ABSTRACT
A series of new hybrids of dehydroandrographolide (TAD), a biologically active natural product, bearing nitric oxide (NO)-releasing moieties were synthesized and designated as NO-donor dehydroandrographolide. The biological activities of target compounds were studied in human erythroleukemia K562 cells and breast cancer MCF-7 cells. Biological evaluation indicated that the most active compound I-5 produced high levels of NO and inhibited the proliferation of K562 (IC 1.55 μmol·L) and MCF-7 (IC 2.91 μmol·L) cells, which were more potent than the lead compound TAD and attenuated by an NO scavenger. In conclusion, I-5 is a novel hybrid with potent antitumor activity and may become a promising candidate for future intensive study.
Subject(s)
Humans , Antineoplastic Agents , Chemistry , Cell Proliferation , Diterpenes , Chemistry , Pharmacology , Drug Design , Drug Screening Assays, Antitumor , K562 Cells , MCF-7 Cells , Nitric Oxide , Chemistry , Pharmacology , Structure-Activity RelationshipABSTRACT
A series of new hybrids of dehydroandrographolide (TAD), a biologically active natural product, bearing nitric oxide (NO)-releasing moieties were synthesized and designated as NO-donor dehydroandrographolide. The biological activities of target compounds were studied in human erythroleukemia K562 cells and breast cancer MCF-7 cells. Biological evaluation indicated that the most active compound I-5 produced high levels of NO and inhibited the proliferation of K562 (IC 1.55 μmol·L) and MCF-7 (IC 2.91 μmol·L) cells, which were more potent than the lead compound TAD and attenuated by an NO scavenger. In conclusion, I-5 is a novel hybrid with potent antitumor activity and may become a promising candidate for future intensive study.
Subject(s)
Humans , Antineoplastic Agents , Chemistry , Cell Proliferation , Diterpenes , Chemistry , Pharmacology , Drug Design , Drug Screening Assays, Antitumor , K562 Cells , MCF-7 Cells , Nitric Oxide , Chemistry , Pharmacology , Structure-Activity RelationshipABSTRACT
AIM: To evaluate the effect of flavored Siwu granules in the clinical adjuvant treatment for phlegm and blood stasis mutual junction retinal vein occlusion. METHODS: Sixty patients (60 eyes) were randomly divided into treatment group and control group, both with retinal laser photocoagulation and intravitreal injection of triamcinolone acetonide, but the treatment group used flavored siwu granules. Vision, fundus change, fundus fluorescein angiography, clinical syndrome of traditional Chinese medicine ( TCM ), hemorheology examination and safety assessment were evaluated before and 8wk after treatment. RESULTS: At 8wk after treatment, there were differences on vision improvement, retinal circulation time, whole blood low shear viscosity and total efficient rate of clinical syndrome of TCM, compared with control group(PCONCLUSION: Flavored siwu granules adjuvant for phlegm and blood stasis mutual junction retinal vein occlusion can improve visual acuity and reduce the eye complications.