MEDICINAL EFFICACY OF ANTIHYPERTENSIVE AGENTS FOR ACUTE INFLAMMATION; AN ASSOCIATED RISK FACTOR OF HYPERTENSION

Hypertension is a lasting therapeutic complaint which can be kept in control by changing one’s dietary and lifestyle habits. Present study is based on identification of risk of acute pancreatitis which may occur with different doses of atenolol in Pakistani population. About 50% of our study population was administered with β-blockers. The β- blockers significantly decreased the levels of CRP (C- Reactive Protein) of test population. This observation strongly depicts high potential of beta blockers in stabilization of CRP levels and decreasing inflammatory response. In our study the patients were administered with many combinations with beta-blocker and their results showed that these combinations lower the CRP level in hypertensive patients. We conclude that antihypertensive also minimize the inflammation associated hypertension but not completely, as inflammation was reversed only in 67.5% population who were using beta-blocker. When treating hypertension, anti-inflammatory medicine treatment needs to be endorsed to successfully treat complaints and increase the communal and psychosomatic status of the patient

Astragalin: A Bioactive Phytochemical with Potential Therapeutic Activities

Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. This review article intends to emphasize on one of the naturally occurring flavonoids, astragalin (kaempferol 3-glucoside), which is a bioactive constituent of various traditional medicinal plants such as Cuscuta chinensis. This multifaceted compound is well known for its diversified pharmacological applications such as anti-inflammatory, antioxidant, neuroprotective, cardioprotective, antiobesity, antiosteoporotic, anticancer, antiulcer, and antidiabetic properties. It carries out the aforementioned activities by the regulation and modulation of various molecular targets such as transcription factors (NF-κB, TNF-α, and TGF-β1), enzymes (iNOS, COX-2, PGE2, MMP-1, MMP-3, MIP-1α, COX-2, PGE-2, HK2, AChe, SOD, DRP-1, DDH, PLCγ1, and GPX), kinases (JNK, MAPK, Akt, ERK, SAPK, IκBα, PI3K, and PKCβ2), cell adhesion proteins (E-cadherin, vimentin PAR-2, and NCam), apoptotic and antiapoptotic proteins (Beclin-1, Bcl-2, Bax, Bcl-xL, cytochrome c, LC3A/B, caspase-3, caspase-9, procaspase-3, procaspase-8, and IgE), and inflammatory cytokines (SOCS-3, SOCS-5, IL-1β, IL-4, IL-6, IL-8, IL-13, MCP-1, CXCL-1, CXCL-2, and IFN-γ). Although researchers have reported multiple pharmacological applications of astragalin in various diseased conditions, further experimental investigations are still mandatory to fully understand its mechanism of action. It is contemplated that astragalin could be subjected to structural optimization to ameliorate its chemical accessibility, to optimize its absorption profiles, and to synthesize its more effective analogues which will ultimately lead towards potent drug candidates

Synthesis, antimicrobial evaluation and hemolytic activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives

2,5-Disubstituted 1,3,4-oxadiazole compounds are one of the most attractive classes for researchers due to their pharmacological activities. In the current research, a new series of 2-[[5-alkyl/aralkyl-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamides (6a–m) were prepared by converting different aryl/aralkyl organic acids (1a–m) successively into corresponding esters (2a–m), hydrazides (3a–m) and 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m). Finally, the target compounds 6a–m were synthesized by stirring 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m) with 2-bromo-N-[4-(4-morpholinyl)phenyl]acetamide (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). The structures of the synthesized compounds were elucidated through IR, 1H-NMR, 13C-NMR and mass spectral data. The compounds were also screened for antimicrobial and hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. The compounds, 6d and 6f were active against the selected panel of microbes and the former was the most potent one. This series showed less toxicity and may be considered for further biological screening and application trial except 6h and 6l, possessing higher cytotoxicity