ABSTRACT
Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.
Subject(s)
Humans , Acetamides , Chemistry , Pharmacology , Antineoplastic Agents , Chemistry , Pharmacology , Apoptosis , Carcinoma, Non-Small-Cell Lung , Pathology , Cell Line, Tumor , Drug Design , Inhibitory Concentration 50 , Molecular Structure , Structure-Activity RelationshipABSTRACT
<p><b>OBJECTIVE</b>To probe into a safe and effective method for treatment of functional ventricular premature, and develop a new preparation of Chinese herbs with high science and technique contents.</p><p><b>METHODS</b>Two hundred and thirty-eight cases were randomly divided into a slowly-releasing medication group (n = 118) and a western medicine group (n = 120). The slowly-control needle group were treated with intramuscular injection of slowly-releasing medication new type preparation made by proved recipe of Chinese herbs with replenishing and strengthening pectoral qi, and nourishing yin and tranquillization into Tanzhong (CV 17), Neiguan (PC 6), Xinshu (BL 15), Pishu (BL 20) and Feishu (BL 13) by a trocar to slowly release and control releasing of the medicine so as to maintain lasting stimulation; the western medicine group with oral administration of Rythmol, thrice daily, 150 mg each time.</p><p><b>RESULTS</b>The cured rate and the cured and markedly effective rate for the ventricular premature was 51.7% and 71.2% in the slowly-releasing medication group, which were significantly higher than 28.3% and 50.8% in the western medicine group (P < 0.001).</p><p><b>CONCLUSION</b>The slowly-releasing medication new type preparation has a better therapeutic effect on functional ventricular premature, with high safety.</p>
Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Acupuncture Points , Acupuncture Therapy , Methods , Delayed-Action Preparations , Medicine, Chinese Traditional , Ventricular Premature Complexes , TherapeuticsABSTRACT
The compound that distributes in the herbs with one common effect was named as "co-effect compound" (CEC). The CECs of three traditional Chinese medicine(TCM) effects, purgative, relieving pain and clearing heat, had been found and studied. A strong corresponding relationship was found between the pharmacological activities of CECs and the TCM effect they belong to. The study shows that it may be a feasible method to connect traditional effect of TCM with modem pharmacological activity.
