Mughal Qayum

Compositional Studies: Antioxidant and Antidiabetic Activities of Capparis decidua (Forsk.) Edgew

Capparis decidua is one of the traditional remedies used for various medicinal treatments in Pakistan. This study presents the determination of proximate composition, amino acids, fatty acids, tocopherols, sterols, glucosinolate and phenolic content in extracts obtained from different aerial parts of C. decidua, as well as their antidiabetic and antioxidant activity. All examined extracts were prominently rich in phenolics and glucosinates, and they showed potent antidiabetic and antihemolytic activity. The present study could be helpful in developing medicinal preparations for the treatment of diabetes and related symptoms.

Anti-inflammatory activities of Taxusabietane A isolated from Taxus wallichiana Zucc.

Current study was conducted to identify constituents of Taxus wallichiana Zucc. that might be responsible for its folk use in anti-inflammatory conditions. Taxusabietane A was isolated from the bark extract of Taxus wallichiana Zucc. Taxusabietane A was analyzed for in-vitro and in-vivo anti-inflammatory activities using Lipoxygenase (LOX) inhibition assay and carrageenan-induced paw edema model. Taxusabietane A revealed considerable LOX inhibitory activity with the IC(50) value being 57 ± 0.31. Standard compound Baicalein showed the IC(50) value being 22.1 ± 0.03 μM. Taxusabietane A also showed significant (5 and 10 mg/kg) anti-inflammatory activity induced by carrageenan. However, this study highlighted the potential of Taxusabietane A to be further explored as a new lead compound for management of conditions associated with inflammation.

Formulation and evaluation of antisebum secretion effects of sea buckthorn w/o emulsion

Purpose: This study was designed to formulate and evaluate the anti-sebum secretion effects of a topical skin-care cream (w/o emulsion) of sea buckthorn versus its vehicle (Base) as control. Materials and Methods: Concentrated sea buckthorn (H.rhamnoides) fruit extract was entrapped in the inner aqueous phase of w/o emulsion. Base containing no extract and a Formulation containing 1% concentrated extract of H.rhamnoides was formulated. Lemon oil was incorporated to the odor. Both the Base and the Formulation were stored at different storage conditions for a period of 4 weeks to predict their stability. Different stability parameters i.e.; physical stability, centrifugation, and pH were monitored at different time intervals. Both the Base and the Formulation were applied to the cheeks of 10 healthy human volunteers (n=10) for a period of 8 weeks. Result: The expected organoleptic stability of creams was achieved from 4 weeks in-vitro study period. Odor disappeared with the passage of time due to volatilization of lemon oil. The pH of the Formulation showed significant (P = 0.0002) decline due to high concentration of organic acids present in sea buckthorn. Similarly the Formulation showed statistically significant (P < 0.05) effects on skin sebum secretion. Conclusion: The in vitro results showed a good stability over 4 weeks of observation period of both the Base and Formulation and the Formulation has anti sebum secretion effects over 8 weeks of observation period.

Structural insights to investigate Conypododiol as a dual cholinesterase inhibitor from Asparagus adscendens

The main aim of the current study was to explore molecular insights for potentially new dual cholinesterase inhibitor(s) from Asparagus adscendens via molecular docking. This medicinal plant is traditionally used as a nerve tonic and remedy for memory impairments. Conypododiol was isolated from the chloroform fraction of methanolic extract of A. adscendens, based on bioactivity guided isolation. Conypododiol exhibited significant inhibition of both acetylcholinesterase and butyrylcholinesterase, having the IC(50) values 2.17 ± 0.1 μM and 11.21 ± 0.1 μM, respectively. IC(50) values of the standard compound Galanthamine for both the enzymes were 0.537 ± 0.018 μM and 8.6 ± 0.27 μM, respectively. Based on MTT cytotoxicity assay, Conypododiol was found safe against LCMK-2 monkey kidney epithelial cells and mice hepatocytes. Molecular docking studies revealed the hydrogen bonding interactions of Conypododiol with His440 and Ser200 at esteratic site (ES), and also with Tyr334 at peripheral anionic site (PAS) of the aromatic gorge of acetylcholinesterase. Simultaneous contacts of Conypododiol with PAS and ES shows its significance as a bivalent ligand. This preliminary study highlighted the potential of Conypododiol to be further developed and modified as new lead compound identified by its folk use.

Molecular simulations probing Kushecarpin A as a new lipoxygenase inhibitor

Zizyphus oxyphylla Edgew is used in Pakistan as a folk medicinal remedy for inflammatory conditions, pains especially rheumatic pain, fevers, allergy and diabetes. The aim of the current study was to scientifically validate the folk use of Z. oxyphylla Edgew by using the isolated compound in vitro and in vivo levels. Kushecarpin A was isolated from ethyl acetate fraction of the plant crude extract. Molecular docking simulations predicted Kushecarpin A as a potential new lipoxygenase (LOX) inhibitor. Kushecarpin A showed significant lipoxygenase inhibition (IC(50): 7.2 ± 0.02 μM) thus validated computational prediction. It also exhibited significant and highly significant inhibition (p < 0.05 and p < 0.01) of carrageenan-induced hind paw oedema at the doses of 5, 10 and 20 mg/kg. Kushecarpin A seems to be a potentially new anti-inflammatory compound responsible for anti-inflammatory activities of Z. oxyphylla Edgew. In vitro and in vivo anti-inflammatory inflammatory activities were found in good agreement with the folk medicinal use of Z. oxyphylla Edgew in inflammatory disorders.

Analgesic and antiinflammatory activities of taxoids from Taxus wallichiana Zucc.

A study was conducted to identify constituents that might be responsible for analgesic and antiinflammatory conditions. Tasumatrol B, 1,13‐diacetyl‐10‐deacetylbaccatin III (10‐DAD) and 4‐deacetylbaccatin III (4‐DAB) were isolated from the bark extract of Taxus wallichiana Zucc. All the compounds were assessed for analgesic and antiinflammatory activities using an acetic acid‐induced writhing model, a hot‐plate test, a carrageenan‐induced paw oedema model, a cotton‐pellet oedema model and in vitro lipoxygenase inhibitory assay. All the compounds, especially tasumatrol B, revealed significant analgesic activity in comparison to a saline group based on an acetic acid‐induced model. Similarly all of the test compounds, particularly tasumatrol B, showed significant antiinflammatory activity. However, all the compounds failed to exhibit any considerable activity in of the hot‐plate test and the in vitro lipoxygenase inhibitory assay. This study has highlighted the potential of tasumatrol B to be further explored as a new lead compound for the management of pain and inflammation, one that has been discovered by scientific validation of the traditional medicinal use of T. wallichiana Zucc. Copyright

Amberlite IR-120H as a recyclable catalyst for the synthesis of 1,8-dioxo-octahydroxanthene analogs and their evaluation as potential leishmanicidal agents

Bioactive 1,8-dioxo-octahydroxanthene analogs were synthesized by employing Amberlite IR-120H as a recyclable heterogeneous catalyst in acetonitrile. Their in vitro cytotoxicities and leishmanicidal activities were evaluated. The synthetic protocol involves a Knoevenagel condensation followed by a Michael addition and finally a cyclodehydration of dimedone with an aldehyde. Among the solvents used for this protocol, acetonitrile gave the best results in terms of isolated yield. Being a one-pot reaction, this protocol presents several advantages over the previously reported methods in terms of its low cost, catalyst recyclability, atom economy, and convenient work-up in addition to the respectable resulting isolated yield. The non-cytotoxic nature of these 1,8-dioxo-octahydroxanthene analogs provides a safer route for related biological studies. Some of the prepared materials (3b, 3c, 3d, 3e and 3g) showed significant leishmanicidal activity against Leishmania major (DESTO) promastigotes in comparison to the standard compound, pentamidine.

CHEMICAL CONSTITUENTS AND ANTIOXIDANT ACTIVITY OF n-HEXANE EXTRACT OF Impatiens bicolor

Plants belonging to the genus Impatiens (Balsaminaceae) are rich in organic acids, anthraquinones, and flavonoids [1–3]. It is well known that these classes of aromatic compounds possess widespread pharmacological activities. Previous investigations showed that various plant extracts of Impatiens bicolor Royle display antimicrobial and antifungal activity [4, 5], as well as acetylcholinesterase inhibition and antioxidant activities [6]. Thus, there is a considerable research interest in the assay of composition and/or antioxidant properties of various extracts of I. bicolor. This study presents the very first investigation on the chemical composition of plant extracts of I. bicolor, as well as their antioxidant activities, and it can provide a broad base for the possibility of further detailed pharmacological studies on this species. The sub-extracted samples of the n-hexane fraction of I. bicolor were subjected to detailed GC and GC/MS analysis in order to determine the impact of chemical composition on their antioxidant activity. About 42 compounds were identified in eight samples, representing 56.64–93.85% in total. The percentage compositions of the samples were computed in each case from GC peak areas and are shown in Table 1. In general, all investigated samples can be characterized as mixtures of aliphatic compounds (20.11–93.85%), with oxygenated aliphatic compounds as the most abundant (5.97–89.38%). The fatty acid esters (FAEs) were found to be major components of the investigated subfractions of the n-hexane extract, comprising trans-methyl 13-octadecenoate (2.44–47.29%), methyl heptadecanoate (8.76–18.82%), methyl octadecanoate (4.96–16.49%), methyl docosanoate (3.14–12.64%), methyl tetracosanoate (1.04–11.23%), and methyl eicosanoate (3.83–10.93%). These compounds were mainly found in samples eluted with solvents with relatively low polarity (MQ-1 to MQ-5), while samples eluted with higher polarity (MQ-6 to MQ-8) contained significant amounts of aromatic compounds and shorter-chain oxygenated aliphatic compounds. The antioxidant activity of sub-extracted samples of the n-hexane fraction of I. bicolor were evaluated by DPPH radical-scavenging test. Assessed samples were able to reduce the stable violet DPPH radical to the yellow DPPH-H, reaching 50% of reduction with IC 50 values ranging from 23.22 0.75 g/mL for sample MQ1 to 59.00 2.01 g/mL for sample MQ8 (Table 2). Those values are comparable to ascorbic acid (IC 50 = 7.80 0.14 g/mL), whose antioxidant properties are already known [7, 8]. Despite the fact that major natural antioxidants belong to the class of phenolic compounds, such as thymol and carvacrol [9, 10], the investigated samples, rich in FAEs, showed radical scavenging activity. The IC 50 values presented in the Table 2 are comparable with the content of FAEs in the investigated sample. However, the percentage of these esters decreases from sample MQ1 to sample MQ8, and due to the polarity of eluent, the antioxidant activity decreases. Sample MQ1 was the exception, with a content of FAEs of 58.33%, which is much lower than in the next sample, MQ2, but sample MQ1 showed uniqueness in the content of 2-(1-naphthyl)acetophenone, a member of a class of already known natural antioxidants [11, 12].

Robust Synthesis of Ciprofloxacin-Capped Metallic Nanoparticles and Their Urease Inhibitory Assay.

The fluoroquinolone antibacterial drug ciprofloxacin (cip) has been used to cap metallic (silver and gold) nanoparticles by a robust one pot synthetic method under optimized conditions, using NaBH4 as a mild reducing agent. Metallic nanoparticles (MNPs) showed constancy against variations in pH, table salt (NaCl) solution, and heat. Capping with metal ions (Ag/Au-cip) has significant implications for the solubility, pharmacokinetics and bioavailability of fluoroquinolone molecules. The metallic nanoparticles were characterized by several techniques such as ultraviolet visible spectroscopy (UV), atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) methods. The nanoparticles synthesized using silver and gold were subjected to energy dispersive X-ray tests in order to show their metallic composition. The NH moiety of the piperazine group capped the Ag/Au surfaces, as revealed by spectroscopic studies. The synthesized nanoparticles were also assessed for urease inhibition potential. Fascinatingly, both Ag-cip and Au-cip NPs exhibited significant urease enzyme inhibitory potential, with IC50 = 1.181 ± 0.02 µg/mL and 52.55 ± 2.3 µg/mL, compared to ciprofloxacin (IC50 = 82.95 ± 1.62 µg/mL). MNPs also exhibited significant antibacterial activity against selected bacterial strains.

Efficient PPA-SiO2-catalyzed Synthesis of β-enaminones Under Solvent-Free Conditions

An efficient method has been developed for the synthesis of β-enaminones under solvent-free reaction conditions using PPA-SiO2 as catalyst. The reaction yields were good to excellent (up to 90%). This methodology affords high selectivity and good tolerance of a variety of different functional groups present on both aromatic and aliphatic amines. In addition, the methodology is environmentally benign and cost-effective due to absence of solvent and easy work-up.