[1]. Vaughan RA, et al. β-alanine suppresses malignant breast epithelial cell aggressiveness through alterations in metabolism and cellular acidity in vitro. Mol Cancer. 2014 Jan 24; 13:14.
备注
以上数据均来自公开文献, Jinpan暂未进行独立验证, 仅供参考。 These protocols are for reference only. Jinpan does not independently validate these methods.
[1]. Jung M1, et al. Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. J Med Chem. 1999 Nov 4;42(22):4669-79. [2]. Weberpals JI, et al. The effect of the histone deacetylase inhibitor M344 on BRCA1 expression in breast and ovarian cancer cells. Cancer Cell Int. 2011 Aug 19;11(1):29
[1]. Alm A, et al. The effect of topical l-epinephrine on regional ocular blood flow in monkeys. Invest Ophthalmol Vis Sci. 1980 May;19(5):487-91. [2]. Simons FE, et al. First-aid treatment of anaphylaxis to food: focus on epinephrine. J Allergy Clin Immunol. 2004 May;113(5):837-44. [3]. Morris KA, et al. Epinephrine and glucose modulate training-related CREB phosphorylation in old rats: relationships to age-related memory impairments. Exp Gerontol. 2013 Feb;48(2):115-27. [4]. Callaway CW, et al. Epinephrine for cardiac arrest. Curr Opin Cardiol. 2013 Jan;28(1):36-42.
2-Benzoxazolinone (BOA), a well-known allelochemical with strong phytotoxicity, is a potential herbicidal candidate.[1] 2-Benzoxazolinone is an anti-leishmanial agent with an LC50 of 40 μg/mL against L. donovani[2]
IC50
LC50: 40 μg/mL (L. donovani)[2]
In Vitro
BOA induces oxidative stress in mung bean as indicated by increased generation of H2O2, enhanced LP and accumulation of endogenous PRO. It is accompanied by an upregulation of the activities of various scavenging enzymes—SODs, peroxidases, CATs and GR—in roots and leaves of mung bean in response to BOA exposure.[1] The LC50 values for BOA and pentamidine are 40 pg/ml and 39.8 pg/mi, respectively. BOA showed antileishmanial activity and compares well with pentamidine. [2]
激酶实验
For the BOA treatment, we followed the method used by Burgos and Talbert , wherein seeds germinated on a filter paper disc moistened with BOA and grow until the measurement of seedling length. Seeds of mung bean were surface sterilized with sodium hypochlorite (0.1%, w/v) followed by washing with distilled water three times. These were subjected to germination in 15 cm diameter Petri dishes lined with a Whatman no. 1 filter circle and moistened with 7 ml of respective BOA treatment solution or distilled water (control). The 7 ml of the 0.1, 0.5, 1.0, 2.5, and 5.0 mM BOA solution used cor_x005frespond to nearly 0.0946, 0.473, 0.946, 2.365, 4.73 mg ml–1 BOA, respectively. It was in the range similar to that used by Burgos and Talbert [13]. Twenty-five mung bean seeds were used in each Petri dish. Five replicates were maintained for each treatment in a completely randomized manner. All the Petri dishes were placed in a seed germinator maintained at 25 ± 2 °C, 75 ± 3% relative humidity and a 16 h:8 h light: dark photoperiod with a photosynthetic photon flux density of 150 μmol m–2 s–1. After 7 days, root and shoot length of emerged seedlings from each treatment were measured. Further, roots and leaves from each treatment were harvested and stored at –80 °C prior to enzyme extraction and other estimations.[1]
SMILES
O=C1OC2=CC=CC=C2N1
靶点
Parasite
细胞实验
Promastigote para- sites in the stationary phase of growth (1 x io parasite/mi) were inoculated into culture tubes containing BHI-agar as solid part and HBSS as hquid part. To these tubes different concentrations (10 to 100 pg/mi, DMSO/PBS) of BOA and pentamidine were added, respectively. The inhibitory effect of BOA was compared with pentamidine which is known to be active against leishmaniasis, and with untreated control cultures. The whole operation was carried out aseptically in an ultraviolet chamber and the tubes were incubated for 5 days at 22 °C. The toxicity of DMSO was determined by adding different amounts of solvent (0.1 to 1.5%) to suspensions of promastigotes under the conditions described above. After five days the value of the non-toxic dilution was found to be 0.6% and growth inhibition (up to 15%) was observed between 0.6% and 1 %; therefore, higher concentrations of DMSO were never used. Antileishmanial activity of each of the com_x005fpounds was determined by counting the number of live parasites per field microscopically. The LC55 values were calculated by probit analysis and no mortallty was observed in mice when BOA was administered ((p.) in the doses ranging from 0.25—1 g/kg. The mice were kept under observation for one week.[2]
数据来源文献
[1] Batish D R , Singh H P , Setia N , et al. 2-Benzoxazolinone (BOA) induced oxidative stress, lipid peroxidation and changes in some antioxidant enzyme activities in mung bean (Phaseolus aureus).[J]. Plant Physiol Biochem, 2006, 44(11-12):819-827. [2]. Kapil A, et al. Leishmanicidal activity of 2-benzoxazolinone from Acanthus illicifolius in vitro. Planta Med. 1994 Apr;60(2):187-8.
小鼠[1]将6周龄小鼠用3-氨基-2-甲基丙酸(BAIBA:100mg / kg /天)处理或保持未处理(对照小鼠)。每周监测它们的重量[1]。
数据来源文献
[1]. Roberts LD, et al. β-Aminoisobutyric acid induces browning of white fat and hepatic β-oxidation and is inversely correlated with cardiometabolic risk factors. Cell Metab. 2014 Jan 7;19(1):96-108.
[1]. Searcey M, et al. Synthesis, DNA-cleaving properties and cytotoxicity of intercalating chelidamic acid derivatives. Anticancer Drug Des. 13(8):837-55. [2]. Espinet P, et al. Mesogenic palladium complexes with pincer ligands derived from dipicolinic acid. Inorg Chem. 2000 Aug, 7;39(16):3645-51. [3]. Porter TG, et al. Chelidonic acid and other conformationally restricted substrate analogues as inhibitors of rat brain glutamate decarboxylase. Biochem Pharmacol. 1985 Dec 1;34(23):4145-50.