The Effects of Solvent Polarity on Hypoglycemic and Hypolipidemic Activities of Securigera Securidaca (L.) Seeds.

The search for indigenous natural antidiabetic and antilipidemec agents is still ongoing. Medicinal plants are widely used for this purpose. These herbs are very rich sources of bioactive compounds as flavonoids, polyphenols, tannins, alkaloids which have been reported as effective role to reduce blood glucose and lipid levels. Securigera securidaca seed is reputed in folk medicine for their value as antidiabetic and antilipidemec drugs. In this research, the effect of solvent polarity in bioactive extraction contents of this plant was evaluated by GC-MS analysis. Then antidiabetic and antilipidemic activies of different extracts were investigated in streptozotocine-induced diabetic rats and compared to glibenclamide as known chemical drug for diabetes.The results indicated that, carbon tetrachloride extract of Securigera securidaca seeds showed the best and significant hypoglycemic and hypolipidemic activities compared to other extracts because of its more sterols and fatty acids content with beta cells protecting effect from high glucose-induced apoptosis and also increasing in insulin level and sensitivity.

Synthesis and Pharmacological Evaluation of New Chemical Entities from Ibuprofen as Novel Analgesic Candidates.

Non-steroidal anti-inflammatory drugs (NSAIDs) are the first choice of drugs that are normally used for the treatment of pain and inflammation. Ibuprofen (I) and its analogues as the most widely used NSAIDs have been synthesized in recent years. In an effort to establish new candidates with improved analgesic properties, derivatives (II-VII) with substituted aromatic as well as aliphatic moieties were synthesized in this experiment and evaluated in formalin test with rats. The results were compared to ibuprofen and control groups. Findings indicated that derivatives with new alkylphenyl rings (VI and VII) had some similar or more analgesic activities relative to the control and ibuprofen groups, respectively; which could be justified as to more alkyl and phenyl groups instead of p-isobutylphenyl moiety in I.

Evaluation of apoptosis in four human tumour cell lines with differing sensitivities to cisplatin.

Four human tumour cell lines were evaluated for their ability to undergo apoptosis when subjected to cisplatin or hyperthermia treatment. In an ovarian carcinoma line (A2780s) and its derivative cisplatin resistant line (A2780cp) the variation in response was expressed for both the colony survival endpoint and the apoptosis endpoint. Apoptosis was measured by the number of floating cells, DNA agarose gels, and electron microscopy. In fact, cisplatin resistance was expressed to a higher level for apoptosis, than colony survival in the A2780cp cell line compared to the A2780s line. The melanoma cell line (Sk Mel-3) also showed induced apoptosis by cisplatin treatment while the glioma line (U87MG) showed little to no apoptosis in response to cisplatin treatment. Hyperthermia (43 degrees C for 1 hour) induced apoptosis in the human melanoma cell line but not in the glioma cell line. These data indicate that, while both cisplatin and hyperthermia can induce apoptosis in human tumour cell lines, the degree of induction is highly cell line dependent.

Synthesis and antinociception activity of new substituted phenothiazines and ethylenediamines as antihistaminic drugs.

Antihistamines play an important role in medicine when it comes to relieving seasonal or non-seasonal rhinitis, the common cold, and itching. They have also shown many various combinations of pharmacological properties such as anti-inflammatory and analgesic activities. Phenothiazines and ethylenediamines are 2 important classes of antihistamines with analgesic activities in addition to other pharmacological effects. In this study, some new derivatives of these compounds (V-IX) were synthesized and their antinociceptive behaviors were examined by pharmacological tests. The results indicated that new analogue with methyl groups produced a better analgesic activity than chlorine atoms but less than III (without any substitutions) in ethylenediamine class. Also in phenothiazine class, adding pyrimidine and pyridine substituted showed the better analgesic activity compared to other groups. Moreover, the analgesic activities proved that dimethylamine is the best group in amino alkyl side chain of these molecules relative to the substituted piperazines in new analogues.

Antihyperglycemic and antihyperlipidemic effects of newly synthesized glibenclamide analogues on streptozotocin-diabetic rats.

In this study, new glibenclamide analogues (5a-d) with substituted pharmacological triethoxysilyl propan, allyl and ethoxyphenyl groups for cyclohexyl moiety have been synthesized by condensing sulfonamide (4) with related isocyanate or isothiocyanate's compounds. The newly synthesized drugs were evaluated for their antihyperglycemic and antihyperlipidemic activities with streptozotocin (STZ)-induced diabetic rats. All showed hypoglycemic and hypolipidemic activities compared to the control animals but 5c and 5d exhibited more and significant lowering blood activities similar to glibenclamide. This was concerned with identical affinities to bind with SUR1 receptor. Moreover, the new drugs displayed high efficiency for reducing serum LDL level which resulted in a high HDL/LDL ratio as a good lipid profile compared to other groups.

Synthesis and antinociceptive behaviors of new methyl and hydroxyl derivatives of phencyclidine.

Phencyclidine (I) and its derivatives show such pharmacological behaviors as analgesic, anticonsulvant, anti-anxiety and antidepressant, while interacting with central nervous system. In this study, new methyl and hydroxyl derivatives of PCP were synthesized and their antinociceptive behaviors in animals were examined by measuring the number of writhing in a writhing test of visceral pain and the pain scores in Formalin test. Compared to control and PCP groups, findings in experimental groups indicated the new synthesized analogues (compounds II, III and V, 10 mg/kg) of PCP were able to produce more analgesic effects in formalin and writhing tests, especially for compound V. It was concluded that the new synthesized derivatives of PCP could substantially and respectively diminish acute and chronic pains.