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Flavonoids are by far the most dominant class of phenolic compounds isolated from Morus alba leaves (MAL). Other classes of compounds are benzofurans, phenolic acids, alkaloids, coumarins, chalcones and stilbenes. Major flavonoids are kuwanons, moracinflavans, moragrols and morkotins. Other major compounds include moracins (benzofurans), caffeoylquinic acids (phenolic acids) and morachalcones (chalcones). Research on the anticancer properties of MAL entailed in vitro and in vivo cytotoxicity of extracts or isolated compounds. Flavonoids, benzofurans, chalcones and alkaloids are classes of compounds from MAL that have been found to be cytotoxic towards human cancer cell lines. Further studies on the phytochemistry and anticancer of MAL are suggested. Sources of information were PubMed, PubMed Central, ScienceDirect, Google, Google Scholar, J-Stage, PubChem and China National Knowledge Infrastructure.
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Background: Benzofuran compounds are shown to have pharmacological properties such as antiarrhythmic, antidepressant, antifungal, and antibacterial activity. Some studies conducted on them have revealed that they are having anti-inflammatory property also. Hence, we carried out this study to know whether the benzofuran compound 3, 4-dihydro 4-oxo-benzofuro (3, 2-d) pyrimidine-2-propionic acid has got anti-inflammatory activity against chronic inflammation. Methods: Wistar albino rats were treated with benzofuran compound under study and phenylbutazone in the dose of 100 mg\kg, orally with 2% gum acacia as suspending agent and the effects were observed in chronic experimental model of inflammation namely, cotton pellet induced granuloma model. Results: In the present study, it was shown that the benzofuran compound under study has got significant anti-inflammatory activity against the chronic model of inflammation. Conclusion: Our experiment shows that the benzofuran compound under study has got significant anti-inflammatory activity and may, as well become an additional anti-inflammatory drug if further studies are conducted in this direction involving human beings.
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Objective To investigate the effect of butylphthalide on brain edema and the expression of phosphorylated myosin light chain in peri-infarct tissue in focal cerebral ischemic rats.Methods A total of 212 adult male Sprague-Dawley rats were divided into a sham operation group (n =12),a cerebral ischemia group (n =100),and a butylphthalide group (n =100) (40 mg/kg,1/day,gavage) according to the random number table.Both the cerebral ischemia group and the butylphthalide group were redivided into 6 h,12 h,1 d,3 d,and 7 d groups (n =20 for each time point).A rat model of focal cerebral ischemic model was induced by photochemical method; 2,3,5-triphenyl tetrazolium chloride (TTC) staining was used to detect infarct volume (n =5); wet-dry weight method was used to detect the water content in brain tissue (n =5);immunohistochemistry (n =5) and Western blot (n =5) were used to detect the protein expression of periinfarct cortical p-MLC.Results TTC staining showed that no infarcts were observed in the sham operation group.The infarct volumes at each time points in the butylphthalide group were significantly less than those at the same time points in the cerebral ischemia group (all P ＜0.05).Wet-dry weight method showed that the water contents in brain tissue in the cerebral ischemia group and the butylphthalide group were significantly higher than that in the sham operation group (all P ＜ 0.05),but the water contents in brain tissue at each time points in the butylphthalide group was significantly lower than those at the same time points in the cerebral ischemia group (all P ＜ 0.05).Both immunohistochemistry and Western blot showed that the expressions of peri-infarct cortical p-MLC in both the cerebral ischemia group and the butylphthalide group were upregulated significantly compared to the sham operation group (all P＜ 0.05),but the expressions of peri-infarct cortical p-MLC at each time points in the butylphthalide group was significantly lower than those at the same time points in the cerebral ischemia group (all P＜ 0.05).Conclusions Butylphthalide can be up-regulated by reducing the expression of p-MLC caused by cerebral ischemia and reduce cerebral edema,and then reduce the infarct volume,and thus play a neuroprotective effect.
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Objective To investigate the effect of butylphthalide and sodium chloride injection postconditioning on focal cerebral ischemia-reperfusion (I/R) injury and endoplasmic reticulum stress in rats.Methods Thirty-six male SPF Sprague-Dawley rats,aged 2-3 months,weighing 260-280 g,were randomly divided into 3 groups (n =12 each):sham operation group (group S),focal cerebral I/R group (group I/R) and butylphthalide and sodium chloride injection postconditioning group (group Buty).The animals were anesthetized with intraperitoneal 10 ％ chloral hydrate 300 mg/kg.Focal cerebral I/R was induced by occluding right middle cerebral artery for 2 h followed by 24 h reperfusion in I/R and Buty groups.Butylphthalide and sodium chloride injection 2.5 mg/kg was injected via the tail vein immediately after onset of reperfusion in Buty group,while the equal volume of normal saline was injected in I/R group.Neurological deficits were assessed and scored at 24 h of reperfusion,and then the brain was isolated for detection of neuronal apoptosis (by TUNEL) and the expression of glucose-regulated protein 78 (GRP78) and caspase-12 in ischemic cerebral cortex (by immunohistochemistry) in brain tissues.Apoptosis index was calculated.Results Compared with group S,the neurological deficit scores and apoptosis index were significantly increased,and the expression of GRP78 and caspase-12 was up-regulated in I/R and Buty groups (P ＜ 0.05 or 0.01).Compared with group I/R,the neurological deficit scores and apoptosis index were significantly decreased,the expression of GRP78 was up-regulated,and the expression of caspase-12 was down-regulated in group Buty (P ＜ 0.05).Conclusion Butylphthalide and sodium chloride injection postconditioning can reduce focal cerebral I/R injury in rats,and inhibition of endoplasmic reticulum stressmediated cell apoptosis is involved in the mechanism.
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Objective To investigate the effects of butylphthalide on brain edema,blood-brain barrier permeability and RhoA expression in cortex in focal cerebral infarction in rats.Methods A total of 220 male Sprague Dawley rats were divided into a control,a model and a butylphthalile group (40 mg/kg,once a day,gavage) according to the random number table method.A model of rat focal cerebral infarction was induced by photochemical method.At 3,12,24,72,and 144 h after modeling,wet-dry weight method and Evans blue extravasation method were used to detect the brain water content and blood-brain barrier permeability.At 24 h after modeling,immunohistochemical staining and Western blot were used to detect the expression of RhoA protein in the periinfarction cortex.Results Compared to the control group,the brain water content (except at 6 h) and blood-brain barrier permeability in the model group and the butylphthalide group were increased significantly (all P ＜ 0.05).The immunohistochemical staining and Western blot suggested that the RhoA expression in the periinfarction cortex was upregulated significantly (all P ＜ 0.05).Compared to the model group,the brain water content and blood-brain barrier permeability at different time points in the butylphthalide group were decreased significantly (all P ＜ 0.05).The expression levels of RhoA were also decreased significantly (P ＜ 0.05).Conclusions Butylphthalide may reduce the brain edema of focal cerebral infarction in rats,inhibit disruption of the blood-brain barrier,and down-regulate the expression of RhoA.
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Objective To investigate the protective effect of butylphthalide for focal cerebral ischemiareperfusion injury and its possible mechanism.Methods A total of 60 healthy and clean adult Sprague-Dawley rats were randomly divided into sham operation,saline control,low-dose butylphthalide and high-dose butylphthalide groups (n =15 in each group).A focal cerebral ischemia-reperfusion model was induced by the suture method.At the beginning of reperfusion,100 rng/kg and 400 mg/kg butylphthalide injection were injected intraperitoneally in the rats of the low-dose butylphthalide and high-dose butylphthalide groups; 0.5 ml/kg saline was injected intraperitoneally in rats of the sham operation and saline control groups.All the rats were sacrificed after 24 h of ischemia-reperfusion.Results The degree of neurological deficit in the low-dose butylphthalide (t =1.488,P =0.000) and high-dose butylphthalide (t =2.362,P =0.000) groups were significantly improved compared to the saline control group,in which the high-dose butylphthalide group was improved more significantly than the low-dose butylphthalide group (t =-0.873,P =0.000).The infarct volume in the low-dose butylphthalide (t =18.589,P =0.000) and high-dose butylphthalide (t =36.963,P =0.000) groups were reduced significantly compared to the saline control group,in which the infarct volume of the high-dose butylphthalide group was reduce more significantly than that of the low-dose butylphthalide group (t =-18.374,P =0.000).HE staining showed that neurons were sparse,there were a large number of degeneration and necrosis,cell space became larger,and the intercellular substances showed vacuolar changes.In the butylphthalide group,the neuronal degeneration and necrosis reduced significantly,the survival of nerve cells increased,and the improvement of the high-dose butylphthalide group was more remarkable.SOD activity of the low-dose and high-dose butylphthalide groups were increased significantly compared to the sham operation and saline control groups (all P ＜0.05),in which the SOD activity in the high-dose butylphthalide group was significantly higher than that in the low-mall dose butylphthalide group (t =80.199,P =0.000); The MDA levels in the low-dose and high-dose butylphthalide groups were decreased significantly compared to the sham operation and saline control groups (all P ＜ 0.05),in which the MDA level in the high-dose butylphthalide group was significantly lower than that in the low-dose butylphthalide group (t =-1.308,P=0.000).Conclusions The protective effect of butylphthalide on ischemia-reperfusion injury may be associated with the increased antioxidant activity.
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Objective To assess the efficacy and safety of dl-3-butylphthalide on the treatment of acute ischemic stroke. Methods A total of 197 patients who were in the period of 72 hours of first attack of ischemic stroke of internal carotid artery with NIHSS from 5 to 25 scores were enrolled in this multi-center, randomized, double-blind and aspirin-control study. Compound " Dan Shen" was used as a baseline therapy. Results Basical recovery plus significant improvement was seen in 74.7% of the patients in dl-3-butylphthalide group and 60.9% in aspirin group (CMH value 4.0,P=0.047);There was a significant improvement for dl-3-butylphthalide group regarding NIHSS total score, total score difference value and Barthel index on the day 11th and 21st after treatment compared with control group. The main adverse reaction of dl-3-butylphthalide was increased aminotransferase and mainly the slight increase of aspartate aminotransferase, by 4.34% and 0 respectively. Conclusion dl-3-butyiphthalide should be regarded as an effective and safe treatment for ischemic stroke and a treatment without severe side effects.
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Objective To study the benzofuran compounds from roots and rhizomes of Ligularia caloxantha, which is a folk medicine used in the Naxi Nationality in Yunnan Province. Methods Compounds were separated and purified by silica gel and Sephadex LH-20 column chromatography. Their structures were elucidated by physicochemical properties and spectral analysis. Results Eighit compounds are isolated from ethanolic extracts of the roots and rhizomes. They were identified as euparin (Ⅰ), 6-methoxy-euparin (Ⅱ), 4, 5-dimethoxy-2-hydroxybenzaldehyde (Ⅲ), 2-acetyl-5, 6-dimethyoxybenzofuran (Ⅳ), 4-hydroxyacetophenone (Ⅴ), 2-isopropenyl-5, 6-dimethoxy-2, 3-hydrocumaran (Ⅵ), 8?-hydroxy-7(11)-eremophilen-12, 8?-olide (Ⅶ), lupeol (Ⅷ). Conclusion All the eight compounds were obtained from L. caloxantha for the first time as benzofurans. Compounds Ⅰ and Ⅱ are two major ones with insecticide and insect food refusal-induced activities. That is the relative reason of L. caloxantha used for folk anti-insect.