ABSTRACT
Three new biflavones, apigenin-(3',8â³)-chrysin (1), (2S)-2,3-Dihydroametoflavone 5,4'-dimethyl ether (2), and (2S)-5â³,7â³-Dihydroxy-2â³-phenoxychromonyl-(4'â³,3')-naringenin (3), together with seven known biflavones (4-10) were isolated from the 75% EtOH extract of Selaginella doederleinii. The structures of new compounds were established by application of spectroscopic methods, including 1D and 2D NMR, HRMS, and CD measurements. In addition, all new compounds were evaluated for their cytotoxic potential against three human cancer cell lines A549, MCF-7, and SMMC-7721 in vitro. Compound 2 exhibited potent cytotoxic activity with IC50 values ranging from 6.35 to 10.18 µM.
Subject(s)
Flavones/pharmacology , Selaginellaceae/chemistry , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Apigenin/chemistry , Apigenin/pharmacology , Cell Death/drug effects , Cell Line, Tumor , Flavanones/chemistry , Flavones/chemistry , Flavonoids/chemistry , Flavonoids/pharmacology , Humans , Magnetic Resonance Spectroscopy , Plant Extracts/chemistryABSTRACT
OBJECTIVE: To observe the regulatory effect of Chinese drugs for stasis removing and collaterals dredging (CDSRCD) on the expressions of podocin and CD2AP in podocyte slit diaphragm (SD) of diabetic nephropathy (DN) rats. METHODS: DN rat model was duplicated in 40 male Sprague- Dawley rats by feeding high fat high glucose diet combined with intraperitoneally injecting 1 % streptozoto- cin (STZ, 35 mg/kg). Totally 36 successfully modeled rats were divided into the model group, the CD- SRCD group,- and the irbesartan group according to random digit table, 12 in each group. Besides, anoth- er 10 normal rats were recruited as a normal group. Rats in the CDSRCD group and the irbesartan group were intragastrically fed with CDSRCD and irbesartan respectively. Rats in the normal group and the mod- el group were fed with equal volume of distilled water at the same time. 24 h urine protein quantitation was detected using ELISA at various time points. Body weight (BW) , kidney weight ( KW), kidney index (KI) , fasting blood glucose (FBG) , serum creatinine (SCr), blood urea nitrogen (BUN), and uric acid (UA) in each group were detected after 16 weeks of intervention. The pathomorphological changes of re- nal tissue were observed under light microscope and electron microscope respectively. The protein and mRNA expressions of podocin and CD2AP were detected by Western blot and Real-time PCR respectively. RESULTS: (1) Compared with the normal group, 24 h urine protein quantitation significantly increased at week 4, 8, 12, and 16, respectively (P <0. 01). BW was decreased; KI and levels of FBG, SCr, BUN, and UA all increased after modeling (P <0. 01). Compared with the model group, 24 h urine protein quan- titation significantly decreased in the CDSRCD group and the irbesartan group at week 4, 8, 12, and 16, respectively (P <0. 01). Besides, it was more obviously reduced in the CDSRCD group than in the irbe- sartan group (P <0. 05, P <0.01). BUN level obviously decreased both in the CDSRCD group and the irbesartan group after modeling (P <0. 05, P <0. 01). (2) Results of renal pathology showed that disar- ranged renal structure, obviously thickened basement membrane, severely proliferated mesenteria, widely fused foot processes in the model group. All these pathological changes were attenuated in the CD- SRCD group and the irbesartan group to some degree. (3) Results of Western blot and Real-time PCR showed, compared with the normal group, protein and mRNA expressions of podocin and CD2AP decreased in the model group (P <0. 01). Compared with the model group, protein and mRNA expressions of podocin and CD2AP increased in the CDSRCD group and the irbesartan group (P <0. 01). Protein and mRNA expressions of podocin and CD2AP increased more in the CDSRCD group than in the irbesartan group (P <0. 05). CONCLUSIONS: CDSRCD could protect renal function by lowering urinary protein in DN rats, improve renal pathological changes. Its mechanism might be related to up-regulating mRNA and protein expressions of podocin and CD2AP.
Subject(s)
Diabetic Nephropathies , Drugs, Chinese Herbal , Intracellular Signaling Peptides and Proteins , Membrane Proteins , Podocytes , Animals , Diabetes Mellitus, Experimental , Diaphragm/metabolism , Drugs, Chinese Herbal/pharmacology , Intracellular Signaling Peptides and Proteins/metabolism , Kidney , Male , Membrane Proteins/metabolism , Rats , Rats, Sprague-DawleySubject(s)
Acupuncture Analgesia , Back Pain/therapy , Intervertebral Disc Displacement/therapy , Moxibustion , Adult , Aged , Combined Modality Therapy , Female , Humans , Lumbosacral Region , Male , Middle AgedABSTRACT
The accumulation of H2O2 by NaCl was observed in the roots of rice seedlings. Treatment with NaCl caused an increase in the activities of ascorbate peroxidase (APX) and glutathione reductase (GR) and the expression of OsAPX and OsGR in rice roots. Exogenously applied H2O2 also enhanced the activities of APX and GR and the expression of OsAPX and OsGR in rice roots. The accumulation of H2O2 in rice roots in response to NaCl was inhibited by the NADPH oxidase inhibitors, diphenyleneiodonium chloride (DPI) and imidazole (IMD). However, DPI, IMD, and dimethylthiourea, a H2O2 trap, did not reduce NaCl-enhanced activities of APX and GR and expression of OsAPX and OsGR. It appears that H2O2 is not involved in the regulation of NaCl-induced APX and GR activities and OsAPX and OsGR expression in rice roots.