and (3) to gain knowledge of the anxiolytic activity of the present new benzodiazepines in rodents in vivo. The nanofibers loaded with 1,2,3-triazolo-1,4-benzodiazepine derivatives were prepared by means of electrospinning (ES). Field-emission scanning electron microscopy and attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy were used for the physicochemical characterization of nanofibers. The anxiolytic activity of new derivatives and drug-loaded nanofibers was studied with an elevated plus maze test and light-dark box test. New 1,2,3-triazolo-1,4-benzodiazepine derivatives showed a promising anxiolytic effect in mice with clear changes in behavioral reactions in both tests. The nanofiber-based DDS was found to be feasible in the oral delivery of the present benzodiazepine derivatives. The nanofibers generated by means of ES presented the diameter in a nanoscale, uniform fiber structure, capacity for drug loading, and the absence of defects. The present findings provide new insights in the drug treatment of anxiety disorders with new benzodiazepine derivatives.
Subject(s)
Anti-Anxiety Agents , Nanofibers , Humans , Female , Male , Mice , Animals , Nanofibers/chemistry , Benzodiazepines , Hypnotics and Sedatives , Anticonvulsants , Drug Delivery SystemsABSTRACT
One of the key pathogenetic links in type 2 diabetes mellitus (T2DM) is the formation of insulin resistance (IR). Besides a wide selection of synthetic antidiabetic drugs, various plant-origin extracts are also available to support the treatment of T2DM. This study aimed to investigate and gain knowledge of the chemical composition and potential IR correction effect of American cranberry (Vaccinium macrocarpon Aiton) leaf extracts and formulate novel 3D-printed oral dosage forms for such extracts. The bioactivity and IR of L-arginine-loaded cranberry leaf extracts were studied in vivo in rats. The cranberry leaf extracts consisted of quinic, 3-caffeoylquinic (chlorogenic), p-coumaroylquinic acids, quercetin 3-O-galactoside, quercetin-3-O-glucoside, quercetin-3-xyloside, quercetin-3-O-arabino pyranoside, quercetin-3-O-arabinofuranoside, quercetin 3-O-rhamnoside, and quercetin-O-p-coumaroyl hexoside-2 identified by HPLC. In vivo studies with rats showed that the oral administration of the cranberry leaf extracts had a positive effect on insulin sensitivity coefficients under the insulin tolerance test and affected homeostasis model assessment IR levels and liver lipid content with experimental IR. A novel 3D-printed immediate-release dosage form was developed for the oral administration of cranberry leaf extracts using polyethylene oxide as a carrier gel in semi-solid extrusion 3D printing. In conclusion, American cranberry leaf extracts loaded with L-arginine could find uses in preventing health issues associated with IR.
ABSTRACT
The liver is an organ with several important biofunctions, for which there are very few effective and safe preparations that promote the functioning, protection, and regeneration of cells. Sufficiently safe preparations with hepatoprotective activity can be found in plants. The aim of our study was to investigate the chemical composition of an extract made from American cranberry (Oxycoccus macrocarpus (Ait.) Pursh) leaves and its amino-acids preparations as well as their possible hepatoprotective activity. Using the UPLC-MS/MS method, we identified 19 phenolic compounds (8 flavonoids (flavones and flavonols), 4 anthocyanins, 3 hydroxycinnamic acids, and 2 catechins). The prophylactic and therapeutic administration of the American cranberry-leaves extracts led to a decrease in the lipid-peroxidation process during a study of tetrachloromethane acute toxic damage in the liver of rats. As a result of animal studies, the most effective hepatoprotective activity was found in the extract preparations with valine and arginine.
ABSTRACT
Overcoming the health threatening consequences of staphylococcal infections and their negative socio-economic effects have become a priority in the medical, pharmaceutical, food and many other sectors globally. Staphylococcal infections are a big challenge for a global health care, since they are difficult to be diagnosed and treated. Therefore, the development of new medicinal products of plant-origin is timely and important, because bacteria have a limited ability to develop resistance to such products. In the present study, a modified eucalypt (Eucalyptus viminalis L.) extract was prepared and further enhanced by using different excipients (surface active agents) to obtain a water-miscible 3D-printable extract (nanoemulsified aqueous eucalypt extract). Phytochemical and antibacterial studies of the eucalypt leaves extracts were conducted as a preliminary investigation for 3D-printing experiments of the extracts. The nanoemulsified aqueous eucalypt extract was mixed with polyethylene oxide (PEO) to form a gel applicable for semi-solid extrusion (SSE) 3D printing. The key process parameters in a 3D-printing process were identified and verified. The printing quality of the 3D-lattice type eucalypt extract preparations was very good, demonstrating the feasibility of using an aqueous gel in SSE 3D printing also exhibiting compatibility of the carrier polymer (PEO) with the plant extract. The SSE 3D-printed eucalypt extract preparations presented a rapid dissolution in water within 10-15 min, suggesting the applicability of these preparations e.g., in oral immediate-release applications.
Subject(s)
Anti-Infective Agents , Staphylococcal Infections , Humans , Drug Liberation , Polyethylene Glycols , Printing, Three-Dimensional , Pharmaceutical Preparations , Technology, Pharmaceutical , TabletsABSTRACT
Inonotus obliquus grows in the Northern Hemisphere on some living broadleaved tree species as a pathogen, causing stem rot. In Estonia, the fungus is well known in the Betula species but can also be found on Alnus. Sterile conks of I. obliquus contain different bioactive compounds, but the quantitative and comparative research of these compounds in conks on different host species is limited. In the current work, I. obliquus was isolated and, evidently, determined from Alnus incana (L.) Moench., Alnus glutinosa (L.) Gaertn., and Betula pendula Roth, and the content of bioactive compounds in conks on these hosts were analysed. All the analysed conks sampled from A. incana and B. pendula contained betulin that varied from 111 to 159 µg/g. A significantly (p < 0.05) higher betulinic acid content was found in conks sampled from A. incana when compared with B. pendula: 474−635 and 20−132 µg/g, respectively. However, the conks from Betula were richer in total polyphenols, flavonols, and glucans. The content of inotodiol was quite similar in the conks from A. incana (7455−8961 µg/g) and B. pendula (7881−9057 µg/g). Also, no significant differences in the lanosterol content were found between the samples from these two tree species. To the best of our knowledge, this study is the first investigation of the chemical composition of I. obliquus parasitizing on Alnus. The results demonstrate that the bioactive compounds are promising in conks of I. obliquus growing not only on Betula but also on the Alnus species. It supports the opportunity to cultivate I. obliquus, also on the Alnus species, thus increasing the economic value of growing this tree species in forestry.
Subject(s)
Alnus , Alnus/chemistry , Betula/chemistry , Flavonols , Glucans , Inonotus , LanosterolABSTRACT
The most promising plant from the genus Agrimony (Agrimonia L.) of the Rosaceae family for use in medical practice is Agrimonia eupatoria L. Phytochemical and pharmacological research in Agrimonia eupatoria L. herb extract, obtained with using 40% ethanol solution as an extractant were carried out. A total of 11 free and 17 bound monosaccharides, 17 amino acids were found in the studied extract, 9 of which are essential. Gallic and ellagic acids, gallocatechin, epigallocatechin, catechin, epicatechin, and epicatechin gallate were identified in the extract of A. eupatoria by the HPLC method; as well as hydroxycinnamic acids: hydroxyphenylacetate, caffeic, syringic, p-coumaric, ferulic, sinapic, cinnamic and quinic acid; flavonoids: quercetin-3-D-glucoside (isoquercitrin), neohesperidin, naringenin, luteolin were found, and their quantitative content was determined, as well by spectrophotometric methods. The herb extract of A. eupatoria belongs to practically non-toxic substances and has pronounced anti-inflammatory (at a dose of 10.0 mg/kg anti-exudative activity reached a maximum in 5 h (88.17%)) and hepatoprotective activity (at a dose of 25 mg/kg it reduce AlAt level by 1.1 and 1.2 times, respectively; AsAt by 1.2 and 1.1 times, respectively), reduces the level of lipid peroxidation and stabilizes the membrane structures of liver cells. Thus, the herb extract of A. eupatoria is a promising substance for the creation of phytomedicines with anti-inflammatory and hepatoprotective activity.
ABSTRACT
Bearberry (Arctostaphylos uva-ursi L.) is a perennial plant of the heather family (Ericaceae). The leaves are dominated by arbutin, phenol carbonic acids flavonoids, saponins, etc. It was previously shown that the bearberry leaves extract reduced blood glucose level in healthy animals under glucose overload, so it need to be studied more detail. The aim of the study was to investigate the chemical composition and the effect of dry alcohol extract from bearberry leaves, which enriched with cysteine, on the rats pancreas under experimental dexamethasone-induced insulin resistance (IR). Arctostaphylos uva-ursi L. leaves extract and its modified cysteine preparation were obtained according to the developed method with 50% ethanol solution. Their phytochemical profile, hypoglycaemic and pancreatic protective effect were investigated. Phenologlycoside (arbutin), phenolic carboxylic acid (gallic acid), 5 flavonoids and 4 hydroxycinnamic acids were identified and quantified in the extracts by HPLC. Present data revealed that bearberry leaves alcoholic dry extract enriched with cysteine has a hypoglycaemic and pancreatic protective effect in treated animals under dexamethasone-induced IR model. Treatment improved hyperglycaemia, insulin resistance and beta cell reduction induced by dexamethasone injections.
ABSTRACT
The aerial parts of Anthemis tinctoria L. and Angelica sylvestris L. and the roots of A. sylvestris have been used as traditional anticancer remedies in Estonian ethnomedicine. The aim of this study was to investigate content of essential oils (by gas chromatography) and polyphenolic compounds (using two different methods of high performance liquid chromatography-mass spectrometry (HPLC-MS)) of both plant species, as well as the in vitro anti-cancer effects of their essential oils and methanolic extracts. The average (n = 5 samples) yield of essential oils was 0.15%, 0.13%, and 0.17%, respectively. The principal compounds of the essential oil from the aerial parts of A. tinctoria were palmitic acid (15.3%), p-cymene (12.6%), and α-muurolene (12.5%), and α-pinene (45.4%), p-cymene (15.5%), and ß-myrcene (13.3%) in aerial parts of A. sylvestris, while isocaryophyllene oxide (31.9%), α-bisabolol (17.5%), and α-pinene (12.4%) were the main constituents in the roots. The most abundant phenolic compounds in aerial parts were the derivatives of caffeic acid, quinic acid, and quercetin; the main compounds in roots of A. sylvestris were chlorogenic acid, quinic acid, and naringenin. The strongest anticancer effects were observed in essential oils of A. sylvestris roots and aerial parts on human carcinoma in the mouth cells (KB, IC50 19.73 µg/mL and 19.84 µg/mL, respectively). The essential oil of A. tinctoria showed a strong effect on KB and LNCaP cells (27.75-29.96 µg/mL). The methanolic extracts of both plants had no effect on the cancer cells studied.
ABSTRACT
Berberine (BBR) is a plant-origin quaternary isoquinoline alkaloid presenting exogenous cholesterol lowering and anti-hyperlipidemia therapeutic effects. The aim of this study was to design and generate BBR-loaded proliposomes (PLs) as solid templates for high-dose liposomes and consequently, to enhance the oral bioavailability and therapeutic effect of BBR. An air-suspension coating (layering) method was used for generating BBR-loaded PLs. The size, distribution size, morphology, and entrapment efficiency (EE) of the final reconstituted liposomes were assessed. The oral bioavailability and endogenous cholesterol lowering effects of BBR loaded in liposomes were investigated in rats and mice, respectively. The BBR-loaded PLs showed a smooth BBR-embedded film around micron-scale carrier particles (mannitol). The reconstituted BBR-loaded liposomes had a nano-scale average size (116.6 ± 5.8 nm), narrow size distribution (polydispersity index, PDI 0.269 ± 0.038), and high EE (87.8 ± 1.0%). The oral bioavailability of reconstituted BBR-loaded liposomes at a dose of 100 mg/kg in rats was increased even 628% compared to that obtained with pure BBR (according to 90% confidence interval). The BBR-loaded liposomes at the daily oral dose 100 mg/kg in P-407- reduced total cholesterol, triglycerides and low-density lipoprotein cholesterol (LDL-C) in hyperlipidemic mice by 15.8%, 38.2%, and 57.0%, respectively.
Subject(s)
Berberine , Animals , Berberine/chemistry , Cholesterol , Cholesterol, LDL , Disease Models, Animal , Liposomes/chemistry , Mice , RatsABSTRACT
Previously, it has been shown that factors like ethnicity and proficiency of state's official language not only influence self-management abilities and medication adherence but may also indicate the level of trust in physicians, medication, and healthcare system. This research aims to examine the potential impact of ethnicity on medication adherence based on the example of a post-Soviet country. The research was carried out as a quantitative survey among 303 hypertension and type 2 diabetes patients in Estonia, involving participants from ethnic majority and minority. Research was conducted in community pharmacies and data analysed statistically with SPSS. The findings were opposite to previous research. Although members of the ethnic minority used less illness-related sources, these sources relied more on evidence-based medicine compared to the ethnic majority. Because of this, medication adherence was also slightly higher for the ethnic minority compared to the majority. Therefore, these findings indicate trust in medical authorities, their decisions, and recommendations. There was a statistically significant relationship between general and illness-related information-seeking activity; however, medication adherence was not related to information-seeking activity. The research outlines that in addition to ethnolinguistic aspect, also potential cultural influence might determine the trust in medicine and medication adherence.
Subject(s)
Diabetes Mellitus, Type 2 , Ethnicity , Chronic Disease , Diabetes Mellitus, Type 2/drug therapy , Humans , Medication Adherence , Minority GroupsABSTRACT
Constant improvement of the quality of community pharmacy services is important in the development of contemporary patient care. A national and voluntary Community Pharmacy Services Quality Guidelines (CPSQG) was developed to formulate the principles of contemporary pharmacy services, including quality criteria for service provision. The purpose of this study was to identify the implementation of the CPSQG as a profession-driven initiative towards improving and harmonizing community pharmacy services in Estonia. Three cross-sectional electronic surveys were conducted among community pharmacies in Estonia in 2014 (N = 478 pharmacies), 2016 (N = 493), and 2019 (N = 494), and the CPSQG indicators were used for evaluation of the service quality. In this study, the aggregated data, collected in three study years were used to identify the implementation of guidelines into practice. For data analysis, the One-Way ANOVA test and Post-hoc multiple comparisons were used. The results demonstrated slow implementation of the CPSQG, but guidelines-based evaluation enabled a detailed overview of the community pharmacy activities and provided services. In order to develop community pharmacy services more efficiently, the use of implementation science principles, continuous introduction of the CPSQG to the pharmacists, and more active involvement of the state could be considered in the future.
ABSTRACT
Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.
Subject(s)
Berberine/administration & dosage , Berberine/chemistry , Drug Compounding , Liposomes , Nanoparticles , Administration, Oral , Chemical Phenomena , Liposomes/chemistry , Molecular Structure , Nanoparticles/chemistry , Nanoparticles/ultrastructure , Particle Size , SolubilityABSTRACT
Increasing need in society to provide collaborative and patient-centered pharmaceutical care has to be addressed in curriculum development. Principles of competency-based pharmacy education (CBPE) could be seen as one solution to the new professional challenges of pharmacists. At the University of Tartu (UT), the Pharmacy curriculum was updated in 2019 to introduce principles of CBPE. The aim of this study was to gather initial students' feedback on the development of CBPE at the UT. The survey was conducted in the spring semester of the 2019/2020 academic year to collect feedback about all curricula at the UT. All 1st, 3rd, and 5th year pharmacy students (n = 67) were invited and 70.1% (N = 47) of them also participated in this study in order to evaluate the Pharmacy curriculum. Pharmacy students were more complacent with the content and less with the fixed structure of the Pharmacy curriculum. Students emphasized more theoretical knowledge and less practical and transferable skills of the competencies developed over the studies. Initial student feedback on the development of CBPE in Estonia demonstrated that theoretical knowledge needs to be more integrated with practice throughout the curriculum. In the future, more attention should be paid to the development of transferable skills, including digital skills.
ABSTRACT
The prospect of creating a new medicine with psychotropic activity is shown as a result of studying the chemical composition and pharmacological activity of modified dry extracts of motherwort (Leonurus cardiaca L.) tincture. The most promising substances were the dry extracts, modified by adding small amounts of arginine, valine, phenylalanine, glycine, lysine, and alanine. A total of 15 main phenolic substances were found in the extracts, and eight of them were identified. There were also 10 hydroxycinnamic acids in these extracts, three of which were identified (chlorogenic, caffeic, and rosmarinic acids). The dominant hydroxycinnamic acids were chlorogenic and caffeic acids. Among flavonoids, catechin, hyperoside, and rutin were identified. It should be noted that the extracts had a significant content of ellagic acid. On the basis of the results of the phytochemical analysis of the extracts, it can be concluded that the composition of phenolic compounds does not differ significantly, and the main differences are related to amino acids, which obviously have an impact on the overall pharmacological effect. The results obtained indicate the presence of anxiolytic activity in the motherwort extracts studied in complex with amino acids. The extracts with glycine, valine, and arginine were more effective in reducing anxiety in animals.
ABSTRACT
The oil from the leaves of Limnocitrus littoralis (Miq.) Swingle was obtained by hydrodistillation and investigated by gas chromatography combined with mass spectrometry (GC/MS), the anti-inflammatory effect of the oil was examined on a LPS-induced RAW264.7 cells. An aggregate of forty components were identified, representing 93.0% of the oil. This oil was subjugated by monoterpene hydrocarbons (27.7%), sesquiterpene hydrocarbons (32.3%) and oxygenated sesquiterpenes (4.6%). The significant constituents of L. littoralis essential oil were determined as follows; myrcene (24.9%), γ-muurolene (11.0%), and oleic acid (10.3%). The essential oil of L. littoralis showed activity against the nitric oxide (NO) generation with the IC50 value to 12.50 ± 1.19 µg/L. The anti-inflammatory effect of essential oil from the leaves of L. littoralis is reported for the first time.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Oils, Volatile/chemistry , Oils, Volatile/pharmacology , Plant Leaves/chemistry , Rutaceae/chemistry , Acyclic Monoterpenes/pharmacology , Alkenes/pharmacology , Animals , Gas Chromatography-Mass Spectrometry , Mice , Monoterpenes/analysis , Nitric Oxide/biosynthesis , RAW 264.7 Cells , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , VietnamABSTRACT
A new flavanol derivative, (2R,3R)-3-acetoxy-7-hydroxy-3',4'-methylenedioxyflavan (1), was co-isolated from the rhizomes of Zephyranthes ajax Hort. with the following seven known compounds: 7-hydroxyflavan (2), 7,4'-dihydroxyflavan (3), 7,4'-dihydroxy-8-methylflavan (4), 7,3'-dihydroxy-4'-methoxyflavan (5), 5,4'-dihydroxy-7-methoxy-6-methylflavan (6), 7-hydroxy-3',4'-methylenedioxyflavanone (7) and haemanthamine (8). Their structures were elucidated by combining 1D-/2D-NMR, CD, UV and HRESIMS data, and comparisons with reported data in literature were made. Among these known compounds, 2, 3, 4, 6 and 7 were isolated from the genus Zephyranthes for the first time. In addition, the cytotoxicity assay indicated that compound 8 has potent cytotoxic activity against human hepatocellular carcinoma (the HepG2 cell line), human lung carcinoma (the SK-LU-1 cell line), human carcinoma in the mouth (the KB cell line), human colon carcinoma (the SW480 cell line) and human stomach gastric adenocarcinoma (the AGS cell line), with IC50 values ranging from 4.4 to 11.3 µM. This is the first study reporting the cytotoxicity of compound 8 against the SK-LU-1 cancer cell lines.