Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives

The 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC50 values 263±0.3 and 456±0.1, respectively.

Changes in thyroid function status of suicidal patients

Abstract Background This study was carried out at Punjab Institute of Mental Health and Centre for Nuclear Medicine Mayo Hospital, Lahore. It is aimed at the possible association of thyroid malfunctioning with suicide attempts of patients. Objective Determination of thyroid function status of suicidal psychiatric patients and their comparison with psychiatric patients without suicide attempt or ideation. Methods Total 54 patients with either past history of suicide attempt or current suicidal ideation were selected for analysis of their thyroid function status (age 15-55 years). Age matched 50 non-suicide psychiatric patients were included for comparison. Results Two patients with suicide attempt had overt thyroid dysfunction. Remaining patients had serum FT4, FT3 and TSH level within normal range. Suicide attempter patients had lower FT4 but increased FT3 and TSH levels compared to suicidal ideation patients. Serum FT4 and TSH levels in suicidal patients were not different from psychiatric patients. Serum FT3 in suicidal patients was lower than psychiatric patients (3.7 ± 0.8 vs. 4.3 ± 0.5; p < 0.05). Female suicidal patients had lower FT3 levels compared to male patients (3.4 ± 0.6 vs. 3.9 ± 0.8 pmol/L; p < 0.05). Discussion Local suicidal patients have higher incidence of overt thyroid disorder and lower FT3 levels compared to non-suicidal psychiatric patients.

Sedative and antinociceptive activities of two new sesquiterpenes isolated from Ricinus communis / 中国天然药物

Two new sesquiterpenes, trivially named ricinusoids A (1) and ricinusoids B (2), were isolated from ethyl acetate fraction of Ricinus communis. The structures of new compounds were elucidated by detailed spectroscopic techniques, including 1D- and 2D-NMR, UV, IR spectroscopy, and mass spectrometry. The compounds (1-2) were also assessed for in-vivo sedative and analgesic like effects in open field and acetic acid induced writhing tests respectively at 5, 10, and 20 mg·kg i.p. Pretreatment of both test compounds caused significant (P ≤ 0.05) reduction in locomotive activity like sedative agents and abdominal constrictions like analgesics. Both compounds (1-2) possessed marked sedative and antinociceptive effects in animal models.

Sedative and antinociceptive activities of two new sesquiterpenes isolated from Ricinus communis / 中国天然药物

Two new sesquiterpenes, trivially named ricinusoids A (1) and ricinusoids B (2), were isolated from ethyl acetate fraction of Ricinus communis. The structures of new compounds were elucidated by detailed spectroscopic techniques, including 1D- and 2D-NMR, UV, IR spectroscopy, and mass spectrometry. The compounds (1-2) were also assessed for in-vivo sedative and analgesic like effects in open field and acetic acid induced writhing tests respectively at 5, 10, and 20 mg·kg i.p. Pretreatment of both test compounds caused significant (P ≤ 0.05) reduction in locomotive activity like sedative agents and abdominal constrictions like analgesics. Both compounds (1-2) possessed marked sedative and antinociceptive effects in animal models.

Evaluation and assessment of prescribing patterns in elderly patients using two explicit criteria based screening tools: [the priscus list and stopp/start criteria]

Background and Objectives: Rational prescribing can prevent medication errors and the associated harm, especially in old age patients, as they are being frequently prescribed with drugs for various ailments .Moreover, polypharmacy is a common practice in them. Therefore, a significant threat of potential drug interactions and adverse effects exist. Current study focuses on assessment of Potentially Inappropriate Medication [PIM] in medication prescribed to old age patients

Methods: It was a forty days, descriptive and observational study conducted from August 15th 2017 to September 25th 2017 in which prescriptions given to elderly patients were reimbursed for collecting various sets of information. In order to assess PIMs [in Pakistani Set-up], STOPP/START addition 2008 [including examples of misprescribing, overprescribing and under prescribing] and the PRISCUS list [misprescribing and overprescribing] was used. Statistical analysis of results was performed using SPSS version 20

Results: One hundred forty six cases of PIMs [including incorrect prescribing, overprescribing and under prescribing] were detected. It included incorrect prescriptions 104, under prescription 28 and over prescriptions 14. NSAIDS accounted for most incorrect prescriptions followed by benzodiazepines. Mostly NSAIDS were used for myalgia, backache and rheumatoid disorders

Conclusion: Current findings highlighted Potentially Inappropriate Prescribing [PIP], particularly of NSAIDs and under prescribing of statins in cardiovascular diseases. Study findings suggest introducing pertinent interventions at the stages involved in prescribing, prescription review and its follow up to reduce the PIP and PIMs

Bioassay-guided isolation of novel and selective urease inhibitors from Diospyros lotus / 中国天然药物

Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-I, carbonic anhydrase-II and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 µmol·L, respectively, using thiourea (IC = 21 ± 0.11 µmol·L) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.

Three new anthraquinone derivatives isolated from Symplocos racemosa and their antibiofilm activity / 中国天然药物

Three new alkyl substituted anthraquinone derivatives, trivially named as symploquinones A-C (Compounds 1-3) were isolated from Symplocos racemosa. The structures of these compounds were determined on the basis of extensive spectroscopic analyses (UV, IR, Mass, H- and C-NMR, and two-dimensional (2D) NMR techniques). The resulting data were also compared with the reported literature. These compounds were then subjected to antibacterial or antibiofilm testing. Compounds 1 and 3 exhibited good antibacterial activity in the concentration range of 160-83 μg·mL against Streptococcus mutans, methicillin resistant Staphylococcus aureus and Proteus mirabilis. Both compounds were further screened for anti-biofilm activity, which revealed promising activities at sub-MIC concentrations. None of the compounds were found to be active against Klebsiella pneumoniae.

Triterpenes and steroids from euphorbia denticulata lam. with anti-herpes symplex virus activity

In this research, dried acetoneichloroform extract of aerial parts of E. denticulata as one of the endemic plants to Iran, afforded a number of triterpenes and steroids including: betulin, 24-methylene-cycloart-3-ol, cycloart-23Z-ene-3beta,25-diol, cycloart-23E-ene-3beta,25-diol, ergosta-8,24-dien-3-ol [obtusifoliol] and beta-sitosterol which were reported for the first time from this plant. The structure of these compounds was elucidated by NMR and mass spectroscopic methods. The MTS assay was used to determine the toxicity and antiviral activity of betulin and [3/beta,23E]-cycloarta-23-ene-3,25-diol. Betulin showed anti-HSV-1 activity with EC50 value of 84.37 +/- 0.02 microg/mL, and toxicity on normal vero cells with CC50 value of 660.718 +/- 0.072 microg/mL. [3beta,23E]-Cycloarta-23-ene-3,25-diol showed antiviral effect with EC50 value of 86.63 +/- 0.03 microg/mL, and toxicity with CC50 value of 1089.2 H0.25 microg/mL. The results revealed that these two compounds have the antiviral activity far below the CC50 value with selectivity index [CC50/EC50] values of 7.83, and 12.57, respectively

Frequency, etiology and characterstics of zygomatic complex fractures

Objective of this study was to find out the frequency, etiology and characteristics of zygomatic complex [ZMC] fractures. Forty patients with ZMC fracture visiting Oral and Maxillofacial Surgery Department, Ayub Teaching Hospital, Abbottabad from 27[th] January 2006 to 16[th] June 2006 were included in the study. A detailed history of patients was taken to find out the etiology, followed by clinical and radiographic examination to find out the characteristics of ZMC fractures. There were 31[77.5%] male and 9 [22.5%] female patients. The most common cause of ZMC fractures was Road Traffic Accident [RTA] 17[42.5%] followed by fall 8[20%], Firearm injury [FM] 5[12.5%], earthquake injury [EQI] 4[10%], interpersonal violence [IPV] 3 [7.5%], sports injury 2 [5%] and explosion [EXP] 1 [2.5%]. The most common characteristic of ZMC fracture in this study was periorbital ecchymosis 13 [32.5%] followed by paresthesia 8 [20%], flattening of cheek 6 [15%], subconjunctival ecchymosis 5 [12.5%], epistaxis 5 [12.5%], pain 5 [12.5%], step deformity of orbital margins 4 [10%], trismnus 3 [7.5%], diplopia 3 [7.5%] and buccal sulcus ecchymosis 2 [5%]

Positive end expiratory pressure [PEEP]; comparison different values during one lung ventilation, for its effects on blood arterial oxygenation and carbon dioxide levels

Thoracic surgeries and aesthesia for lung resection has presented anaesthesiologists with certain unique physiological problems. These include placing [lateral decubitus position] in order to obtain optimal access for most operations on lungs, pleura, esophagus, and great vessels, opening the chest wall [open pneumothorax] and one lung ventilation anaesthesia. One lung ventilation anaesthesia and lateral decubitus position produces decrease in functional residual capacity and an obligatory right to left shunt that ranges from 15% to 40% leading to increase in ventilation perfusion [V/Q] mismatch thus causing hypoxia and or hypoxemia. An optimal level of positive end expiratory pressure of 5cmH O when added to dependent lung is known to improve arterial oxygenation and improve ventilator 2 efficiency. To compare different values of positive end expiratory pressure [PEEP] during one lung ventilation, for its effects on blood arterial oxygenation and carbon dioxide levels. Study Randomized controlled trial [RCT]. Conducted in surgical Unit-III and Department of anaesthesia and Intensive Care, Combined Military Hospital, Rawalpindi. Duration of study with dates: Ten months from 25-12-2008 to 01-10-2009, Additional quantum of Data was collected from 01-01-2011 to 25-01-2011. The patients were divided into two equal groups of 100 patients each, by random allocation of patients to either in-group A [subjected to zero PEEP] or group-B [subjected to PEEP 5cm of water]. At induction and start of two lung ventilation 14 [14.0%] of the patients from group-A and 16 [16.0%] from group-B had normal PaCO. At initiation of one lung ventilation 25 [25.0%] of the patients from group-A and 80 [80.0%] from group-2 B had normal PaO. At initiation of one lung ventilation 26 [26.0%] of the patients from group-A and 80 [80.0%] from group-B had normal PaCO 2 2 with p<0.001. At end of procedure one lung ventilation 30 [30.0%] of the patients from group-A and 90 [90.0%] from group-B had normal PaO. 2 At end of procedure one lung ventilation 32 [32.0%] of the patients from group-A and 91 [91.0%] from group-B had normal PaCO. 2 The execution of one-lung ventilation still constitutes a challenge in clinical and surgical practice

Frequency of unerupted mandibular third molar in mandibular angle fractures

Fractures of the mandibular angle are common and comprise 31% of all mandibular fractures. Multiple recent studies report a 2-3 fold increased risk for mandibular angle fractures when un-erupted mandibular third molars are present. The objective of this study was to assess the frequency of un-erupted mandibular third molar in mandibular angle fractures. This crosssectional study was conducted at the Department of Oral and Maxillofacial Surgery, Ayub Medical College, Abbottabad from April to October 2009. One hundred and two patients were included both from the outdoor and ward on consecutive non-probability sampling base. Data were recorded on a structured Performa and analysed using SPSS-16. A hemi-mandible containing un-erupted mandibular third molar was seen to have a 1.41 times the risk of mandibular angle fracture then a hemi-mandible containing an erupted mandibular third molar. The presence of unerupted mandibular third molar is associated with an increased risk for mandibular angle fracture.