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Objective To observe the effect of Acanthus ilicifolius alkaloid A (HBOA) on PI3K/AKT/mTOR/p70S6K signaling pathway in rats with hepatic fibrosis induced by carbon tetrachloride (CCl4), and to explore the mechanism of action of HBOA against liver fibrosis. Methods Rats were randomly divided into normal group, model group, high, medium; and low-dose HBOA groups (100, 50, 25 mg/kg), and colchicine group (0.4 mg/kg). Except for the normal group, the rats in other groups were given with a 50% CCl4 olive oil solution twice a week for 12 weeks to induce a rat model of liver fibrosis. From the ninth week of modeling, the drug-administered group was given the corresponding test drug once daily for 4 weeks. After the experiment, the body mass change and liver index were calculated. The levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the liver homogenate of each group were detected. The protein expression of p-PI3K, p-Akt, p-mTOR, and p-p70S6K in liver tissue was detected by Western blotting. Results Compared with the model group, the body weight of mice of each drug-administered group was significantly increased, and the liver index, and ALT and AST levels were decreased in liver tissue. In addition, HBOA high and medium-dose groups significantly inhibited the protein expression of p-PI3K, p-Akt, p-mTOR, and p-p70S6K. Conclusion HBOA has a protective effect on hepatic fibrosis rats, and its mechanism may be related to the inhibition of PI3K/Akt/mTOR/p70S6K signaling pathway.
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Viral diseases caused by virus infection have the characteristics of strong pathogenicity, high incidence of disease and easy to produce drug resistance. At present, chemical drugs are commonly used in clinical treatment to fight viral diseases, but the therapeutic effect of chemical drugs is not significant and most of them have toxic and side effects, which are easy to cause secondary injury to patients. The complexity of the active ingredients of Chinese materia medica makes it play an antiviral role at multiple levels and targets. Marine traditional medicine species are rich and diverse, it has been suggested that they have good antiviral effect and low side effects. The development and application of marine Chinese materia medica with anti-virus effect will attract more attention in the future, and has a broad market prospect. In this paper, 250 kinds of marine Chinese materia medica with antiviral effect recorded in the book "Marine traditional Chinese medicine" were reviewed, hoping to provide some reference for the basic and clinical research of marine Chinese materia medica with antiviral effect.
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OBJECTIVE To study the bioactive phytochemicals in the leaves of A.ilicifolius against Hepatocellular carcinoma (HCC) through in silico, in vitro and in vivo studies. METHODS A. ilicifolius leaves were collected from Cuddalore District,Tamil Nadu,India.Authenticated by the Botanical Survey of India. The fresh leaves of A. ilicifolius were washed and shade dried at room temperature (28 ± 2)℃. The dried leaves were powdered by electrical blender.25 gms of A.ilicifolius leaf powder was used for methanol extraction in the Soxhlet apparatus.The Phytochemical compounds were analyzed by GC-MS and the structure was retrieved from PubChem.Totally,seven HCC target proteins were collected from literature, ligand and proteins were prepared for in silico molecular docking. HepG2 cell lines were used for in vitro (MTT assay). BALB/c mice were used for in vivo studies, the biochemical parameters and histopathological studies were carried out with standard procedure. RESULTS The phytochemical 26.27-Di (nor)-cholest-5, 7, 23-trien-22-ol, 3-methoxymethoxy exhibited maximum docking score against the HCC target protein C-Jun N-terminal kinase 1 (JNK 1) (-6.839798). MTT assay revealed that the extract at a concentration of 200 μg·mL-1,caused 60% cell death in HepG2 cell lines.Further animal studies using to injecting HCC induced BALB/c mice,restoration of haematological parameters and cells to normal was observed after 15 days of oral administration of the extract.These findings suggest the possibility of using A.ilicifolius leaves in the treatment of HCC.CONCLUSION The in silico,in vitro and in vivo studies indicated that the A.ilicifolius leaves had anticancereous activity against Hepatocellular carcinoma.There can be a possibility of synergistic activity of phytochemicals together against HCC.
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Aim To investigate anti-hepatic fibrotic mechanism of Acanthus ilicifolius alkaloid A ( HBOA ) involved in high mobility group box 1 ( HMGB1 ) . Methods A hepatic fibrosis model of rat was estab-lished by the olive oil of CCl4 for 12 weeks. Then, at the 8th week,the successful model rats were randomly divided into model control group, colchicine group, HBOA high-dose group and HBOA low-dose group. From the 9th week,the rats in each group were treated with the drugs daily for 4 weeks respectively. The changes of liver histopathology and collagen were ob-served by HE staining and Masson staining, and the serum indicators including aspartate aminotransferase (AST),alanine aminotransferase(ALT) , total biliru-bin ( T-BIL ) , HMGB1 , interleukin-1β( IL-1β) and tumor necrosis factor-α( TNF-α) were determined. Moreover , the protein of HMGB1 in liver was examined by immunohistochemistry, and the expression of HMGB1 mRNA was measured by real-time fluores-cence quantitative PCR. Results Compared with the model control group,HBOA high-dose and HBOA low-dose groups significantly attenuated the fibrotic degree induced by CCl4 , markedly decreased the levels of ALT, AST, T-BIL, HMGB1, IL-1β, TNF-α. Moreo-ver, the expression of HMGB1 protein and mRNA in liver was decreased. And furthermore, serum HMGB1 level had significant positive correlation with IL-1β, TNF-α,ALT,AST and T-BIL. Conclusion HBOA has beneficial effects against liver fibrosis in rat which is induced by CCl4 , the mechanisms may be related to the inhibition of inflammatory response to HMGB1 .
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Aim: The main aim of this study is to evaluate the anti-oxidant and antimicrobial activity of mangrove species and the development of the callus biomass. Study Design: This is the first comparative evaluation report of field grown root and tissue cultured root callus of mangrove on anti-oxidant and anti-bacterial activity. Acanthus ilicifolius, Calophyllum inophyllum and Excoecaria agallocha were tested in this present investigation. Place and Duration of Study: Centre of Advanced Study in Marine Biology, Faculty of Marine Sciences, Annamalai University, Parangipettai 608 502, Tamil Nadu, India. Between February 2012 and July 2013 Methodology: In order to develop callus biomass, a number of growth hormones were supplemented with the MS medium. Following the callus development, anti-oxidant and anti-microbial activities were tested with field grown root and its tissue cultured root callus of Acanthus ilicifolius, Calophyllum inophyllum and Excoecaria agallocha. This was confirmed by different anti-oxidant, anti-bacterial and minimum inhibitory concentration assays. Results: Maximum (89%) root callus biomass was obtained from Acanthus ilicifolius on MS medium fortified with 0.3+0.3 mg/L of 2,4-D and KIN. 2,4-D 0.3mg/L and BAP 0.5 mg/L showed the maximum callus from both Calophyllum inophyllum (81%), Excoecaria agallocha (58%). In addition anti-oxidant and anti-bacterial effect of root and root callus of these three species were tested. In this study the root callus materials of all the three species showed the best anti-oxidant anti-bacterial activities. Conclusion: The metabolites from mangroves are good remedy for number of health problems especially the enhanced level of metabolites through the tissue culture techniques. The present study confirmed the anti-oxidant and anti-bacterial effect of Acanthus ilicifolius, Calophyllum inophyllum, Excoecaria agallocha n root extract. This study will be a key to develop a new drug to achieve healthy life. especially the root callus materials showed the better activity when compared to the field grown plants.
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<p><b>OBJECTIVE</b>To investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius (A. ilicifolius).</p><p><b>METHODS</b>Antioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil (DPPH) method and cytotoxic assay was undertaken using brine shrimp lethal toxicity test.</p><p><b>RESULTS</b>A. ilicifolius flower contained terpenoid, phenolic compounds, and alkaloid. The methanol extract of A. ilicifolius flower showed the highest antiradical efficiency (AE=1.41×10(-3)) against DPPH radicals and the highest cytotoxicity (LC50=22 µg/mL) against brine shrimp nauplii.</p><p><b>CONCLUSIONS</b>It is suggested that active compounds of A. ilicifolius flower solved in methanol play a role to inhibit free radical activity and kill Artemia salina nauplii. The substances can be considered as potential antioxidant and cytotoxic agents as well as imminent candidate for cancer therapy.</p>
Subject(s)
Animals , Acanthaceae , Chemistry , Antioxidants , Pharmacology , Artemia , Biphenyl Compounds , Chemistry , Pharmacology , Cytotoxins , Toxicity , Flowers , Chemistry , Lethal Dose 50 , Picrates , Chemistry , Pharmacology , Plant Extracts , Chemistry , PharmacologyABSTRACT
Objective: To investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius (A. ilicifolius). Methods: Antioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil (DPPH) method and cytotoxic assay was undertaken using brine shrimp lethal toxicity test. Results: A. ilicifolius flower contained terpenoid, phenolic compounds, and alkaloid. The methanol extract of A. ilicifolius flower showed the highest antiradical efficiency (AE=1.41í10-3) against DPPH radicals and the highest cytotoxicity (LC50=22 μg/mL) against brine shrimp nauplii. Conclusions: It is suggested that active compounds of A. ilicifolius flower solved in methanol play a role to inhibit free radical activity and kill Artemia salina nauplii. The substances can be considered as potential antioxidant and cytotoxic agents as well as imminent candidate for cancer therapy.
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OBJECTIVE: To research the protective effects of Acanthus ilicifolius alkaloids A and its two derivatives in the rats with immune hepatic fibrosis. METHODS: Immune hepatic fibrosis model was established by intraperitoneal administration porcine serum. SD rats were treated intragastric administration with [4-hydroxy-2 (3H)-benzoxazolone, HBOA], [4-acetoxy-2 (3H)-benzox-azolone, AcO-BOA], (3-acetyl-4-acetoxy-2-benzoxazolone, TC-3). The activities of ALT, AST in serum and the levels of HA and LN in serum were measured. RESULTS: Compared with the normal control group, the activities of ALT, AST and the levels of HA and LN in the model group were significantly increased. Compared with the model group, animals treated with the HBOA, AcO-BOA or TC-3 could decrease the activities of ALT and AST and the levels of HA and LN markedly. Histopathological results showed that treatment groups could relieve the porcine serum-induced liver damage. CONCLUSION: HBOA and its derivatives have protective effect on the rats with immune-mediated hepatic fibrosis.
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Background and objectives: Primary liver cancer also called hepatocellular carcinoma or hepatoma is the fifth most common cancer in the world with a poor prognosis. An Indian medicinal plant Acanthus ilicifolius shows encouraging results in preventing liver cancer cells from progressing. The aqueous leaf extract (ALE) of the plant was substantially effective in preventing hepatic DNA alterations and sister-chromatid exchanges (a type of chromosomal damage) in tumor-bearing mice. The ALE treatment was able to limit liver metallothionein 1B expression, a potential marker for cell proliferation, and lengthen the mean survival of animals to a significant extent. The findings suggest that Acanthus ilicifolius may be used as a potential chemoprotector against hepatic neoplasia. Methods: The protein ID from Swissprot data base was selected for obtaining the description and function of the protein, its domains structure, post-translational modifications etc. BLAST analysis was performed to identify template protein sequence for metallothionein protein. The comparative modelling of the Metallothionein 1Bby different algorithms like Hidden Markov Model of homology modelling and multiple threading alignments and iterative alignments methods for Ab initio was performed by using the programs like Swiss Model, CPH Model, Wurst and I.TASSES respectively. Results: The obtained models were verified with structure validation programs like, PROCHEK & SAVS. Interpretation and Conclusions: Schrodinger was used for energy refinement of the model. Active site determination through CASTp and surface visualization by Molegro Virtual Docker suggests that this protein can act as a potential drug target.
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Objective To study the chemical constituents in the stem of Acanthus ilicifolius.Methods Some compounds were repeatedly isolated and purified on silica gel column chromatography and vacuum liquid chromatography,their chemical structures were elucidated by their physicochemical properties and spectral data,such as IR,(()~1HNMR),(()~(13)C-NMR),and ESI-MS.Results Eight compounds were obtained from the stem of A.ilicifolius and identified as hexacosanoic acid(Ⅰ),stigmasterol(Ⅱ),tetratriacontanol(Ⅲ), 2-benzoxazolinone(Ⅳ),stigmasterol-3-O-?-D-glucopyranoiside(Ⅴ),vanillic acid(Ⅵ),4-hydroxy-2-benzoxazolone(Ⅶ),quercetin(Ⅷ).Conclusion Compound Ⅶ is first reported as a natural product.Compounds Ⅰ,Ⅲ,and Ⅵ-Ⅶ are reported from this plant for the first time.
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Objective To study the chemical constituents of Acanthus ilicifolius. Methods Compounds were isolated and purified on silica gel,SephadexLH -20 and HPLC,and their chemical structures were elucidated by spectral evidence,physical and chemical analyses. Results and Conclusion Nine compounds,named as stigmasta-4-en-3-one(1),stigmasta-4,22-diene-3-one(2),campest-4-en-3-one(3),tigmasta-4-en-3,6-dione(4),Stigmasta-4,22-diene-3,6-dione(5),Stigmasta-4,22-diene-6?-ol-3-one(6),6?-hydroxyl-stigmasta-4-en-3-one(7),3?-hydroxyl-stigmasta-5,22-diene-7-one(8),3?-hydroxyl-stigmasta-5-en-7-one(9),respectively,were obtained from the petroleum ether soluble portion in the methanol extracts of Acanthus ilicifolius. Among them,compounds 4~8 were reported from this plant for the first time,compounds 2,4 and 9 showed moderate activity against selected tumor cell lines.