The antidiabetic and antioxidant activities of the ethyl acetate-soluble extract (MFE) of mulberry fruit (Morus alba L.) were investigated. In vitro, MFE showed potent α-glucosidase inhibitory ...activity and radical-scavenging activities against DPPH and superoxide anion radicals. In vivo, MFE could significantly decrease fasting blood glucose (FBG) and glycosylated serum protein (GSP), and increase antioxidant enzymatic activities (SOD, CAT, GSH-Px) in streptozotocin (STZ)-induced diabetic mice. Bioactivity-guided fractionation of the MFE led to the isolation of 25 phenolic compounds, and their structures were identified on the basis of MS and NMR data. All the 25 compounds were isolated from mulberry fruit for the first time. Also, the α-glucosidase inhibitory activity and antioxidant activity of the phenolics were evaluated. Potent α-glucosidase inhibitory and radical-scavenging activities of these phenolics suggested that they may be partially responsible for the antidiabetic and antioxidant activities of mulberry fruit.
Harmine, a β-carboline alkaloid from Peganum harmala, has multiple anti-tumor activities, especially for its folk therapy for digestive system neoplasm. However, the underlying mechanism of harmine ...on gastric cancer remains unclear.
To illuminate the potential anti-tumor activity and mechanism of harmine against gastric cancer cells.
The anti-proliferative activity of harmine in vitro was evaluated by MTT assay. The autophagic activity induced by harmine was assessed using GFP-LC3 transfection. FITC/PI double staining was applied for the apoptosis inspection. The mitochondrial membrane potential was detected by JC-1 fluorescence probe. The potential mechanisms for proteins level in autophagy and apoptosis were analyzed by Western blot.
Harmine exhibited potent effects on both autophagy and apoptosis. Treatment with harmine could enhance dots of GFP-LC3 in cells. Meanwhile, the process had connection with Beclin-1, LC3-II, and p62 by the inhibition of Akt/mTOR/p70S6K signaling. However, high concentration of harmine led to apoptosis characterized by the propidium/Annexin V-positive cell pollution, cell shrunk and the collapse of mitochondrial membrane potential. The regulation of Bcl-2, Bax and the gathering of cleaved-PARP, cleaved-caspase 3 and cleaved-caspase 9 contributed to the induction of apoptosis. In addition, 10μM LY294002 (a specific inhibitor of PI3K/Akt) combination with 40μM harmine significantly increased the cytotoxicity to the gastric cancer cells and up-regulated both the apoptosis-related protein (cleaved-PARP, cleaved-caspase-3) and autophagy-related protein (Beclin-1, LC3-II, and p62). Adding the inhibitor of autophagy, 3-MA or BafA1, increased the viability of harmine-exposured gastric cancer cells, which confirmed the role of autophagy played in the gastric cancer cell death induced by harmine.
Harmine might be a potent inducer of apoptosis and autophagy, which offered evidences to therapy of harmine in gastric carcinoma in the folk medicine.
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Bioactivity-guided fractionation of Red Delicious apple peels was used to determine the chemical identity of bioactive constituents, which showed potent antiproliferative and antioxidant activities. ...Twenty-nine compounds, including triterpenoids, flavonoids, organic acids and plant sterols, were isolated using gradient solvent fractionation, Diaion HP-20, silica gel, and ODS columns, and preparative HPLC. Their chemical structures were identified using HR-MS and 1D and 2D NMR. Antiproliferative activities of isolated pure compounds against HepG2 human liver cancer cells and MCF-7 human breast cancer cells were evaluated. On the basis of the yields of isolated flavonoids (compounds 18−23), the major flavonoids in apple peels are quercetin-3-O-β-d-glucopyranoside (compound 20, 82.6%), then quercetin-3-O-β-d-galactopyranoside (compound 19, 17.1%), followed by trace amounts of quercetin (compound 18, 0.2%), (−)-catechin (compound 22), (−)-epicatechin (compound 23), and quercetin-3-O-α-l-arabinofuranoside (compound 21). Among the compounds isolated, quercetin (18) and quercetin-3-O-β-d-glucopyranoside (20) showed potent antiproliferative activities against HepG2 and MCF-7 cells, with EC50 values of 40.9 ± 1.1 and 49.2 ± 4.9 μM to HepG2 cells and 137.5 ± 2.6 and 23.9 ± 3.9 μM to MCF-7 cells, respectively. Six flavonoids (18−23) and three phenolic compounds (10, 11, and 14) showed potent antioxidant activities. Caffeic acid (10), quercetin (18), and quercetin-3-O-β-d-arabinofuranoside (21) showed higher antioxidant activity, with EC50 values of <10 μM. Most tested flavonoids and phenolic compounds had high antioxidant activity when compared to ascorbic acid and might be responsible for the antioxidant activities of apples. These results showed apple peel phytochemicals have potent antioxidant and antiproliferative activities.
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•Phytochemicals of mulberry fruit were conducted.•Three novels and forty-seven known compounds were isolated from mulberry fruit.•Some phenols showed potent anti-neuroinflammatory and ...antioxidant activities.•Mulberry fruit could serve as a healthy product for neuroinflammatory related diseases.
Mulberry (Morus alba L.) fruit is a delicious, fleshy, succulent berry, which is served as a famous fruit in many countries and as traditional herb in China. In our current study, three new (1, 44, 47) and forty-seven known compounds were isolated and identified from mulberry fruit. Anti-neuroinflammatory, antioxidant and antidiabetic activities of these compounds were evaluated in vitro. Compound 7 significantly inhibited nitric oxide (NO) production induced by lipopolysaccharides (LPS) in microglia cells (BV-2) with the IC50 value of 10.09 ± 0.51 μM. Compounds 1, 5, 7, and 14 dose-dependently reduced the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Simultaneously, they could block LPS-induced nuclear translocation of nuclear factor-κB (NF-κB). Moreover, phenols from mulberry fruit displayed evidently antioxidant and antidiabetic activities. These results suggested that reasonable consumption of mulberry might assist people to prevent and reduce the occurrence of neuroinflammatory and oxidative related diseases.
Tupistra chinensis is widely distributed in southwestern China and its rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis. Its chemical identity of potent ...antiproliferative and anti-inflammatory constituents has been carried out in this study. Twenty-three polyhydroxylated spirostanol saponins, including nine novels, were isolated and identified. The new spirostanol saponins were elucidated as spirost-25(27)-en-1β,2β,3β,4β,5β-pentol-2-O-β-D-xylopyranoside (1), spirost-25(27)- en-1β,2β,3β,4β,5β-pentol-2-O-α-L-arabinopyranoside (2), spirost-25(27)-en- 1β,3α,5β-triol (12), spirost-25(27)-en-1β,3α,4β,5β,6β-pentol (13), spirost-25(27)-en- 1β,2β,3β,5β-tetraol-5-O-β-D-glucopyranoside (16), 5β-spirost-25(27)-en-1β,3β-diol- 3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (17), (25R)-5β-spirostan- 1β,3β-diol-3-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranoside (18), (25R)-5β- spirostan-1β,3β-diol-3-O-β-D-fructofuranosyl-(2 → 6)-β-D-glucopyranoside (19), 5β-spirost-25(27)-en-3β-ol-3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (20). The antiproliferative effects against seven human cancer cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds. Compounds 17, 19 and 21 exhibited potential antiproliferative activities against all of human cancer cell lines tested. Compounds 21 showed significant inhibition on NO production with IC50 values of 11.5 μM. These results showed that the spirostanol saponins isolated from the dried rhizomes of T. chinensis have potent antiproliferative and anti-inflammatory activities and T. chinensis might be used as anticancer and.anti-inflammatory supplement.
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•Twenty bioactive compounds were isolated and identified from lychee seed.•Methyl jasmonate analogs were first isolated from lychee.•Antioxidant and anti-inflammatory activity of all ...compounds were evaluated.•The methyl jasmonate analogs show anti-inflammatory capacities.•Lignanoside and some flavonoids exhibit antioxidant effects.
Lychee (Litchi chinensis Sonn.) is a famous tropical fruit. While enjoying its delicacy, it also produces a lot of lychee seeds as waste. In this study, bioactive phytochemical study of the seeds of lychee led to the isolation and identification of four methyl jasmonate analogs (1–4), one lignanoside (5), together with fifteen flavonoids (6–20). Their chemical structures were established on the basis of spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR spectra. The anti-inflammatory and antioxidant activities were evaluated for the isolated compounds. Compounds 2 and 3 exhibited notable inhibition on NO production induced by lipopolysaccharides (LPS) in macrophages cell line RAW 264.7. Compound 5 and some flavonoids revealed potent antioxidant capacities. The results disclosed that the methyl jasmonates in lychee seeds may be partially responsible for anti-inflammatory activity of lychee and could be served as anti-inflammatory agent in functional food.
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•Bioactive phytochemicals of the mango leaves were investigated.•Four novels and eighteen known phenolics were isolated from mango leaves.•Some phenolics showed potent ...anti-inflammatory and antioxidant activities.•Mango leaves may be beneficial to metabolic related diseases.
Mango leaves (Mangifera indica L.) are a kind of crop waste and the present work is focusing on its bioactive constituents. Phytochemical study on the extract of mango leaves resulted in the isolation and identification of 5 benzophenones and 17 flavonoids. Among them, there were 4 new benzophenone glycosides, elucidated as 4′,6-dihydroxy-4-methoxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-β-fructopyranoside, 4,4′,6-trihydroxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-β-fructopyranoside, 4,4′,6-trihydroxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-β-fructofuranoside, and 2,4′,6-trihydroxy-4-methoxybenzophenone-3-C-(2-O-p-hydroxybenzoyl-p-hydroxybenzoyl)-α-d-galactoside, together with eighteen known compounds. The anti-inflammatory, antioxidant and α-glucosidase inhibitory activities of the isolated compounds were evaluated. The results displayed that some phenolics showed significant anti-inflammatory, antioxidant and antidiabetic activities. The study provided a phytochemical evidence for further development and utilization of mango leaves in health products.
•Bioactive phytochemicals of the roots of hairy fig were conducted.•Four new and twenty-five known phenolics were isolated from hairy fig.•The main phenolics were quantified by HPLC in the exact of ...hairy fig.•Some phenolics showed potent anti-inflammatory and antioxidant activities.•Hairy fig may be beneficial to inflammation related diseases.
The roots of hairy fig (Ficus hirta Vahl.), known as Cantonese ginseng, is widely used as a plant-derived popular food to improve fatigue resistance by Hakka people in southern China. In the current study, four new phenolics (17, 18, 22 and 24) along with twenty-five known congeners were isolated and purified from the roots of hairy fig. Their structures were elucidated by extensive spectroscopic analysis and chemical degradation. The antioxidant and anti-inflammatory activities of the purified compounds were also evaluated. Results indicated that some phenolics showed moderate antioxidant activity compared to those of l-ascorbic acid in DPPH and superoxide anion radical scavenging capacity assay. Most of the isolated compounds exhibited pronounced inhibitory effects on the lipopolysaccharides (LPS)-induced nitric oxide (NO) production in murine macrophage RAW264.7. The results strongly demonstrated that the phenolics may be partially responsible for the roots of hairy fig’s anti-inflammatory activity.
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•Bioactive phytochemicals of Chinese acorns were conducted.•Four new and thirteen known triterpenoids were isolated and identified.•All isolated triterpenoids showed potent ...anti-neuroinflammatory activities.•Chinese acorns may be beneficial to neuro-inflammation related diseases.
Chinese acorns are served as a healthy food supplementary and cuisine in the local residents. The anti-neuroinflammatory phytochemicals of Chinese acorns have been investigated in this study. Four new triterpenoids (1, 8, 16 and 17), together with thirteen known congeners (2–7, 9–15), were isolated and their structures were elucidated by spectroscopic analysis and chemical degradation. The isolated compounds were evaluated for anti-neuroinflammatory activity. Some triterpenoids showed obvious inhibitory effects on the production of nitric oxide (NO) induced by lipopolysaccharide (LPS) in microglia cells (BV-2). Compounds 1, 2, and 16 could dose-dependently reduce the expression levels of pro-inflammatory mediator iNOS, while compounds 1, 2, 8 and 16 could dose-dependently reduce the COX-2 expression induced by LPS in BV-2 cells. This study suggested that Chinese acorns could be served as healthy product for neuroinflammatory related diseases, such as Alzheimer’s disease.
A novel sodium borohydride/chloranil-based (SBC) assay for quantifying total flavonoids, including flavones, flavonols, flavonones, flavononols, isoflavonoids, flavanols, and anthocyanins, has been ...developed. Flavonoids with a 4-carbonyl group were reduced to flavanols using sodium borohydride catalyzed with aluminum chloride. Then the flavan-4-ols were oxidized to anthocyanins by chloranil in an acetic acid solution. The anthocyanins were reacted with vanillin in concentrated hydrochloric acid and then quantified spectrophotometrically at 490 nm. A representative of each common flavonoid class including flavones (baicalein), flavonols (quercetin), flavonones (hesperetin), flavononols (silibinin), isoflavonoids (biochanin A), and flavanols (catechin) showed excellent linear dose–responses in the general range of 0.1−10.0 mM. For most flavonoids, the detection limit was about 0.1 mM in this assay. The recoveries of quercetin from spiked samples of apples and red peppers were 96.5 ± 1.4% (CV = 1.4%, n = 4) and 99.0 ± 4.2% (CV = 4.2%, n = 4), respectively. The recovery of catechin from spiked samples of cranberry extracts was 97.9 ± 2.0% (CV = 2.0%, n = 4). The total flavonoids of selected common fruits and vegetables were measured using this assay. Among the samples tested, blueberry had the highest total flavonoid content (689.5 ± 10.7 mg of catechin equiv per 100 g of sample), followed by cranberry, apple, broccoli, and red pepper. This novel SBC total flavonoid assay can be widely used to measure the total flavonoid content of fruits, vegetables, whole grains, herbal products, dietary supplements, and nutraceutical products.
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