cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.7420151.v1
title: Synthesis and in vitro anti-HIV-1 evaluation of some N-arylsulfonyl-3-formylindoles

description: As our ongoing work on research of anti-HIV-1 inhibitors, fifteen N-arylsulfonyl-3-formylindoles (3a-o) were designed and prepared through two step synthetic route. Firstly, 3-formylindoles (2a-c) were synthesized via the Vilsmeier-Haack reaction. Subsequently, treatment of 2a-c with the appropriate arylsulfonyl chlorides led to the corresponding target compounds in excellent yields. All analogues were also preliminary evaluated in vitro for their inhibitory activity against HIV-1 replication. Among of all the reported analogues, three compounds 3c, 3g and 3i displayed significant anti-HIV-1 activity, with EC50 values of 9.57, 11.04 and 5.02 μM, and TI values of 31.89, 13.79 and 81.69, respectively. N-m-nitrophenylsulfonyl-3-formylindole (3c) and N-m-nitrophenylsulfonyl-6-methyl-3-formylindole (3i) especially exhibited the best promising anti-HIV-1 activity. In addition, it demonstrated that insertion of a methyl group at the C-6 position of the indolyl ring and a nitro group at the meta position of the arylsulfonyl ring, as in compound 3i, resulted in both low cytotoxicity (CC50= 410.41 μM) and good antiviral activity.
DOI: 10.6084/m9.figshare.7420139.v1
title: A study of the phytotoxic effects of the aerial parts of Senecio westermanii Dusén (Asteraceae) on Lactuca sativa L. and Allium cepa L. seeds

description: The objective of this study was to evaluate the effects of the ethanolic crude extracts and fractions of the species Senecio westermanii Dusén on Lactuca sativa L. (lettuce) and Allium cepa L. (onion) seeds. We assessed the germination, growth, root respiration and photosynthesis of the target species in Petri dishes (9.0 cm diameter) containing filter paper n°6. The study was conducted using 50 seeds per plate and held in 4 replicates per concentration of each sample. In the germination there was an inhibitory effect of fractions hexane (FH) and chloroform (FCl) at concentrations of 500 and 1000 µg/mL. There was a reduction in the radicle growth of lettuce by 14 to 24% and a reduction of hypocotilum by 14 to 28%. As for the radicle of the onion was up 74% reduction to the FCl and the coleoptile was 24 and 45% reduction for FH and FCl, respectively. Inhibitory effects in the root respiration of lettuce were detected in all the samples analyzed, with results ranging from 16 to 83%. For the seeds of A. cepa, there was an encouragement for the FCl and ethyl acetate fractions (FAE), with results ranging from 94 to 142% and 76 to 150%, respectively. With regard to the photosynthesis of L. sativa, there was no significant difference between the control, and as for the A. cepa, there was a strain in inhibition concentrations of 250 and 500 µg/mL, which ranged from 27 to 68%. The samples of S. westermanii caused changes in the target species and thus can be used as a natural herbicide.
DOI: 10.6084/m9.figshare.7420148
title: 6 weeks consumption of pure fresh coconut milk caused up-regulation of eNOS and CSE protein expression in middle-aged male rats

description: Coconut milk (CCM) has been an important cooking ingredient in the Asia-Pacific region since ancient time. Due to its high content of saturated fatty acids, it has been considered atherogenic. We have tested if chronic consumption of fresh coconut milk by middle-aged male rat affects vascular function, plasma glucose and lipid profiles. Compared to control, CCM caused lower maximal contraction to phenylephrine of thoracic aortic rings and increased relaxation to acetylcholine that was abolished by N G-nitro-L-arginine (L-NA) or disruption of the endothelium. DL-propargylglycine caused slight increase in baseline tension of L-NA treated aortic rings of CCM-treated rats and produced higher contractile response of the aortic rings to low concentrations of phenylephrine. The aortic eNOS- and cystathionine-γ-lyase(CSE) proteins expression of the CCM-treated rats were also higher than in controls. Except for lower fasting plasma glucose there were no changes in blood chemistry for the CCM treated rats. CCM consumption caused up-regulation of eNOS and CSE protein expression which resulted in increased production of NO and H2S from the blood vessels with attenuation of vasocontraction to phenylephrine and increased relaxation to acetylcholine. These novel benefits may be expected to reduce the development of cardiovascular risk factors in the aging rat.
DOI: 10.6084/m9.figshare.7420148.v1
title: 6 weeks consumption of pure fresh coconut milk caused up-regulation of eNOS and CSE protein expression in middle-aged male rats

description: Coconut milk (CCM) has been an important cooking ingredient in the Asia-Pacific region since ancient time. Due to its high content of saturated fatty acids, it has been considered atherogenic. We have tested if chronic consumption of fresh coconut milk by middle-aged male rat affects vascular function, plasma glucose and lipid profiles. Compared to control, CCM caused lower maximal contraction to phenylephrine of thoracic aortic rings and increased relaxation to acetylcholine that was abolished by N G-nitro-L-arginine (L-NA) or disruption of the endothelium. DL-propargylglycine caused slight increase in baseline tension of L-NA treated aortic rings of CCM-treated rats and produced higher contractile response of the aortic rings to low concentrations of phenylephrine. The aortic eNOS- and cystathionine-γ-lyase(CSE) proteins expression of the CCM-treated rats were also higher than in controls. Except for lower fasting plasma glucose there were no changes in blood chemistry for the CCM treated rats. CCM consumption caused up-regulation of eNOS and CSE protein expression which resulted in increased production of NO and H2S from the blood vessels with attenuation of vasocontraction to phenylephrine and increased relaxation to acetylcholine. These novel benefits may be expected to reduce the development of cardiovascular risk factors in the aging rat.
DOI: 10.6084/m9.figshare.20039311
title: Preparation and in vitro & in vivo evaluation of cephalexin matrix tablets

description: The purpose of the study is to develop cephalexin controlled-release matrix tablets by using lower proportions of release retardant polymer and to establish their in vitro & in vivo correlation. Tablets were compressed by incorporating polymers in a matrix form along with drug which prolong the drug release. Twelve formulations were prepared by mixing ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) (three different viscosity grades) in various proportions. F-1 to F-4 formulations were prepared by incorporating drug, HPMC K4M and ethyl cellulose in 100 : 5 : 5, 100 : 10 : 5, 100 : 15 : 5 and 100 : 20 : 5; similarly, F-5 to F-8 were prepared with HPMC K15M; and F-9 to F-12 were prepared with HPMC K100M using a wet granulation process maintained same proportions, along with drug and EC. Tablets were evaluated for their pre-compression and post-compression characteristics and they were found to be in limits. From the dissolution testing, F-4 showed 100.34% medicament release in 12 h. In vivo studies were conducted on rabbit and pharmacokinetic parameters of the optimized formulation were evaluated using HPLC method. It was found that matrix tablets showed increased t1/2 and decreased Kel. The design signified that the drug release rate from tablets was influenced by the small proportion (around 7% of a tablet weight) of polymer mixture and it controlled 100% medicament release upto 12 h effectively with the low grade viscosity of HPMC combination, with good in vitro & in vivo correlation.
DOI: 10.6084/m9.figshare.20039311.v1
title: Preparation and in vitro & in vivo evaluation of cephalexin matrix tablets

description: The purpose of the study is to develop cephalexin controlled-release matrix tablets by using lower proportions of release retardant polymer and to establish their in vitro & in vivo correlation. Tablets were compressed by incorporating polymers in a matrix form along with drug which prolong the drug release. Twelve formulations were prepared by mixing ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) (three different viscosity grades) in various proportions. F-1 to F-4 formulations were prepared by incorporating drug, HPMC K4M and ethyl cellulose in 100 : 5 : 5, 100 : 10 : 5, 100 : 15 : 5 and 100 : 20 : 5; similarly, F-5 to F-8 were prepared with HPMC K15M; and F-9 to F-12 were prepared with HPMC K100M using a wet granulation process maintained same proportions, along with drug and EC. Tablets were evaluated for their pre-compression and post-compression characteristics and they were found to be in limits. From the dissolution testing, F-4 showed 100.34% medicament release in 12 h. In vivo studies were conducted on rabbit and pharmacokinetic parameters of the optimized formulation were evaluated using HPLC method. It was found that matrix tablets showed increased t1/2 and decreased Kel. The design signified that the drug release rate from tablets was influenced by the small proportion (around 7% of a tablet weight) of polymer mixture and it controlled 100% medicament release upto 12 h effectively with the low grade viscosity of HPMC combination, with good in vitro & in vivo correlation.
DOI: 10.6084/m9.figshare.7419047.v1
title: Synthesis of leading chalcones with high antiparasitic, against Hymenolepis nana, and antioxidant activities

description: The hymenolepiosis by Hymenolepis nana is a major public health problem in developing countries, and the commercial drugs against this parasitosis are not enough effective. The combination of antiparasitic and antioxidant agents has improved the treatment of some parasitoses. Thus, the development of new cestocidal and antioxidant agents to treat the hymenolepiosis cases is important. In the present study, four hydroxy- and four dihydroxy-chalcones were synthesized using the catalyst boron trifluoride diethyl etherate (BF3•OEt2). The antioxidant activity and antiparasitic against H. nana of chalcones were tested, as well as the toxicity by the brine shrimp lethality bioassay and the method of Lorke. The antioxidant activity was measured by three radical scavenging assays: 2,2’-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP). The hydroxyl substitution pattern (number and position), mainly in ring B, was responsible for the chalcone antiparasitic activity. At least one meta or para hydroxyl group in ring B was essential for activity of the synthetic chalcones against H. nana; The time taken for the parasite to die by the 3b and 3e chalcones (20 mg/mL) treatment was up to six times lower than the control drug Praziquantel. On the other hand, chalcones with catechol structure in ring B (3g and 3h) showed the highest antioxidant values. The toxicity evaluations suggests that synthetic hydroxychalcones with cestocidal (3b and 3e) and antioxidant (3g and 3h) activities are safe compounds and potential in vivo agents to treat this parasitosis.
DOI: 10.6084/m9.figshare.7419047
title: Synthesis of leading chalcones with high antiparasitic, against Hymenolepis nana, and antioxidant activities

description: The hymenolepiosis by Hymenolepis nana is a major public health problem in developing countries, and the commercial drugs against this parasitosis are not enough effective. The combination of antiparasitic and antioxidant agents has improved the treatment of some parasitoses. Thus, the development of new cestocidal and antioxidant agents to treat the hymenolepiosis cases is important. In the present study, four hydroxy- and four dihydroxy-chalcones were synthesized using the catalyst boron trifluoride diethyl etherate (BF3•OEt2). The antioxidant activity and antiparasitic against H. nana of chalcones were tested, as well as the toxicity by the brine shrimp lethality bioassay and the method of Lorke. The antioxidant activity was measured by three radical scavenging assays: 2,2’-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP). The hydroxyl substitution pattern (number and position), mainly in ring B, was responsible for the chalcone antiparasitic activity. At least one meta or para hydroxyl group in ring B was essential for activity of the synthetic chalcones against H. nana; The time taken for the parasite to die by the 3b and 3e chalcones (20 mg/mL) treatment was up to six times lower than the control drug Praziquantel. On the other hand, chalcones with catechol structure in ring B (3g and 3h) showed the highest antioxidant values. The toxicity evaluations suggests that synthetic hydroxychalcones with cestocidal (3b and 3e) and antioxidant (3g and 3h) activities are safe compounds and potential in vivo agents to treat this parasitosis.
DOI: 10.6084/m9.figshare.20039317
title: A smart approach for delivery of aripiprazole via oro-soft palatal mucosal route for improved therapeutic efficacy

description: Effective management of schizophrenia, acute mania, mixed episodes associated with bipolar disorders, and depression can be managed with aripiprazole moiety. In the present research work an attempt was made to minimize the dose related side effects thus improving the quality life of the patients. A novel biopolymer was isolated from the fruits of Trachyspermum ammi. Ten optimized nanosized aripiprazole loaded formulations were prepared in 1-5% concentration of biopolymer (FA1-FA5) and sodium CMC (FM1-FM5) by solvent casting technique. The formulated flexy films were evaluated for thickness, folding endurance, weight uniformity, surface pH, mucoadhesivity, In-vitro drug release studies, In-vivo pharmacodynamic study and stability studies. The isolated biopolymer showed inbuilt fimability and mucoadhesivity and consists of carbonyl, hydroxyl and thiocarbonyl functional groups. All formulations showed folding endurance from 153 to 170, mucoadhesion time in the range of 24-48hrs., and in-vitro drug release was performed using dynamic Franz Diffusion cell and analyzed using BIT-SOFTWARE. The experimental animals showed improved activity score on actophotometer. The formulated nanosized aripiprazole loaded bio-flexy films showed pharmacotherapeutic response. Conclusion can be drawn that optimized formulation showed effective Pharmacodynamic activity and can be used as for improving therapeutic efficacy of aripiprazole through this platform.
DOI: 10.6084/m9.figshare.7419872
title: Evaluation of community pharmacists’ involvement in public health activities in Nigeria

description: The aims of the study were to identify the types, determine the extent of community pharmacists’ involvement, and evaluate the factors influencing their participation in public health activities in Nigeria. The study was a cross-sectional survey of randomly selected 130 registered community pharmacies. Pretested questionnaire was the instrument for data collection. Descriptive and inferential statistics were used to analyse data. Response rate was 94.9%. The study identified 31 types of public health activities which community pharmacists participated in. Their extent of involvement was highest in patient counseling (4.93 ± 0.25), personal hygiene (4.90 ± 0.37), maintenance of normal blood pressure (4.88 ± 0.32), and techniques for using vagina pessaries (4.85 ± 0.38). Lowest areas of involvement were elimination of smokeless tobacco use (2.27 ± 1.56), use of seat belts when driving (2.03 ± 1.46), and the need to live in a safe neighborhood (1.42 ± 0.53). Inadequate training (96%), lack of pharmacists’ time (94.6%), inadequate personnel (92.3%), lack of patients’ time (88.5%), lack of profit (85.4%), inadequate space in the pharmacy (82.3%) and inadequate patients’ information (69.9%) significantly influenced their participation. The study concluded that community pharmacists would participate more in public health activities if the identified barriers are reduced.
DOI: 10.6084/m9.figshare.7419872.v1
title: Evaluation of community pharmacists’ involvement in public health activities in Nigeria

description: The aims of the study were to identify the types, determine the extent of community pharmacists’ involvement, and evaluate the factors influencing their participation in public health activities in Nigeria. The study was a cross-sectional survey of randomly selected 130 registered community pharmacies. Pretested questionnaire was the instrument for data collection. Descriptive and inferential statistics were used to analyse data. Response rate was 94.9%. The study identified 31 types of public health activities which community pharmacists participated in. Their extent of involvement was highest in patient counseling (4.93 ± 0.25), personal hygiene (4.90 ± 0.37), maintenance of normal blood pressure (4.88 ± 0.32), and techniques for using vagina pessaries (4.85 ± 0.38). Lowest areas of involvement were elimination of smokeless tobacco use (2.27 ± 1.56), use of seat belts when driving (2.03 ± 1.46), and the need to live in a safe neighborhood (1.42 ± 0.53). Inadequate training (96%), lack of pharmacists’ time (94.6%), inadequate personnel (92.3%), lack of patients’ time (88.5%), lack of profit (85.4%), inadequate space in the pharmacy (82.3%) and inadequate patients’ information (69.9%) significantly influenced their participation. The study concluded that community pharmacists would participate more in public health activities if the identified barriers are reduced.
DOI: 10.6084/m9.figshare.20039317.v1
title: A smart approach for delivery of aripiprazole via oro-soft palatal mucosal route for improved therapeutic efficacy

description: Effective management of schizophrenia, acute mania, mixed episodes associated with bipolar disorders, and depression can be managed with aripiprazole moiety. In the present research work an attempt was made to minimize the dose related side effects thus improving the quality life of the patients. A novel biopolymer was isolated from the fruits of Trachyspermum ammi. Ten optimized nanosized aripiprazole loaded formulations were prepared in 1-5% concentration of biopolymer (FA1-FA5) and sodium CMC (FM1-FM5) by solvent casting technique. The formulated flexy films were evaluated for thickness, folding endurance, weight uniformity, surface pH, mucoadhesivity, In-vitro drug release studies, In-vivo pharmacodynamic study and stability studies. The isolated biopolymer showed inbuilt fimability and mucoadhesivity and consists of carbonyl, hydroxyl and thiocarbonyl functional groups. All formulations showed folding endurance from 153 to 170, mucoadhesion time in the range of 24-48hrs., and in-vitro drug release was performed using dynamic Franz Diffusion cell and analyzed using BIT-SOFTWARE. The experimental animals showed improved activity score on actophotometer. The formulated nanosized aripiprazole loaded bio-flexy films showed pharmacotherapeutic response. Conclusion can be drawn that optimized formulation showed effective Pharmacodynamic activity and can be used as for improving therapeutic efficacy of aripiprazole through this platform.
DOI: 10.6084/m9.figshare.7419875
title: In vitro UV absorption properties and radical scavenging capacity of Morella parvifolia (Benth.) Parra-Os. extracts

description: The goal of this research was to identify major compounds of the aerial parts of M. parvifolia (Benth.) Parra-Os., that could enhance its possible application as additive in dermocosmetic products, as well as evaluate the antioxidant properties. The extracts agreed with the broad-spectrum UVB/UVA absorption detected and could act as broad-spectrum sunscreens, covering the UVA and UVB range. Methanolic extracts showed an important antiradical capacity (0.46 and 0.47 g/µmol DPPH), TPC (37.58 and 51.41mg GAE/g DS) and TAC (1.12 and 3.31 mg C3GE/g DS) in fruits and leaves, respectively. M. parvifolia could be considered as a prospective source of natural UV-radiation absorbers with antioxidant capacity. Although the results have clearly demonstrated the potential photoprotection capacity, more studies are needed to enhance its application as an additive in pharmaceutical and medicinal formulations.
DOI: 10.6084/m9.figshare.7419875.v1
title: In vitro UV absorption properties and radical scavenging capacity of Morella parvifolia (Benth.) Parra-Os. extracts

description: The goal of this research was to identify major compounds of the aerial parts of M. parvifolia (Benth.) Parra-Os., that could enhance its possible application as additive in dermocosmetic products, as well as evaluate the antioxidant properties. The extracts agreed with the broad-spectrum UVB/UVA absorption detected and could act as broad-spectrum sunscreens, covering the UVA and UVB range. Methanolic extracts showed an important antiradical capacity (0.46 and 0.47 g/µmol DPPH), TPC (37.58 and 51.41mg GAE/g DS) and TAC (1.12 and 3.31 mg C3GE/g DS) in fruits and leaves, respectively. M. parvifolia could be considered as a prospective source of natural UV-radiation absorbers with antioxidant capacity. Although the results have clearly demonstrated the potential photoprotection capacity, more studies are needed to enhance its application as an additive in pharmaceutical and medicinal formulations.
DOI: 10.6084/m9.figshare.7419860
title: Demographic, clinical and lifestyle predictors for severity of erectile dysfunction and biomarkers level in Malaysian patients

description: The incidence of erectile dysfunction (ED) is rising worldwide and its prevalence is one of the main health concerns that affect overall men well-being in Malaysia. The cluster of demographic, clinical and lifestyle factors may have contributed to the severity of ED and changes in biomarkers level; nevertheless these have not been studied extensively. This cross sectional study involved a total of 276 patients with 138 was diagnosed with ED. The demographic, clinical, lifestyle factors and severity of ED were assessed using a set of questionnaire and the International Index of Erectile Function (IIEF-5). Meanwhile, Total Testosterone (TT) and Asymmetric dimethylarginine (ADMA) levels were determined using the enzyme-linked immunosorbant assay (ELISA). Binary logistic regression test was used to demonstrate the predictors of severity of ED, TT and ADMA levels. Significant predictors for worsening of severity of ED are self-employed [10.55 (0.43 - 257.06), p=0.004], pensioner [8.07 (0.19 - 352.45), p=0.026], non-government employee [1.16 (0.05 - 26.26), p=0.04] and TT [0.41 (0.25 - 0.69), p=0.001]. Nevertheless, pensioner [0.08 (0.01 - 0.87), p=0.038] and unemployed [0.04 (0.01 - 0.42), p=0.007], were the predictors that may influence the changes of TT levels. On the other hand, academic qualification (secondary) [4.51 (0.48 - 42.83), p=0.014] and intensity of physical activities (&lt; 1 hour/day) [2.61 (0.65 - 10.48), p=0.008] were the predictors which were more likely to influence the changes of ADMA levels in ED patients. TT and ADMA levels were influenced by demographic and lifestyle factors whilst severity of ED was predicted by demographic and clinical factors in Malaysian ED population. These predictors may provide new knowledge on risk factors of severity of ED and help in management of ED. Thus, the predictive models could serve as a primary guidance to physicians to ensure ED being managed and treated more effectively.