ABSTRACT
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.
Subject(s)
Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Hypolipidemic Agents/chemistry , Hypolipidemic Agents/pharmacology , Securidaca/chemistry , Seeds/chemistry , Solvents/chemistry , Alkaloids/chemistry , Alkaloids/pharmacology , Animals , Antioxidants/metabolism , Blood Glucose/drug effects , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Experimental/drug therapy , Flavonoids/chemistry , Flavonoids/pharmacology , Glyburide/pharmacology , Hypolipidemic Agents/metabolism , Male , Plant Extracts/chemistry , Plant Extracts/pharmacology , Polyphenols/chemistry , Polyphenols/pharmacology , Rats , Rats, Wistar , Streptozocin/pharmacology , Tannins/chemistry , Tannins/pharmacologyABSTRACT
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.
Subject(s)
Analgesics/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Ibuprofen/analogs & derivatives , Ibuprofen/pharmacology , Pain Measurement/drug effects , Analgesics/chemical synthesis , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Male , Molecular Structure , RatsABSTRACT
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.
Subject(s)
Analgesics/chemical synthesis , Ethylenediamines/chemical synthesis , Histamine Antagonists/chemical synthesis , Phenothiazines/chemical synthesis , Analgesics/pharmacology , Animals , Ethylenediamines/pharmacology , Histamine Antagonists/pharmacology , Male , Mice , Phenothiazines/pharmacology , Rats , Rats, Wistar , Structure-Activity RelationshipABSTRACT
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.
