Muhammad Farman

Analgesic and anti-inflammatory effects of Pistacia integerrima extracts in mice.

AIM OF STUDY Extracts of Pistacia integerrima galls have been dispensed by Traditional Practitioners of Subcontinent for chest diseases as well as for aches and pains in the body. This study was planned to evaluate the possible analgesic and antiinflammatory effects of Pistacia integerrima extracts. MATERIALS AND METHODS Analgesia was determined using acetic acid induced abdominal constriction and formalin induced paw licking in mice. Antinociceptive effect was observed by thermally induced algesia in mice. RESULTS Pistacia integerrima leaves extracts showed significant response against chemically induced pain (P<0.001) whereas galls extracts had highly significant protection (P<0.0001) in a dose dependent manner. In thermally induced algesia, Pistacia integerrima galls extracts 200 mg/kg (p.o.), showed significant (P<0.05) response but less than pentazocine and diclofenac, positive references. The extracts of Pistacia integerrima 50-200 mg/kg (p.o.) had modest activity against hind paw acute and chronic inflammation induced by formalin (P<0.01). CONCLUSION These results demonstrate that Pistacia integerrima extracts have antinociceptive and analgesic effects and no apparent acute toxicity on oral administration.

Ethnopharmacological importance of medicinal flora from the district of Vehari, Punjab province, Pakistan

ETHNOPHARMACOLOGICAL RELEVANCE Ethnopharmacological studies are important for the discovery of new drugs from reported indigenous flora. The current study was aimed to document medicinal flora and its therapeutic actions along with the relative importance in local health care system of the district of Vehari, Punjab province, Pakistan. MATERIALS AND METHOD Rapid appraisal approach (RAA) and semi structured interviews were used along with the group meetings with herbalists, local inhabitants and landowners to collect the relevant data. RESULTS AND DISCUSSIONS A total 77 medicinal plants belonging to 41 families disseminated among 71 genera were reported. Fabaceae was the predominant family over others with 9 reported medicinal plant species. Use frequency of leaves was at peak with 30.12% followed by stem 24.62%, fruit 14.22%, flower 12.97%, seeds 12.13%, bark 4.6% and pod 1.25%, in herbal preparations. Allium cepa exhibited the highest use value (0.90) while lowest use value (UV) was reflected by Aerva javanica (0.10). Documentation of various medicinal plants for the treatment of cancer, hepatitis and cardiac disorders is evidence in favor to highlight the value of medicinal flora. CONCLUSIONS Unfortunately, no attention has been paid to this treasure in term of conservation and utilization in modern healthcare system, where these plants can be a best replacement of chemically synthesized drugs. It is also recommended that plants exhibiting high UV should be screened for detailed bio-active phytochemicals.

Synthesis, anti-HIV activity and molecular modeling study of 3-aryl-6-adamantylmethyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives

Abstract A series of novel 3-aryl-6-adamantylmethyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles 6a–l were synthesized by a simple method with the aim of developing novel HIV non-nucleoside reverse transcriptase inhibitors. All the synthesized compounds were structurally confirmed by spectral analyses. The structure of 6a was unambiguously verified by X-ray structure determination. The synthesized compounds were evaluated for their anti-HIV activity and four analogs displayed moderate inhibitory activity with EC50 values ranging from 10.10 to 12.40 μg mL–1. Molecular docking of 6g with HIV-1 reverse transcriptase was studied to rationalize some structure-activity relationships (SARs).

Conjugates of degraded and oxidized hydroxyethyl starch and sulfonylureas: synthesis, characterization, and in vivo antidiabetic activity.

Orally administered drugs usually face the problem of low water solubility, low permeability, and less retention in bloodstream leading to unsatisfactory pharmacokinetic profile of drugs. Polymer conjugation has attracted increasing interest in the pharmaceutical industry for delivering such low molecular weight (Mw) drugs as well as some complex compounds. In the present work, degraded and oxidized hydroxyethyl starch (HES), a highly biocompatible semisynthetic biopolymer, was used as a drug carrier to overcome the solubility and permeability problems. The HES was coupled with synthesized N-arylsulfonylbenzimidazolones, a class of sulfonylurea derivatives, by creating an amide linkage between the two species. The coupled products were characterized using GPC, FT-IR, (1)H NMR, and (13)C NMR spectroscopy. The experiments established the viability of covalent coupling between the biopolymer and N-arylsulfonylbenzimidazolones. The coupled products were screened for their in vivo antidiabetic potential on male albino rats. The coupling of sulfonylurea derivatives with HES resulted in a marked increase of the hypoglycemic activity of all the compounds. 2,3-Dihydro-3-(4-nitrobenzensulfonyl)-2-oxo-1H-benzimidazole coupled to HES10100 was found most potent with a 67% reduction in blood glucose level of the rats as compared to 41% reduction produced by tolbutamide and 38% by metformin.

Chemometrics Methods for Specificity, Authenticity and Traceability Analysis of Olive Oils: Principles, Classifications and Applications

Background. Olive oils (OOs) show high chemical variability due to several factors of genetic, environmental and anthropic types. Genetic and environmental factors are responsible for natural compositions and polymorphic diversification resulting in different varietal patterns and phenotypes. Anthropic factors, however, are at the origin of different blends’ preparation leading to normative, labelled or adulterated commercial products. Control of complex OO samples requires their (i) characterization by specific markers; (ii) authentication by fingerprint patterns; and (iii) monitoring by traceability analysis. Methods. These quality control and management aims require the use of several multivariate statistical tools: specificity highlighting requires ordination methods; authentication checking calls for classification and pattern recognition methods; traceability analysis implies the use of network-based approaches able to separate or extract mixed information and memorized signals from complex matrices. Results. This chapter presents a review of different chemometrics methods applied for the control of OO variability from metabolic and physical-chemical measured characteristics. The different chemometrics methods are illustrated by different study cases on monovarietal and blended OO originated from different countries. Conclusion. Chemometrics tools offer multiple ways for quantitative evaluations and qualitative control of complex chemical variability of OO in relation to several intrinsic and extrinsic factors.

4-Eth-oxy-benzohydrazide.

The title compound, C9H12N2O2, is approximately planar (r.m.s. deviation = 0.13 Å for all non-H atoms). The carbonyl O atom is involved as acceptor in three different hydrogen-bond interactions. One N—H⋯O and the C—H⋯O(carbonyl) contact together with a weak C—H⋯O(ethoxy) interaction link the molecules into sheets parallel to (102). These are further linked into a three-dimensional network via the remaining C—H⋯O(carbonyl) hydrogen bond and a C(methylene)—H⋯π interaction

2-(3-Methoxyphenyl)acetohydrazide

Ahmad, R., Iqbal, R., Akhtar, R. H., Haq, Z. U., Duddeck, H., Stefaniak, L. & Sitkowski, J. (2001). Nucleosides Nucleotides Nucleic Acids, 20, 1671–1682. Allen, F. H., Kennard, O., Watson, D. G., Brammer, L., Orpen, A. G. & Taylor, R. (1987). J. Chem. Soc. Perkin Trans. 2, pp. S1–19. Al-Soud, Y. A., Al-Deeri, M. N. & Al-Mosoudi, N. A. (2004). Il Farmaco, 59, 775–783. Al-Talib, M., Tastoush, H. & Odeh, N. (1990). Synth. Commun. 20, 1811–1814. Bruker (1998). SMART. Bruker AXS Inc., Madison, Wisconsin, USA. Bruker (1999). SAINT and SHELXTL. Bruker AXS Inc., Madison, Wisconsin, USA. Burla, M. C., Caliandro, R., Camalli, M., Carrozzini, B., Cascarano, G. L., De Caro, L., Giacovazzo, C., Polidori, G. & Spagna, R. (2005). J. Appl. Cryst. 38, 381–388. El-Emam, A. A., Al-Deeb, O. A., Al-Omar, M. & Lehmann, J. (2004). Bioorg. Med. Chem. 12, 5107–5113. Furniss, B. S., Hannaford, A. J., Rogers, V., Smith, P. W. G. & Tatchell, A. R. (1978). Editors. Vogel’s Textbook of Practical Organic Chemistry, 4th ed. London: Longman. Sheldrick, G. M. (1996). SADABS. University of Göttingen, Germany. Sheldrick, G. M. (1997). SHELXL97. University of Göttingen, Germany. Yousif, M. Y., Ismail, A. M., Elman, A. A. & El-Kerdawy, M. M. (1986). J. Chem. Soc. Pak. 8, 183–187. Zheng, X., Li, Z., Wang, Y., Chen, W., Huang, Q., Liu, C. & Song, G. (2003). J. Fluorine Chem. 117, 163–169. organic compounds

2-(2-Fluoro­biphenyl-4-yl)-N′-(propan-2-yl­idene)propanohydrazide

In the title compound, C18H19FN2O, the hydrazide side chain is approximately perpendicular to the central ring [dihedral angle = 76.80 (5)°]. The F atom is disordered over two positions with occupancies of 0.818 (2) and 0.182 (2). The packing consists of chains of molecules parallel to the a axis, connected by a bifurcated N—H⋯(O,N) hydrogen bond and a weak Cphenyl—H⋯O hydrogen bond. The packing is extended to a layer structure parallel to the ab plane by a weak Cphenyl—H⋯F hydrogen bond.

1-(4-Ethoxy-benzo-yl)-4-(4-methoxy-phen-yl)thiosemicarbazide.

The title compound, C17H19N3O3S, crystallizes with two closely similar independent molecules related by a pseudotranslation of c/2. Each molecule consists of three approximately planar moieties centred on the N2CS group and the two ring systems. The packing involves classical H bonds of the form Namide—H⋯S and Nhydrazine—H⋯OC, together with various weak hydrogen bonds and Nhydrazine—H⋯π interactions. The overall packing is three-dimensional, but layer substructures parallel to the xz plane can be readily identified. Each molecule forms a topologically equivalent set of hydrogen-bond interactions.