The Effective Activation of Apoptosis by AO-95 from the Aerial Part of Alpiniae officinarum in A549 Cell Line

The study was designed to examine the apoptosis inducing activity of the AO-95 from the aerial part ofAlpiniae officinarum. The AO-95 treatment to three human lung cancer cell lines （A549, NCI-H460 and NCI-H23） resulted in a dose-dependent inhibition of cell growth. The authors selected A549 cell line as a test model system. The AO-95 induced apoptosis ofA549 obviously, as shown by the results of cell cycle distribution analysis and cell apoptosis assay. Treatment of A549 with AO-95 markedly decreased the mitochondrial transmembrane potential （△ψm） suggesting AO-95-induced apoptosis may involve a mitochondrial-related pathway. Two compounds were isolated from AO-95 and their structures were identified as 3-phenylpropanal and 4-phenylbutan-2-one. Meanwhile, ten different components accounting for 98.38% of the total A0-95 composition were identified by gas chromatography-mass spectrometry. The major components were 3-phenylpropanal （33.09%） and 4-phenylbutan-2-one （51.16%）. And these two compounds showed notable cytotoxic activity with IC50 values of 14.90-78.46 μg/mL. In summary, the AO-95, dominated by phenylpropanoid constituents, shows effective apoptosis inducing activity by mitochondrial-related pathway and may be developed as an agent against human lung cancer.

A novel diarylheptanoid bearing flavonol moiety from the rhizomes of Alpinia officinarum Hance

A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was accomplished by HRESI -MS,1D and 2D NMR methods.

Anti-inflammatory activity of Alpinia officinarum hance on rat colon inflammation and tissue damage in DSS induced acute and chronic colitis models

The purpose of this study was to investigate the possible prophylactic effects of Alpinia officinarum hance on experimentally induced acute and chronic colitis models,in-vivo and in-vitro.Acute and chronic colitis were induced in Male Wistar rats by administration of Dextran Sulfate Sodium(DSS)in drinking water.DSS induction exhibited colon shrinkage,increased the Disease Activity Index(DAI)score,increased the levels of inflammatory markers and caused severe anemia.DSS induced animals,co-treated with the hexane extract of Alpinia officinarum(HEAO)(200 mg/kg body wt),effectively suppressed colonic injury that was evidenced by the reduced DAI score,colon weight/length ratio,histological damage,proinflammatory markers and MPO activity.Further,it restored the colonic antioxidants near to normal levels by regulating the oxidative stress via attenuation of lipid peroxidation.Our results revealed that the degree of colitis caused by the administration of DSS was significantly attenuated by HEAO.In addition,the in-vitro study showed that HEAO treatment inhibited the proliferation of HT-29 cells and down regulated the mRNA expression of NF-B and COX-2.Taken together,these results suggest that HEAO is a promising anti-oxidant and anti-inflammatory agent that support its possible therapeutic role in the treatment of colitis.

Herb-drug interaction in the protective effect of Alpinia officinarum against gastric injury induced by indomethacin based on pharmacokinetic, tissue distribution and excretion studies in rats

Alpinia officinarum Hance of the Chinese traditional herb for the treatment of emesis, abdominal pain and diarrhea has been used to counteract gastric disease induced by indomethacin in rats without obvious side effects. However, the role of herb-drug interaction between indomethacin and A. officinarum based on pharmacokinetic, tissue distribution and excretion still remains unknown. In this study, an ultra-fast liquid-tandem mass spectrometry(UFLC-MS/MS) method was developed for simultaneous determination of indomethacin and its three metabolites, O-desmethylindomethacin(ODI), deschlorobenzoylindomethacin(NDI) and indomethacin acyl-b-D-glucuronide(IDAbG) by oral administration of indomethacin solution with and without the ethanolic extract of A. officinarum and applied to comparative pharmacokinetic, tissue distribution and excretion studies. Our results clarified that oral administration of A. officinarum produced significant alterations in the pharmacokinetic parameters of indomethacin. And the pharmacokinetic interaction between indomethacin and A. officinarum reduced the systemic exposure of indomethacin and increased its elimination. Tissue distribution results demonstrated that co-administration of A. Officinarum could not reduce the accumulation of indomethacin in the target tissue of the stomach, but could accelerate the excretions of indomethacin and its three metabolites including ODI, NDI and IDAb G in the bile and feces of rats in the excretion study.Therefore, A. Officinarum might have a gastrointestinal protective effect through the interaction role with indomethacin based on the pharmacokinetics and excretion in rats.

Study on mechanism of two related Chinese herbs A.officinarum-Pogostemon in treatment of delayed emptying in diabetic gastroparesis based on network pharmacology

Objective:To explore the potential active components,therapeutic targets and critical path of Alpinia officinarum and Pogostemonis Herba in the treatment of diabetic gastroparesis(DGP)by using network pharmacology.Methods:The main chemical components and corresponding targets genes of A.officinarum-Pogostemonis Herba were screened through TCMSP database retrieval[oral bioavailability(OB)≥30%and drug like(DL)≥0.18].Tgenes of diabetic gastroparesis were screened by the Human Gene Database(GeneCards),and Venny 2.1 software was used to obtained common targets for the active ingredients of A.officinarum-Pogostemonis Herba and DGP.Then,the protein-protein interaction(PPI)network of the common targets was constructed by STRING database and analyzed to performed the core targets.GO function and KEGG pathway enrichment analysis of the common target genes were obtained by using ClusterProfiler R package.Finally,the network diagram of"active ingredient-pathway-target"was used to establish by Cytoscape 3.8 software.Results:Totally 23 ingredients of A.officinarum-Pogostemonis Herba,97 active ingredients targets and 533 DGP related targets,including 46 common targets were selected.The common targets were mainly enriched in the cell constituents such as the nuclear chromatin and mitochondria outer membrane,involved in the biological processes as oxidative stress,apoptosis signal regulation,and molecular functions as enzyme binding,protein phosphatase binding,and cytokine activity.They were also concentrated in the signal pathways such as PI3K/Akt,HIF-1 and MAPK.The network of“active ingredients-targets-pathways”indicated the active components such as quercetin,kaempferol and galangin in A.officinarum-Pogostemonis Herba played an anti-delayed gastric emptying in diabetic gastroparesis by acting on PTGS2,NOS2,BCL2,IL6,VEGFA and other targets to jointly regulate PI3K-Akt,HIF-1 and MAPK pathways.Conclusion:This study initially reveals that the combined treatment of A.officinarum-Pogostemonis Herba for delayed gastric emptying in diabetic gastroparesis is a complex process with multi-components,multi-targets and multi-pathways,and provides a new idea for followup researches.

The effect of characteristic Li-medicine Alpinia officinarum Hance on improving insulin resistance

Objective:To study the effects of characteristic Li-medicine Alpinia officinarum Hance on improving insulin resistance(IR),and provide scientific evidence for the adjuvant treatment T2DM.Methods:CCK8 kit was used to detect the viability of HepG2 cells with 0-200μg/mL Alpinia officinarum Hance extract(AOE)and 0-100μmol/L galangin,and determine the administration concentration.The IR model was established by inducing HepG2 cells with high glucose for 48 hours,and rosiglitazone(ROSI)was used as the positive control drug.Furthermore,we detected intracellular and extracellular glucose contents in IR-HepG2 cells after dosing AOE and galangin by flow cytometry and glucose detection kit,and evaluated the effect of regulating glucose metabolism and IR.Western blot was used to detect the effects of AOE and galangin on the expression of glucose transporter-4(GLUT4)in IR-HepG2 cells.Results:CCK8 kit test result showed that 0-200μg/mL AOE and 0-50μmol/L galangin had no significant effect on HepG2 cell viability.The results of flow cytometry and glucose detection kit showed that the glucose uptake and consumption of the IR model group induced by high glucose was significantly lower than that of the blank group,and thus the IR model was successfully established.Both 50μg/mL AOE and 10,20μmol/L galangin significantly increased the glucose uptake and consumption of IR-HepG2 cells(P<0.05);Western blot experiment showed that AOE and galangin significantly increased GLUT4 level of IR-HepG2 cells(P<0.01).Conclusion:Alpinia officinarum Hance could promote the uptake and consumption of glucose in IR-HepG2 cells by up-regulating the expression of GLUT4 protein,thereby improving IR and enhancing insulin sensitivity.

A new dimeric diarylheptanoid from the rhizomes of Alpinia officinarum

AIM: To study the chemical constituents of the rhizomes of Alpinia officinarum Hance. METHOD: Compounds were isolated by repeated column chromatography, and their structures were elucidated on the basis of spectral analysis. The cytotoxic activities of these compounds were evaluated with the T98G and B16F10 cell lines by the MTT assay. RESULTS: A dimeric diarylheptanoid, named alpinin B(1), along with three known diarylheptanoids were obtained, and their structures were identified as alpinin B(1), 1, 7-diphenyl-3,5-heptanedione(2),(4E)-1, 7-diphenylhept-4-en-3-one(3) and(4E)-7-(4-hydroxyphenyl)-1-phenylhept-4-en-3-one(4). CONCLUSION: Compound 1 is a new dimeric diarylheptanoid. The biosynthetic pathway of 1 was speculated to originate from a Michael reaction between compounds 2 and 3. Compound 3 showed cytotoxicity against the human glioblastoma T98G cell line with IC50 of 27 μmol L 1.

Chromatographic fingerprint analysis and quantitative evaluate the rhizomes of Alpinia officinarum Hance(lesser galangal)

The rhizome of Alpinia officinarum Hance is a well-known traditional Chinese medicine(TCM)and has been widely used for the remedy of gastrointestinal diseases.In the present study,a simple and rapid HPLC-DAD was developed for the quality control of the rhizomes of A.officinarum.Its chemical fingerprint was established using raw material of 15 different origins in China.Similarity analysis(SA)and hierarchical clusting analysis(HCA)were applied to select the qualitative markers.Principal components analysis(PCA)was conducted to select the quantitative markers of the rhizomes of A.officinarum samples from different origins.The constituents were confirmed by(+)electrospray ionization LC-MS.12 constituents were selected as common peaks and 10 of them were confirmed by(+)electrospray ionization LC-MS.Six bioactive constituents including DPHA,galangin flavanone,galangin,galangin 3-methylether,DPHB and DPHC were simultaneous determination by using the HPLC-DAD analysis.The developed method was able to determine the bioactive components with excellent resolution,precision and recovery.The results indicated that chromatographic fingerprint combination with multi-components determination method is suitable for quality assessment of the rhizomes of A.officinarum.

A novel dimeric diarylheptanoid from the rhizomes of Alpinia officinarum

A novel dimeric diarylheptanoid,named alpinin A（1）,along with two known compounds,1,7-diphenyl-5-ol-3-heptanone and 7- （4＇-hydroxy-3＇-methoxyphenyl）-l-phenyl-4-heptene-3-one,were isolated from the rhizomes of Alpinia officinarum Hance.The structure of compound 1 was elucidated on the basis of spectral analysis,including HR-IT-TOF-MS,1D and 2D NMR.And a possible biogenetic pathway had been proposed for 1.