Albiflorin

Albiflorin is a major constituent contained in peony root; possesses therapeutic potential for neurodegenerative diseases. IC50 value: Target: in vitro: Albiflorin significantly ameliorated Glu-induced reduction of cell viability, nuclear and mitochondrial apoptotic alteration, reactive oxygen species accumulation, and B-cell lymphoma 2 (Bcl-2)/Bax ratio. Albiflorin also enhanced phosphorylation of AKT and its downstream element glycogen synthase kinase-3β, and this effect was abrogated by the AKT inhibitor LY294002 [1]. in vivo: Mice were exposed to X-ray radiation (400 Roentgen), and both mice and rabbits were intraperitoneally injected with cyclophosphamide (100.0 mg/kg) and cytarabine chloride (92.7 mg/kg), respectively, for 3 days to induce myelosuppression. Albiflorin was subsequently administrated intravenously at low (15.0 mg/kg for mice, 6.00 mg/kg for rabbits), intermediate (30.0 mg/kg for mice, 12.0 mg/kg for rabbits) and high (60.0 mg/kg for mice, 24.0 mg/kg for rabbits) doses, as well as orally (60.0 mg/kg for mice, 24.0 mg/kg for rabbits) for 7 days. Shenqi tablets were used as positive controls (oral administration of 936.0 mg/kg for mice, 336.0 mg/kg for rabbits). The administration of Albiflorin significantly ameliorated myelosuppression in all cases [2].

References:
[1]. Wang D, et al. Neuroprotective effects of paeoniflorin, but not the isomer albiflorin, are associated with the suppression of intracellular calcium and calcium/calmodulin protein kinase II in PC12 cells. J Mol Neurosci. 2013 Oct;51(2):581-90. [2]. Xu W, et al. Therapeutic effects of combination of paeoniflorin and albiflorin from Paeonia radix on radiation and chemotherapy-induced myelosuppression in mice and rabbits. Asian Pac J Cancer Prev. 2011;12(8):2031-7.

Therapeutic effects of combination of paeoniflorin and albiflorin from Paeonia radix on radiation and chemotherapy-induced myelosuppression in mice and rabbits.[Pubmed:22292646]

Asian Pac J Cancer Prev. 2011;12(8):2031-7.

The aim of this study was to investigate the therapeutic effects of the combination of paeoniflorin and Albiflorin (CPA) extracted from Paeonia radix on radiation and chemotherapy induced myelosuppression in two animal models: mice and rabbits. Mice were exposed to X-ray radiation (400 Roentgen), and both mice and rabbits were intraperitoneally injected with cyclophosphamide (100.0 mg/kg) and cytarabine chloride (92.7 mg/kg), respectively, for 3 days to induce myelosuppression. CPA was subsequently administrated intravenously at low (15.0 mg/kg for mice, 6.00 mg/kg for rabbits), intermediate (30.0 mg/kg for mice, 12.0 mg/kg for rabbits) and high (60.0 mg/kg for mice, 24.0 mg/kg for rabbits) doses, as well as orally (60.0 mg/kg for mice, 24.0 mg/kg for rabbits) for 7 days. Shenqi tablets were used as positive controls (oral administration of 936.0 mg/kg for mice, 336.0 mg/kg for rabbits). The administration of CPA significantly ameliorated myelosuppression in all cases. For the X-ray irradiated mice and the chemotherapy treated mice and rabbits, high dosages of CPA resulted in the recovery of, respectively, 94.4%, 95.3% and 97.7% of hemoglobin content; 67.7%, 92.0% and 94.3% of platelet numbers; 26.8%, 137.1% and 107.3% of white blood cell counts; as well as a reversal in the reduction of peripheral differential white blood cell counts. There was also a recovery of 50.9%, 146.1% and 92.3%, respectively, in the animals' relative spleen weight. Additionally, a recovery of 35.7% and 87.2% in the number of bone marrow nucleated cells was observed in the radio- and chemotherapy treated mice, respectively. Bone marrow white blood cell counts also resumed to normal levels. These results substantiate the marked therapeutic effects of CPA to ameliorate myelosuppression induced by radio and chemotherapy.

Inhibition of beta-amyloid Aggregation By Albiflorin, Aloeemodin And Neohesperidin And Their Neuroprotective Effect On Primary Hippocampal Cells Against beta-amyloid Induced Toxicity.[Pubmed:25938872]

Curr Alzheimer Res. 2015;12(5):424-33.

Being one of the hallmarks of Alzheimer's disease, beta-amyloid (Abeta) aggregates induce complicated neurotoxicity. Evidences show that the underlying mechanism of neurotoxicity involves a glutamate receptor subtype, N-methyl-D-aspartate (NMDA) receptor, an increase in intracellular calcium(II) ion loading as well as an elevation in oxidation stress. In this work, among the 35 chemical components of Chinese herbal medicines (CHMs) being screened for inhibitors of Abeta aggregation, four of them, namely Albiflorin, aloeemodin, neohesperidin and physcion, were found for the first time to exhibit a potent inhibitory effect on Abeta(1-40) and Abeta(1-42) aggregation. Their neuroprotective capability on primary hippocampal neuronal cells was also investigated by MTT assay, ROS assay and intracellular calcium(II) ion concentration measurement. It was interesting to find that physcion was rather toxic to neuronal cells while Albiflorin, aloeemodin and neohesperidin reduced the toxicity and ROS induced by both monomeric and oligomeric Abeta species. In addition, Albiflorin was particularly powerful in maintaining the intracellular Ca(2+) concentration.

Paeoniflorin and Albiflorin Attenuate Neuropathic Pain via MAPK Pathway in Chronic Constriction Injury Rats.[Pubmed:27429639]

Evid Based Complement Alternat Med. 2016;2016:8082753.

Neuropathic pain remains as the most frequent cause of suffering and disability around the world. The isomers paeoniflorin (PF) and Albiflorin (AF) are major constituents extracted from the roots of Paeonia (P.) lactiflora Pall. Neuroprotective effect of PF has been demonstrated in animal models of neuropathologies. However, only a few studies are related to the biological activities of AF and no report has been published on analgesic properties of AF about neuropathic pain to date. The aim of this study was to compare the effects of AF and PF against CCI-induced neuropathic pain in rat and explore the underlying mechanism. We had found that both PF and AF could inhibit the activation of p38 mitogen-activated protein kinase (p38 MAPK) pathway in spinal microglia and subsequent upregulated proinflammatory cytokines (interleukin-1beta (IL-1beta) and tumor necrosis factor-alpha (TNF-alpha)). AF further displayed remarkable effects on inhibiting the activation of astrocytes, suppressing the overelevated expression of phosphorylation of c-Jun N-terminal kinases (p-JNK) in astrocytes, and decreasing the content of chemokine CXCL1 in the spinal cord. These results suggest that both PF and AF are potential therapeutic agents for neuropathic pain, which merit further investigation.

Protective effect of albiflorin against oxidative-stress-mediated toxicity in osteoblast-like MC3T3-E1 cells.[Pubmed:23707745]

Fitoterapia. 2013 Sep;89:33-41.

Albiflorin isolated from Paeoniae Radix was investigated for its ability to protect against antimycin A-induced osteoblast toxicity in the MC3T3-E1 cell line. MC3T3-E1 cells showed significantly reduced viability, increased apoptosis and lactate dehydrogenase release, elevated ROS/RNS levels, and decreased mitochondrial function after exposure to antimycin A. Pretreatment with Albiflorin reversed the loss of cell viability in antimycin A-treated cultures. Similarly, pretreatment with Albiflorin before antimycin A resulted in decreased apoptosis and lactate dehydrogenase release, decreased ROS/RNS levels, and increased mitochondrial function compared to antimycin A-treated cultures. In addition, Albiflorin increased the mineralization reduced by antimycin A. Albiflorin reduced antimycin A-induced mitochondrial cytochrome c loss and cardiolipin peroxidation, conferring protection against ROS. These results confirmed the crucial role of cytochrome c and cardiolipin in the underlying mechanistic action of Albiflorin. Therefore, the results suggest that Albiflorin enhances mitochondrial function to suppress antimycin A-induced oxidative damage via the preservation of cytochrome c and cardiolipin. All of these data indicate that Albiflorin may reduce or prevent osteoblast degeneration in osteoporosis.

Comparative studies of paeoniflorin and albiflorin from Paeonia lactiflora on anti-inflammatory activities.[Pubmed:24646307]

Pharm Biol. 2014 Sep;52(9):1189-95.

CONTEXT: Paeonia lactiflora Pall. (Ranunculaceae) has been used for more than 1000 years in traditional Chinese medicine for the treatment of gynecological problems, cramp, pain, giddiness, and congestion. Paeoniflorin, monoterpene glycosides isolated from P. lactiflora, possesses a variety of pharmacological activities. However, the pharmacological activity of the pharmacological activity of Albiflorin, another main monoterpene glycoside, has not been well studied. OBJECTIVES: The present study investigated the anti-inflammatory activities of paeoniflorin and Albiflorin using models of lipopolysaccharides (LPS) induced RAW 264.7 cells. MATERIALS AND METHODS: Production of nitric oxide (NO) was measured by the Griess colorimetric method. In addition, prostaglandin E2 (PGE2), interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-alpha) synthesis were analyzed using an enzyme-linked immunosorbent assay (ELISA). The protein expression of cyclooxygenase-2 (COX-2) was detected by a cell-based ELISA. The gene expression levels of inducible nitric oxide synthase (iNOS), COX-2, TNF-alpha, and IL-6 were detected by quantitative real-time reverse-transcription polymerase chain reaction (real-time RT-PCR). RESULTS: Compared with the LPS-induced group, the inhibition rates of NO, PGE2, TNF-alpha, and IL-6 production were 17.61, 27.56, 20.57, and 29.01% by paeoniflorin and 17.35, 12.94, 15.29, and 10.78% by Albiflorin. The IC50 values of paeoniflorin and Albiflorin on NO production were 2.2 x 10(-4 )mol/L and 1.3 x 10(-2 )mol/L, respectively. The protein expression of COX-2 was reduced by 50.98% with paeoniflorin and 17.21% with Albiflorin. The inhibition rates of gene expression of iNOS, COX-2, IL-6, and TNF-alpha were 35.65, 38.08, 19.72, and 45.19% by paeoniflorin and 58.36, 47.64, 50.70, and 12.43% by Albiflorin, respectively. CONCLUSION: These results show that Albiflorin has similar anti-inflammatory effects to paeoniflorin, which provides new evidence that Albiflorin can serve as a new chemical marker for the quality control of Paeoniae Radix and the Chinese Pharmacopoeia can be updated.

Antidepressant-like effects of albiflorin extracted from Radix paeoniae Alba.[Pubmed:26719283]

J Ethnopharmacol. 2016 Feb 17;179:9-15.

ETHNOPHARMACOLOGY RELEVANCE: Albiflorin, a monoterpene glycoside, is a main component of Radix paeoniae Alba, which could be a Chinese herbal medicine used in the treatment of psychiatric disorders. However, the exact role of Albiflorin in depression is poorly understood. AIM OF THE STUDY: The current study aimed to evaluate the antidepressant effect of Albiflorin in mice and rats, and the possible mechanism was also determined. MATERIALS AND METHODS: The antidepressant-like effects of Albiflorin was determined by using animal models of depression including forced swim and tail suspension tests in mice and chronic unpredictable stress (CUS) in rats. The acting mechanism was explored by determining the effect of Albiflorin on the expression of brain-derived neurotrophic factor (BDNF) in the hippocampus by western blot and the levels of monoamine in the hippocampus by HPLC. RESULTS: Our results showed that 7 days treatment with Albiflorin significantly decreased immobility time in the forced swimming test (FST) and the tail suspension test (TST) at doses of 3.5, 7.0 and 14.0mg/kg without alter the locomotor activity in mice. Moreover, western blot analysis showed that Albiflorin could increase the expression of BDNF in the hippocampus. We further exposed rats to a chronic unpredictable stress (CUS) protocol for a period of 35d to induce depressive-like behaviors. We found that chronic treatment with Albiflorin, at doses of 7.0 and 14.0mg (i.g., once daily for 35d), restored the sucrose preference in CUS rats. In the open-field test, Albiflorin significantly increased the number of crossings and rearings in the CUS rats at three doses. Moreover, chronic treatment with Albiflorin up-regulated the hippocampal BDNF expression levels and the hippocampal 5-HT, 5-HIAA, and NA levels. CONCLUSION: Albiflorin produced significant antidepressant-like effects, which were closely related to the hippocampal 5-HT/NE increase and BDNF expression. Our data indicated that Albiflorin could be a potential anti-depressant drug.

Simultaneous determination of gallic acid, albiflorin, paeoniflorin, ferulic acid and benzoic acid in Si-Wu decoction by high-performance liquid chromatography DAD method.[Pubmed:15797805]

J Pharm Biomed Anal. 2005 Apr 1;37(4):805-10.

A high-performance liquid chromatographic method was applied to the determination of gallic acid, Albiflorin, paeoniflorin, ferulic acid and benzoic acid in Si-Wu decoction and other 13 combinations of the formula. These five compounds were analyzed simultaneously with a Zorbox SB C-18 column by gradient elution using 0.01% (v/v) phosphoric acid-acetonitrile as the mobile phase. The flow rate was 1 ml min(-1), and detection was set at 230 nm. The recovery of the method was in the range of 94.8-103.1%, and all the compounds showed good linearity (r>0.9995) in a relatively wide concentration range. The result indicated that the content of these five compounds changed after decocting process. The contents of paeoniflorin, Albiflorin, ferulic acid and gallic acid increased and that of benzoic acid decreased significantly.