Oridonin prevents oxidative stress-induced endothelial injury via promoting Nrf-2 pathway in ischaemic stroke.

Oridonin, a natural diterpenoid compound extracted from a Chinese herb, has been proved to exert anti-oxidative stress effects in various disease models. The aim of the present study was to investigate the protective effects of oridonin on oxidative stress-induced endothelial injury in ischaemic stroke. We found oridonin repaired blood-brain barrier (BBB) integrity presented with upregulation of tight junction proteins (TJ proteins) expression, inhibited the infiltration of periphery inflammatory cells and neuroinflammation and thereby reduced infarct volume in ischaemic stroke mice. Furthermore, our results showed that oridonin could protect against oxidative stress-induced endothelial injury via promoting nuclear translocation of nuclear factor-erythroid 2 related factor 2 (Nrf-2). The specific mechanism could be the activation of AKT(Ser473)/GSK3ß(Ser9)/Fyn signalling pathway. Our findings revealed the therapeutic effect and mechanism of oridonin in ischaemic stroke, which provided fundamental evidence for developing the extracted compound of Chinese herbal medicine into an innovative drug for ischaemic stroke treatment.

A Review on Annona squamosa L.: Phytochemicals and Biological Activities.

Annona squamosa L. (Annonaceae) is a fruit tree with a long history of traditional uses. A. squamosa is an evergreen plant mainly located in tropical and subtropical regions. Srikayas, the fruits of A. squamosa, are extensively used to prepare candies, ice creams and beverages. A wide range of ethno-medicinal uses has been related to different portions of A. squamosa, such as tonic, apophlegmatisant, cool medicine, abortient and heart sedative. Numerous research projects on A. squamosa have found that it has anticancer, anti-oxidant, antidiabetic, antihypertensive, hepatoprotective, antiparasitic, antimalarial, insecticidal, microbicidel and molluscicidal activities. Phytochemistry investigations on A. squamosa have considered annonaceous acetogenins (ACGs), diterpenes (DITs), alkaloids (ALKs) and cyclopeptides (CPs) as the main constituents. Until 2016, 33 DITs, 19 ALKs, 88 ACGs and 13 CPs from this species were reported. On the basis of the multiple researches on A. squamosa, this review strives to integrate available information on its phytochemicals, folklore uses and bioactivities, hoping to promote a better understanding of its medicinal values.

Antitumor activity of Annona squamosa seed oil.

CONTEXT: Custard apple (Annona squamosa Linn.) is an edible tropical fruit, and its seeds have been used to treat "malignant sore" (cancer) and other usage as insecticide. A comparison of extraction processes, chemical composition analysis and antitumor activity of A. squamosa seed oil (ASO) were investigated. MATERIALS AND METHODS: The optimal extraction parameters of ASO were established by comparing percolation, soxhlet, ultrasonic and SFE-CO2 extraction methods. The chemical composition of fatty acid and content of total annonaceous acetogenins (ACGs) of ASO was investigated by GC-MS and colorimetric assay, and anti-tumor activity of ASO was tested using H22 xenografts bearing mice. RESULTS: The optimal extraction parameters of ASO were obtained as follows: using soxhlet extraction method with extraction solvent of petroleum ether, temperature of 80°C, and extraction time of 90min. Under these conditions, the yield of ASO was 22.65%. GC-MS analysis results showed that the main chemical compositions of fatty acid of ASO were palmitic acid (9.92%), linoleic acid (20.49%), oleic acid (56.50%) and stearic acid (9.14%). The total ACGs content in ASO was 41.00mg/g. ASO inhibited the growth of H22 tumor cells in mice with a maximum inhibitory rate of 53.54% by oral administration. Furthermore, it was found that ASO exerted an antitumor effect via decreasing interleukin-6 (IL-6), janus kinase (Jak) and phosphorylated signal transducers and activators of transcription (p-Stat3) expression. DISCUSSION AND CONCLUSION: The results demonstrated that ASO suppressed the H22 solid tumor development may due to its main chemical constituents unsaturated fatty acid and ACGs via IL-6/Jak/Stat3 pathway. ASO may be a potential candidate for the treatment of cancer.

[Structure activity relationship of annonaceous acetogenins against multidrug resistant human lung cancer cell line A549/Taxol in vitro].

10 kinds of annonaceous acetogenins were selected for antitumor activity testing against human lung cancer cell line A549/Taxol and the structure activity relationship was analyzed.MTT assay was used to detect the inhibitory activities of 10 kinds of annonaceous acetogenins and positive drugs against A549/Taxol cells, respectively uvariamicin-Ⅲ(1), uvariamicin-Ⅱ(2), annosquacin D(3), desacetyluvaricin(4), annosquatin A(5), squamostatin D(6), bullatacin(7), squamocin(8), motrilin(9), annosquatin B(10), verapamil and cisplatin. Annonaceous acetogenins showed significant inhibitory activities against A549/Taxol cells, and were more potent than the positive drug verapamil and cisplatin.The more carbon atoms between the tetrahydrofuran ring and the lactone ring of annonaceous acetogenins exhibited more potency.Besides,ACGs with two substituted hydroxyl showed more potency than the compounds with three substituted hydroxyl in the bis-adjacent-THF ACGs. Furthermore, ACGs with three substituted hydroxyl showed more potency than the compounds with four substituted hydroxyl among the no bis-adjacent-THF ACGs.

[Low Polar Constituents from Annona squamosa Fruit Pericarp].

OBJECTIVE: To study the low polar constituents from Annona squamosa fruit pericarp. METHODS: The fruit pericarp was percolated with 95% EtOH at room temperature. The extract was subjected to Silica gel chromatography and eluted with gradually more polar and EtOAc-MeOH mixtures. The part eluted range Pet-EtOAc from 5:1 to 1:1 was subjected to repeated column chromatography. The constituents were identified by physicochemical property and NMR data. RESULTS: Eight constituents were isolated and identified as tricosane(1), ß-sitosterol(2), succinic acid (3), annosquamosin D(4), 4α-hydroxy-19-nor-(E)-kauran-17-oic acid(5), (E)-16ß, 17-dihydroxy-kauran-19-oic acid(6), (E)-16α, 17-dihydroxy-kauran-19-oic acid(7), and 16ß-hydroxy-17-acetoxy-(E)-kauran-19-oic acid(8). CONCLUSION: All constituents are firstly isolated from Annona squamosa fruit pericarp except compound 6.

[Studies on chemical constituents from seed of Psoralea corylifolia].

OBJECTIVE: To study the chemical constituents of Psoralea corylifolia. METHOD: Chromatographic methods were used to separate compounds, and spectroscopic methods were used to determine the structures. RESULT: Five compounds were isolated and identified as furano (2", 3", 7, 6)-4'-hydroxyflavanone (1), psoralidin (2), genistein (3), psoralen (4), isopsoralen (5). CONCLUSION: Compounds 1 was a new compound named psoraleflavanone. And 13C-NMR data of compound 2 were assined for the first time.