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Breast cancer has become the most prevalent malignant tumor among women, putting the health of women at serious risk. Screening for lead compounds in the active ingredients of plant that are effective and less toxic continues to be an important strategy for treating breast cancer. Gerbeloid J, a coumarin isolated from Gerbera piloselloides (L.) Cass., showed significant anti-cancer activity. But there is no report on the effect and mechanism of gerbeloid J on cycle and apoptosis of breast cancer. By using the CCK-8, clone formation, and PI staining assays, the effects of gerbeloid J on the proliferation of MCF-7 and MDA-MB-231 cells were assessed in this study. The effects of gerbeloid J on the apoptosis and mitochondrial function of MCF-7 and MDA-MB-231 cells were assessed using DAPI, Annexin V/TO-PRO-3, Rhod-2 AM, TMRM, DCFDA staining assays, and Western blot. The results demonstrated that gerbeloid J regulated the P21/CDC25C/CDK-1/cyclin B1 pathway and arrested the cell cycle at G2/M phase to suppressed the proliferation of MCF-7 and MDA-MB-231 cells. Additionally, gerbeloid J induced apoptosis through the stimulation of mitochondrial calcium excess, reduction of mitochondrial membrane potential, and promotion of ROS generation, and its mechanism was related to the activation of mitochondrial apoptotic pathway. In conclusion, by regulating the P21/CDC25C/CDK-1/cyclin B1 pathway and activating the mitochondrial apoptosis pathway, gerbeloid J could cause breast cancer cell cycle arrest and apoptosis, which might offer a promising candidate for the creation of new drugs against breast cancer.
RESUMEN
OBJECTIVE To improve th e quality standard for Gerbera piloselloides. METHODS The properties of G. piloselloides were observed and microscopic identification was conducted for powder. The moisture ，total ash ，acid-insoluble ash and ethanol-soluble extract were detected according to the method stated in 2020 edition of Chinese Pharmacopoeia （part Ⅳ）. The contents of nodakenin，luteolin-7-O-β-D-lutinoside，luteoloside，apigenin-7-O-β-D-lutinoside，apigenin-7-O-β-D-glucopyranoside and marmesin were determined by high performance liquid chromatography method. RESULTS G. piloselloides were shrunken ，densely covered with thick white cotton wool ，with many fibrous roots ；the surface was taupe or gray-brown ；its texture was brittle and easy to break ；the cross section was yellow-white ，and there was an obvious small wooden heart in the center. Its powder was tan ， and non-glandular hairs ，stone cells ，calcium oxalate cubes ，ducts，fibers could be seen unde r microscope. The measured values of moisture，total ash ，acid-insoluble ash and alcohol-soluble extract ， for 15 batches of samples were 8.63％-11.34％，10.39％-14.93％， 3.29％-6.37％ and 9.03％-15.02％，respectively；average values were 10.01％，12.26％，4.61％，12.36％. The linear ranges of nodakenin，luteolin-7-O-β-D-rutinoside，luteoloside，apigenin- 7-O-β-D-lutinoside，apigenin-7-O-β-D-glucopyranoside and marmesin we re 3.87-154.88，1.64-65.41，1.60-64.00，1.92-76.96， 1.27-50.93，0.40-15.89 μg/mL，respectively（r≥0.999 1）. RSDs of precision ，stability（24 h）and repeatability tests were all less than 3％. The average recoveries were 101.88％，100.89％，102.64％，95.75％，96.71％ and 103.48％，respectively；RSDs were 0.55％，0.43％，0.34％，0.49％，0.47％ and 0.37％，respectively（n＝6）；the contents of above 6 components were 0.152 7-0.852 2， 0.084 5-0.669 7，0.136 7-0.961 0，0.126 0-1.193 2，0.128 8-1.102 2，0.046 9-0.678 0 mg/g. CONCLUSIONS The established method can be used for the quality control of G. piloselloides . It is preliminarily proposed that the moisture in G. piloselloides is not more than 12.0％；the total ash is not more than 15.0％，the acid-insoluble ash is not more than 6.0％，the alcohol-soluble extract is not less than 9.0％；the contents of luteoloside and apigenin- 7-O-β-D-glucopyranoside are not less than 0.016％.
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Ten compounds were isolated from the 95% ethanol extract of the whole plant of Gerbera piloselloides by silica gel column chromatography, MCI column chromatography and semi-preparative HPLC methods. Their structures were identified on the basis of physicochemical properties, spectral data (UV, IR, MS and NMR), circular dichroism (CD) spectra and single crystal X-ray diffraction analysis as 3′R-gerpilosecoumarin A (1a), 3′S-gerpilosecoumarin A (1b), gymnastone (2), gerberinside (3), divaricataester C (4), luteolin (5), caffeic acid methyl ester (6), ethyl chlorogenate (7), 6-(β-D-glucopyranosyloxy)-7-methoxy-5-benzoranpropanoic acid methyl ester (8) and glucozaluzanin C (9). Among them, new compounds 1a and 1b were new compounds and optical enantiomers, which were obtained by chiral resolution, and their absolute configurations were determined by quantum chemical calculation ECD. Compounds 1 and 1a/1b significantly increased the survival of IEC-6 in rat small intestinal crypt epithelial cells after LPS injury.
RESUMEN
Object To study the chemical constituents from the roots of Gerbera piloselloides Cass Methods The compounds were isolated using RA polystyrene resin and silica gel column chromatography, and the structures of these compounds were elucidated by means of spectral analysis Results Arbutin, daphnetin 8 O ? D glucopyranoside, 2, 6 dimethoxy 4 hydroxyphenol 1 O ? D glucopyranoside, koaburaside, glucosyringic acid, marmesinin were elucidated Conclusion Compounds Ⅱ Ⅵ were isolated from Gerbera L ex Cass for the first time