Primary care indicators for disease burden, monitoring and surveillance of COVID-19 in 31 European countries: Eurodata Study.

BACKGROUND: During the COVID-19 pandemic, the majority of patients received ambulatory treatment, highlighting the importance of primary health care (PHC). However, there is limited knowledge regarding PHC workload in Europe during this period. The utilization of COVID-19 PHC indicators could facilitate the efficient monitoring and coordination of the pandemic response. The objective of this study is to describe PHC indicators for disease surveillance and monitoring of COVID-19's impact in Europe. METHODS: Descriptive, cross-sectional study employing data obtained through a semi-structured ad hoc questionnaire, which was collectively agreed upon by all participants. The study encompasses PHC settings in 31 European countries from March 2020 to August 2021. Key-informants from each country answered the questionnaire. Main outcome: the identification of any indicator used to describe PHC COVID-19 activity. RESULTS: Out of the 31 countries surveyed, data on PHC information were obtained from 14. The principal indicators were: total number of cases within PHC (Belarus, Cyprus, Italy, Romania and Spain), number of follow-up cases (Croatia, Cyprus, Finland, Spain and Turkey), GP's COVID-19 tests referrals (Poland), proportion of COVID-19 cases among respiratory illnesses consultations (Norway and France), sick leaves issued by GPs (Romania and Spain) and examination and complementary tests (Cyprus). All COVID-19 cases were attended in PHC in Belarus and Italy. CONCLUSIONS: The COVID-19 pandemic exposes a crucial deficiency in preparedness for infectious diseases in European health systems highlighting the inconsistent recording of indicators within PHC organizations. PHC standardized indicators and public data accessibility are urgently needed, conforming the foundation for an effective European-level health services response framework against future pandemics.

Synthesis, Antimicrobial Activities, and Molecular Modeling Studies of Agents for the Sortase A Enzyme.

Sortase A (SrtA) is an attractive target for developing new anti-infective drugs that aim to interfere with essential virulence mechanisms, such as adhesion to host cells and biofilm formation. Herein, twenty hydroxy, nitro, bromo, fluoro, and methoxy substituted chalcone compounds were synthesized, antimicrobial activities and molecular modeling strategies against the SrtA enzyme were investigated. The most active compounds were found to be T2, T4, and T19 against Streptococcus mutans (S. mutans) with MIC values of 1.93, 3.8, 3.94 µg/mL, and docking scores of -6.46, -6.63, -6.73 kcal/mol, respectively. Also, these three active compounds showed better activity than the chlorohexidine (CHX) (MIC value: 4.88 µg/mL, docking score: -6.29 kcal/mol) in both in vitro and in silico. Structural stability and binding free energy analysis of S.mutans SrtA with active compounds were measured by molecular dynamic (MD) simulations throughout 100 nanoseconds (ns) time. It was observed that the stability of the critical interactions between these compounds and the target enzyme was preserved. To prove further, in vivo biological evaluation studies could be conducted for the most promising precursor compounds T2, T4, and T19, and it might open new avenues to the discovery of more potent SrtA inhibitors.

The role of primary health care in long-term care facilities during the COVID-19 pandemic in 30 European countries: a retrospective descriptive study (Eurodata study).

BACKGROUND AND AIM: Primary health care (PHC) supported long-term care facilities (LTCFs) in attending COVID-19 patients. The aim of this study is to describe the role of PHC in LTCFs in Europe during the early phase of the pandemic. METHODS: Retrospective descriptive study from 30 European countries using data from September 2020 collected with an ad hoc semi-structured questionnaire. Related variables are SARS-CoV-2 testing, contact tracing, follow-up, additional testing, and patient care. RESULTS: Twenty-six out of the 30 European countries had PHC involvement in LTCFs during the COVID-19 pandemic. PHC participated in initial medical care in 22 countries, while, in 15, PHC was responsible for SARS-CoV-2 test along with other institutions. Supervision of individuals in isolation was carried out mostly by LTCF staff, but physical examination or symptom's follow-up was performed mainly by PHC. CONCLUSION: PHC has participated in COVID-19 pandemic assistance in LTCFs in coordination with LTCF staff, public health officers, and hospitals.

Analysis of Volatile Constituent by Hydrodistillation and Solid-Phase Microextraction Techniques and Antimicrobial and Scolicidal Activities of Essential Oil and Soxhlet Extracts of Ulva rigida grown in Turkey.

In the present study, the volatile composition of Ulva rigida (U. rigida) was elucidated by two different methods. As a result of the identification process of volatile components using the GC/MS-FID instrument, 31 compounds were identified by hydrodistillation (HD) method, and 15 compounds were identified by solid-phase microextraction (SPME) method, elucidating the structure of 99.86 % and 92.65 %, respectively. The most abundant compounds in the essential oil of U. rigida were n-hexadecanoic acid and pentadecanal, while the most abundant compound according to the SPME analysis was heptadecyne, a hydrocarbon compound. In the next step, hexane, dichloromethane, chloroform and methanol solvent extracts of U. rigida were prepared and the antimicrobial activities of the extracts and the essential oil obtained by hydro-distillation as well as the scolicidal activities of the solvent extracts were determined. The results of the antimicrobial activity test of the essential oil showed a high level of activity against Bacillus cereus ATCC 10876 and MRSA. The highest activity was found on the microorganism of Pseudomonas aeruginosa ATCC 9027 in chloroform and methanol extracts of U. rigida. Furthermore, viability detection was performed and the scolicidal effects of the extracts on protoscoleces were assessed. The values of lethal concentration doses (LD50 , LD75 and LD90 ) were calculated using probit analysis.

Clinical pathway of COVID-19 patients in primary health care in 30 European countries: Eurodata study.

BACKGROUND: Most COVID-19 patients were treated in primary health care (PHC) in Europe. OBJECTIVES: To demonstrate the scope of PHC workflow during the COVID-19 pandemic emphasising similarities and differences of patient's clinical pathways in Europe. METHODS: Descriptive, cross-sectional study with data acquired through a semi-structured questionnaire in PHC in 30 European countries, created ad hoc and agreed upon among all researchers who participated in the study. GPs from each country answered the approved questionnaire. Main variable: PHC COVID-19 acute clinical pathway. All variables were collected from each country as of September 2020. RESULTS: COVID-19 clinics in PHC facilities were organised in 8/30. Case detection and testing were performed in PHC in 27/30 countries. RT-PCR and lateral flow tests were performed in PHC in 23/30, free of charge with a medical prescription. Contact tracing was performed mainly by public health authorities. Mandatory isolation ranged from 5 to 14 days. Sick leave certification was given exclusively by GPs in 21/30 countries. Patient hotels or other resources to isolate patients were available in 12/30. Follow-up to monitor the symptoms and/or new complementary tests was made mainly by phone call (27/30). Chest X-ray and phlebotomy were performed in PHC in 18/30 and 23/30 countries, respectively. Oxygen and low-molecular-weight heparin were available in PHC (21/30). CONCLUSION: In Europe PHC participated in many steps to diagnose, treat and monitor COVID-19 patients. Differences among countries might be addressed at European level for the management of future pandemics.

Phytochemicals, antimicrobial, and sporicidal activities of moss, Dicranum polysetum Sw., against certain honey bee bacterial pathogens.

Beekeeping is an important agricultural and commercial activity globally practiced. Honey bee is attacked by certain infectious pathogens. Most important brood diseases are bacterial including American Foulbrood (AFB), caused by Paenibacillus larvae (P. larvae), and European Foulbrood (EFB) by Melissococcus plutonius (M. plutonius) in addition of secondary invaders, e.g. Paenibacillus alvei (P. alvei) and Paenibacillus dendritiformis (P. dendritiformis). These bacteria cause the death of larvae in honey bee colonies. In this work, antibacterial activities of extracts, fractions, and isolated certain compounds (nominated 1-3) all originated from moss, Dicranum polysetum Sw. ( D. polysetum), were tested against some honey bee bacterial pathogens. Minimum inhibitory concentration, minimum bactericidal concentration, and sporicidal values ​​of methanol extract, ethyl acetate, and n-hexane fractions ranged between 10.4 and 18.98, 83.4-303.75 & 5.86-18.98 µg/mL against P. larvae, respectively. Antimicrobial activities of the ethyl acetate sub-fractions (fraction) and the isolated compounds (1-3) were tested against AFB- and EFB-causing bacteria. Bio-guided chromatographic separation of ethyl acetate fraction, a crude methanolic extract obtained from aerial parts of D. polysetum resulted in three natural compounds: a novel one, i.e. glycer-2-yl hexadeca-4-yne-7Z,10Z,13Z-trienoate (1, dicrapolysetoate; given as trivial name), in addition to two known triterpenoids poriferasterol (2), and γ-taraxasterol (3). Minimum inhibitory concentration ranges were 1.4-60.75, 8.12-65.0, 2.09-33.44 & 1.8-28.75 µg/mL for sub-fractions, compounds 1, 2, and 3, respectively.

Dihydroisocoumarins and Phenylglycosides from Scorzonera longiana, Their Antimicrobial Activities and Molecular Docking Studies.

Five new phenyl dihydroisocoumarin glycosides (1-5) and two known compounds (6-7) were identified from the butanol fraction of Scorzonera longiana. The structures of 1-7 were elucidated based on spectroscopic methods. Antimicrobial, antitubercular, and antifungal evaluation of compounds 1-7 were carried out using the microdilution method against nine microorganisms. Compound 1 was active only against Mycobacterium smegmatis (Ms) with a MIC value of 14.84 µg/mL. All tested compounds (1-7) were active against Ms but only compounds 3-7 were active against fungi (C. albicans, S. cerevisiae) with MIC values of 25.0-125 µg/mL. In addition, molecular docking studies were conducted against Ms DprE1 (PDB ID: 4F4Q), Mycobacterium tuberculosis (Mbt) DprE1 (PDB ID: 6HEZ), and arabinosyltransferase C (EmbC, PDB ID: 7BVE) enzymes. Compounds 2, 5, and 7 are the most effective Ms 4F4Q inhibitors. Compound 4 was the most promising inhibitory activity on Mbt DprE with the lowest binding energy of -9,9 kcal/mol.

Two new dihydroisocoumarins and terpenoids from Scorzonera longiana Sümbül an endemic species to Turkey and their antimicrobial activity.

Two new dihydroisocoumarins (scorzolongin I (1), and scorzolongin II (2)) and nine known compounds (3',5'-dimethoxy hydrangenol (scorzolongin III, 3), cladantholide (4), dammar-24-ene-3ß-ol (5), taraxasterol (6), ß-sitosterol (7), mangifgerursanone (8), and a mixture of α-amyrenone (9a), ß-amyrenone (9b), and dammar-24-ene-3-one (9c) in about 1:1:2 ratio) were identified from the dichloromethane fraction of Scorzonera longiana. The structure of all compounds (1-9a-c) were elucidated by extensive 1D and 2D NMR (1H, 13C/APT, COSY, HMBC, HSQC, and NOESY) spectroscopy, UV, FT-IR, and LC-QTOF-MS data and by comparison of their NMR data with the literature. These compounds have been isolated from S. longiana for the first time. An antimicrobial assay against eight microorganisms was applied to isolated compounds 1-3. Scorzolongin I, and scorzolongin II, and scorzolongin III showed notable activity against gram (-) (Escherichia coli and Yersinia pseudotuberculosis) and fungi (Candida albicans, Saccharomyces cerevisiae) with 20 mm inhibition zone each. Scorzolongin II (2) exhibited strong activity against E. coli, Y. pseudotuberculosis, Mycobacterium smegmatis C. albicans, S. cerevisiae with MIC value of 33.8 µg/mL.

Biological Activity and Phytochemical Analysis of Dicranum scoparium against the Bacterial Disease for Honey Bee.

Bacterial diseases, such as American Foulbrood (AFB) and European Foulbrood (EFB), are known to have catastrophic effects on honey bees (if left to spread, can wipe out entire colonies), leading to severe financial losses in the beekeeping industry. The aim of this study was to evaluate the pharmacological properties of methanol extract and its fractions (ethyl acetate, hexane, water) derived from Dicranum scoparium Hedw., which could be utilized as a potential drug to prevent the bacterial diseases (AFB and EFB) affecting the honey bees. For this purpose, crude methanol extract and ethyl acetate/hexane/water fractions were prepared from the aerial part of D. scoparium, collected from Trabzon province. Bio-guided fractionation of the extract and its fractions led to the first-time isolation of five compounds. The structure of all compounds was elucidated by nuclear magnetic resonance (NMR) spectroscopy, ultraviolet (UV) spectral analysis, Fourier-transform infrared spectroscopy (FT-IR), liquid chromatography quadrupole time-of-flight mass spectroscopy (LC-QToF-MS), and by comparison of their NMR data with that of literature. The analysis of these compounds revealed significant antibacterial and sporicidal activities against bacteria causing larval diseases in honey bees. The antibacterial activity of these compounds ranged from 0.6 to 60 µg/mL against AFB and EFB causing bacteria. Therefore, the natural raw extract and fractions of D. scoparium could be used as potential therapeutic agents against bacterial agents affecting honey bees.

Antimicrobial and lipase inhibition of essential oil and solvent extracts of Cota tinctoria var. tinctoria and characterization of the essential oil.

The essential oil (EO) of Cota tinctoria var. tinctoria was analyzed using GC-FID / MS. A total of 51 compounds were determined from this taxon, accounting for 99.79% in hydrodistillation. Monoterpenes were the primary chemical class for the volatile organic compounds in the EO (36.1%, 13 compounds). Borneol (18.1%), camphor (14.9%), and ß-pinene (11.3%) were the major components in the EO of C. tinctoria var. tinctoria. The antimicrobial activities of EO and n-hexane, acetonitrile, methanol, and water solvent extracts of the taxon were screened in vitro against ten microorganisms. The EO yielded the best activity (15 mm, 372.5 MIC, 59600 µg/µL) against Mycobacterium smegmatis. The acetonitrile extract was the most active against the Staphylococcus aureus and Bacillus cereus with 274 µg/mL MIC value. IC50 values for the lipase enzyme inhibitory activity of EO and solvent extracts (n-hexane, acetonitrile, methanol, and water) were found to be 59.80 ± 4.3285 µg/mL 68.28 ± 3.1215 µg/mL, 52.60 ± 3.7526 µg/mL, 48.73 ± 2.8265 µg/mL, and 99.50 ± 5.5678 µg/mL, respectively.

Irregularity in Plantar Fascia, Muscle Edema and Tendon Thickness in Patients with High-Risk for Diabetic Foot.

AIM: To investigate the alterations in the plantar fascia (PF), intrinsic muscles, and tendons in the feet of patients at high risk for developing diabetic foot. METHODS: The healthy feet of 22 patients with type 2 diabetes, who had developed diabetic foot ulcers on a single foot without any pathology on the contralateral extremity, and those of 22 healthy volunteers were evaluated by magnetic resonance imaging. The volume of the Achilles tendon (AT), the surface area of the PF, the thickness of AT, flexor hallucis longus, flexor digitorum longus, tibialis posterior, and peroneus longus tendons, irregularity in the PF, and edema of intrinsic foot muscles were examined. RESULTS: Nineteen patients (86%) had irregularity in the PF, whereas none of the healthy controls had any (p<0.001). Intrinsic muscle edema was more common in the group with diabetes (p=0.006). The volume of AT and the surface area of PF were decreased in patients with peripheral arterial disease (PAD) (p<0.05). Patients with diabetes mellitus but without PAD had a larger surface area of PF than that of controls (p<0.05). There were no differences in the volume of AT, the surface area of the PF, and other tendon thickness between the groups. CONCLUSION: Irregularity in the PF and muscle edema may indicate a high risk for the diabetic foot. The presence of PAD may lead to regression in the structure of AT and PF.

Chemical Variation, Antimicrobial, Nitric Oxide Scavenging Activities and Tyrosinase Inhibition of Essential Oils and Solvent Extracts from Filipendula vulgaris Moench Growing in Turkey.

Volatile organic compositions of the essential oils (EOs), solid-phase microextraction (SPME) and SPME of n-hexane extracts from the flower and stem-leaf of Filipendula vulgaris (F. vulgaris) were analyzed by GC-FID/MS. A total of 107 constituents were characterized, flower and stem-leaf parts of the plant were found to contain different volatile organic compounds. Tricosane (29.6%), n-nonanal (20.5%) were identified as the main components in the essential oil of the flower, while phytol (35.2%) was found to be a major constituent in the essential oil of stem-leaf. Benzaldehyde (56.0%) and n-nonanal (31.6%) were the major groups in the SPME of stem-leaf and flower, respectively. The volatiles for the SPME of n-hexane extracts of the flower and stem-leaf of F. vulgaris were predominated by aromatic compounds (75.0% and 78.5%) and ketones (18.1% and 10.1%), respectively. On the other hand, a total of terpene compounds was found at the most in the EO of the stem-leaf part of the plant (48.6%). In addition, antimicrobial, tyrosinase inhibition, and nitric oxide scavenging activities of the n-hexane (H), methanol (M), aqueous extracts (A) and EOs of F. vulgaris were investigated. EOs and methanol extracts of flower and stem-leaf had high antimicrobial activity against tested various microorganisms. However, n-hexane extracts of the flower and stem-leaf only displayed activity against Mycobacterium smegmatis. Methanol extracts of flower and stem-leaf possessed the best tyrosine inhibition and NO scavenging activity.

Anti-inflammatory secondary metabolites from Scrophularia kotschyana.

The species belonging to Scrophularia genus grow mainly in Irano-Turanian and Mediterranean regions and have been used as folk remedy for inflammatory-related diseases since ancient times. The present study was aimed to evaluate the anti-inflammatory activity of the extracts of Scrophularia kotschyana as well as the isolated compounds. The aerial parts and the roots of the plant were separately extracted with methanol. Anti-inflammatory activities of both extracts were evaluated with formalin test in mice. As the methanolic extract of the aerial parts significantly (p < .05) inhibited inflammation, it was then submitted to successive solvent extractions with n-hexane, dichloromethane, ethyl acetate and n-butanol to yield subextracts. Anti-inflammatory activities of the subextracts were evaluated within the same test system. Among the subextracts tested, the n-butanol subextract produced a significant (p < .05) anti-inflammatory activity at all doses (5, 10, and 30 mg/kg, ip.). Sequential chromatographic separation of the n-butanol subextract yielded 8-O-acetyl-4'-O-(E)-p-coumaroylharpagide, 8-O-acetyl-4'-O-(Z)-p-coumaroylharpagide, ß-sitosterol 3-O-ß-glucopyranoside, apigenin 7-O-ß-glucopyranoside, apigenin 7-O-rutinoside, luteolin 7-O-ß-glucopyranoside and luteolin 7-O-rutinoside. The anti-inflammatory activities of the isolates were evaluated at 5 mg/kg dose. Luteolin 7-O-ß-glucopyranoside and apigenin 7-O-rutinoside caused a significant (p < .05) inhibition of oedema formation.

Attitudes of a geriatric population towards risks about COVID-19 pandemic: in the context of anxiety and depression.

BACKGROUND: A curfew for elderly people was announced in Turkey to protect the geriatric population during the COVID-19 pandemic. Although this may have the beneficial effect of preventing infection, psychological distress may also increase with prolongation of the pandemic. METHODS: Geriatric patients were interviewed by telephone due to the ongoing curfew. Demographical characteristics, comorbidities, personal risk perception of COVID-19, common concerns related to COVID-19, and experiences of delayed hospital admission due to the pandemic were recorded. The Hospital Anxiety and Depression Scale (HADS) was used to assess psychological distress, anxiety, and depression. RESULTS: Participants (n = 136; 82 females, 60.3%) had a mean age of 73.4 ± 5.9 years. The most common comorbidity was hypertension (75%). Approximately 80% of the participants reported a decrease in physical activity during the curfew period. The HADS scores indicated rates of anxiety as 25.7% and depression as 16.9%. Anxiety was significantly more common in females than males (P = 0.002). Sleep problems (P = 0.000), fatigue (P = 0.000), and hopelessness (P = 0.000) were more common in participants with depression and anxiety. Logistic regression analyses showed an association between a delay in hospital admission and the presence of depression (P = 0.0029, R2  = 0.146). Personal risk perception of COVID-19 was statistically significantly higher among patients with anxiety (P = 0.0027, R2  = 0.157). CONCLUSION: Decreased adaptation to external and internal factors among older individuals may facilitate unfavourable outcomes of the pandemic. These results indicate that the geriatric population was mentally and physically affected by the restrictions and isolation.

The effectiveness of an exercise intervention in reducing the severity of postpartum depression: A randomized controlled trial.

PURPOSE: This study aims to identify the effectiveness of an exercise program in reducing the severity of postnatal depression in women who had a spontaneous vaginal delivery. DESIGN AND METHODS: This randomized control trial was conducted with 65 postpartum women residing in a city located in south-eastern Turkey. In the first postpartum month, following random assignment of subjects, the experimental group (n = 40) performed exercises for 4 weeks, and the control group (n = 40) received standard care. The participating women were administered the Edinburgh postpartum depression scale. FINDINGS: The average age of the participants was 28.90 ± 4.83 (min:19, max:40). Pretest mean depression scores of the exercises (16.41 ± 1.61) and control group (15.74 ± 2.35) were found to be similar, and there were no statistically significant differences (P > .05). After the 4-week exercise program, a statistically significant difference was found between the posttest mean scores of the exercises (7.29 ± 1.67) and control (12.54 ± 2.65) group participants. Pretest mean scores were found to be similar, and there were no statistically significant differences (Z = -6.501, P = .001). CONCLUSION: The 4-week exercise program was found to be an effective method in decreasing the severity of depressive symptoms experienced in the postpartum period. Nurses and midwives providing care in the postpartum period are recommended to provide women in this period with exercise training. PRACTICE IMPLICATIONS: Postpartum depression is a specific psychological disorder in which preventive interventions might lead to dramatic benefits. Exercises done in the postpartum period are reported to enable psychosocial well-being, less anxiety, and depression.

The Volatile Chemical Compositions of the Essential Oil/SPME and Enzyme Inhibitory and Radical Scavenging Activities of Solvent Extracts and the Essential oils from Coronilla orientalis Miller and C. varia L. grows in Turkey.

The volatile organic compounds (VOCs) of two Coronilla species (Coronilla orientalis Miller and Coronilla varia L.) obtained by hydrodistillation (HD) and solid phase microextraction (SPME) techniques were identified by GC-FID/MS. The major compounds identified in the SPME extracts were limonene (43.4%) in Coronilla orientalis (C. orientalis), (Z)-ß-ocimene and (E)-ß-ocimene (34.3% and 32.4%) in Coronilla varia (C. varia), whereas, the essential oils of C. orientalis and C. varia were rich with γ-terpinene (22.4%) and phytol (30.7%), respectively. In addition, acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), tyrosinase, α-glucosidase enzyme inhibitory, and radical scavenging activities (DPPH) of chloroform, ethyl acetate, methanol, and water extracts, and also essential oils obtained from C. orientalis and C. varia were investigated. The tyrosinase activity was studied at the doses of 25 µg/mL, 50 µg/mL and 100 µg/mL. Tyrosinase inhibition percentage was observed to increase by dose and methanol extracts of the both species were found to have the highest activity. Essential oils of the both species were found to have significant acetylcholinesterase and butyrylcholinesterase inhibition activities. α-Glucosidase enzyme inhibition of the ethyl acetate and water extracts of C. orientalis was determined as 80.11 ± 4.07% and 80.32 ± 3.47% at the 100 µg/mL concentration, respectively. Essential oils, chloroform, ethyl acetate, methanol, and water extracts were determined to have moderate DPPH radical scavenging activities.

α-Glucosidase inhibitory effects of polyphenols from Geranium asphodeloides: Inhibition kinetics and mechanistic insights through in vitro and in silico studies.

Some Geranium species have been used to treat diabetes. To evaluate the scientific basis of this ethnopharmacological use, we aimed to isolate potent α-glucosidase inhibitory metabolites of Geranium asphodeloides Burm. through in vitro bioactivity-guided fractionation. All the tested extracts showed high α-glucosidase inhibitory effect compared to acarbose. Among the tested extracts, the ethyl acetate subextract showed the highest activity with an IC50 value of 0.85 ±â€¯0.01 µM. A hydrolysable tannin, 1,2,4-tri-O-galloyl-ß-d-glucopyranose (1), and five flavonoid glycosides, kaempferol-3-O-α-rhamnopyranoside (2), kaempferol-3-O-α-arabinofuranoside (3), quercetin-3-O-ß-glucopyranoside (4), quercetin-3-O-α-rhamnopyranoside (5), and quercetin-3-O-α-rhamnofuranoside (6), were isolated from the ethyl acetate subextract. Their structures were identified by 1D- and 2D-NMR experiments. 1 exhibited the highest α-glucosidase inhibitory effect, approximately 61 times more potent than positive control, acarbose, with an IC50 value of 0.95 ±â€¯0.07 µM. Also, 2 was more potent than acarbose. An enzyme kinetics analysis revealed that compounds 2, 3 and 4 were competitive, whereas 1 and 6 uncompetitive inhibitors. Molecular docking studies were performed to get insights into inhibition mechanisms of the isolated compounds in the light of the enzyme kinetic studies using various binding sites of the enzyme model.

In Vitro Protection by Crataegus microphylla Extracts Against Oxidative Damage and Enzyme Inhibition Effects.

OBJECTIVES: Crataegus species have been used as food and also in folk medicine for the treatment of various diseases. The present study aimed to make investigations on the biologic properties of different extracts prepared from Crataegus microphylla C. Koch, which was collected from Turkey. MATERIALS AND METHODS: Dried leaf, stem bark, and fresh fruit samples of C. microphylla were separated and ethanol extract, acidified (0.5% HCl, pH: 2.5) ethanol extract, ethanol:water (1:1) extract, methanol extract, acidified (0.5% HCl, pH: 2.5) methanol extract, methanol:water (1:1) extract, water extract, and acidified (0.5% HCl, pH: 2.5) water extract were prepared for each. Various biologic effects such as the prevention of oxidative DNA damage, acetylcholinesterase, tyrosinase, α-glucosidase inhibition, and antioxidant effects with 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, PRAP, and FRAP assays of these extracts at different concentrations were studied. RESULTS: Acidified methanol extract of stem barks exhibited the highest acetylcholinesterase and tyrosinase inhibitions among the other extracts with IC50 values of 204.02±0.95 µg/mL and 37.30±0.27 µg/mL, respectively. Acidified ethanol extract of leaves was the most efficient extract against α-glucosidase, giving an IC50 of 15.78±0.14 µg/mL. The IC50 value of the acidified ethanol extract for DPPH was 9.89±0.09 µg/mL. Methanol extracts of leaves and stem barks at the dose of 125 µg/mL exhibited significant protective activity against DNA strand scission by hydroxyl radicals (.OH) on supercoiled pBR322 DNA. CONCLUSION: Acidified methanol or ethanol extracts prepared with stem bark and leaf from C. microphylla have potential antioxidant, hypoglycemic, and neuroprotective effects.

Evaluation of in vivo analgesic activity of Scrophularia kotscyhana and isolation of bioactive compounds through activity-guided fractionation.

The present study was undertaken to evaluate the in vivo analgesic activities of the extracts prepared from the aerial parts and roots of Scrophularia kotscyhana and to isolate the bioactive metabolites from the most active extract. Analgesic activities of all extracts and subextracts at the doses of 5, 10 and 30 mg/kg (i.p.) were examined using hot plate test in mice. Among the tested extracts, MeOH extract prepared from the aerial parts and the n-butanol subextract prepared thereof displayed the best analgesic activity at all doses. Phytochemical studies on n-butanol subextract led to the isolation of two new iridoid glycosides as an inseparable mixture, 8-O-acetyl-4'-O-(E)-(p-coumaroyl)-harpagide (1) and 8-O-acetyl-4'-O-(Z)-(p-coumaroyl)-harpagide (2) along with five known secondary metabolites, ß-sitosterol 3-O-ß-glucopyranoside (3), apigenin 7-O-ß-glucopyranoside (4), apigenin 7-O-rutinoside (5), luteolin 7-O-ß-glucopyranoside (6) and luteolin 7-O-rutinoside (7). The iridoid mixture (1 and 2), 3 and 4 elicited significant inhibition of pain at 5 mg/kg dose.