Dracorhodin

In vivo pro-angiogenic effects of dracorhodin perchlorate in zebrafish embryos: A novel bioactivity evaluation platform for commercial dragon blood samples.[Pubmed:30648579]

J Food Drug Anal. 2019 Jan;27(1):259-265.

Dragon blood has been used in wound treatment for many years and can be obtained from several distinct plant species. Dracorhodin, the active substituent of dragon blood, is a characteristic compound of the palm tree, Daemonorops draco. At present, the only method to evaluate the quality of commercial dragon blood samples is a HPLC method which determines the amount of Dracorhodin in a dragon blood sample. In this study, we used zebrafish embryos as a platform to demonstrate the in vivo pro-angiogenic activity of Dracorhodin perchlorate, the chemically synthesized analog of Dracorhodin. By using this platform, three different commercial dragon blood samples were also examined. Our results clearly show that even though the commercial dragon blood samples had similar amounts of Dracorhodin, they showed highly variable biological activity, such as pro-angiogenic effects and toxicity. In short, an in vivo activity assay platform for rapidly examining the biological activity of commercial dragon blood samples was successfully established here, which complements the current HPLC-based assay method.

Dracorhodin perchlorate inhibits biofilm formation and virulence factors of Candida albicans.[Pubmed:29477784]

J Mycol Med. 2018 Mar;28(1):36-44.

OBJECTIVE: The aim of this study was to investigate the antifungal activity of Dracorhodin perchlorate (DP) against planktonic growth and virulence factors of Candida albicans. METHODS: Microdilution method based on CLSI-M27-A3 was used to test the antifungal susceptibility of DP. The activity of DP against biofilm formation and development of C. albicans was quantified by XTT assay and visualized by confocal laser scanning microscope. The effect of DP on the morphological transition of C. albicans induced by four kinds of hyphal-inducing media at 37 degrees C for 4hours was observed under microscope. The rescue experiment by adding exogenous cAMP analog was performed to investigate the involvement of cAMP in the yeast to hyphal transition and biofilm formation of C. albicans. Egg yolk emulsion agar was used to determine the inhibition of DP on the phospholipase production of C. albicans. Human JEG-3 and HUVEC cell lines, as well as the nematode Caenorhabditis elegans was used to assess the toxicity of DP. RESULTS: The minimum inhibitory concentration (MIC) of DP is 64muM while the antifungal activity was fungistatic. As low as a concentration at 16muM, DP could inhibit the yeast to hyphal transition in liquid RPMI-1640, Spider, GlcNAc and 10% FBS-containing Sabouroud Dextrose medium, as well as on the solid spider agar. Exogenous cAMP analog could rescue part of biofilm viability of C. albicans. DP could inhibit the production of phospholipase. The toxicity of DP against human cells and C. elegans is low. CONCLUSION: DP could inhibit the planktonic growth and virulent factors in multiple stages, such as yeast to hyphal transition, adhesion, biofilm formation and production of phospholipase of C. albicans.

Dracorhodin perchlorate regulates fibroblast proliferation to promote rat's wound healing.[Pubmed:29428295]

J Pharmacol Sci. 2018 Feb;136(2):66-72.

In recent years, plant-derived extracts are increasing interest from researchers worldwide due to good efficacy and lower side effects. Among the different plant extracts, Dracorhodin perchlorate (DP) is originated from Dragon's blood which has long been used as a natural medicine with various pharmacological activities. In the present study, we have explored the potential regulation of DP on fibroblast proliferation which promotes wound healing both in vitro and in vivo. DP at treatment of 12-24 h significantly induced fibroblast proliferation which is associated with increasing level of phosphorylated-extracellular signal-regulated kinase (ERK). Moreover, if ERK is halted with siRNA, DP cannot induce fibroblast proliferation. In vivo, DP ointment treatment at low- (2.5 mug/mL), medium- (5 mug/mL) and high-(10 mug/mL) doses, rat wounds healed more rapidly compared with the control group. After DP treatment for 7 days, Serpin family H member 1 (SERPINH1) staining confirmed enhanced fibroblast proliferation in the wound tissue. Finally, phosphorylated-ERK in the wound tissue remarkably increased with DP ointment treatment. Therefore, DP may be developed into a potential lead compounds for the treatment of wounds in clinical trials in the near future.

Dracorhodin Perchlorate Accelerates Cutaneous Wound Healing in Wistar Rats.[Pubmed:29333188]

Evid Based Complement Alternat Med. 2017;2017:8950516.

Dracorhodin perchlorate (DP) is extracted from Dragon's blood, which is widely used in traditional Chinese medicine, especially in wound healing. The aim of this paper is to investigate the influence of DP ointment, which contained DP dissolved in DMSO and mixed with Vaseline, on cutaneous wound healing in Wistar rats. Forty Wistar rats were divided into two groups: control and DP groups. The skin on the back of each rat was punched with two full-thickness wounds and then treated with the corresponding drug. After 3, 7, 10, 14, and 21 days, four rats were sacrificed for immunological, biochemical, and histological analyses. Compared with the control treatment, DP could significantly promote wound closure. Histological and biochemical analyses of the skin biopsies also showed that DP regulated the expression of inflammatory responses by TNF-alpha and IL-beta and by supporting wound tissue growth and collagen deposition. Western blot revealed that DP could also facilitate the expression of EGF and VEGF proteins. In conclusion, DP promotes wound healing.

Dracorhodin Perochlorate attenuates Staphylococcus aureus USA300 virulence by decreasing alpha-toxin expression.[Pubmed:27900629]

World J Microbiol Biotechnol. 2017 Jan;33(1):17.

alpha-Toxin, a pore-forming toxin secreted by most Staphylococcus aureus, plays critical role in the pathogenesis associated with various infectious diseases. The USA300 which is a major international epidemic methicilin-resisrant S. aureus has spread rapidly to multiple countries and become an emerging public health concern. In this study, the in vitro efficacy of Dracorhodin Perochlorate (DP) against USA300 virulence was evaluated. Using susceptibility testing, immunoblots, rabbit blood haemolytic assay and real-time RT-PCR, we observed that the alpha-toxin production was decreased when USA300 was co-cultured with different sub-inhibitory concentration of DP. Further, the protective effect of DP against USA300-mediated injury of human alveolar epithelial cells (A549) and MH-S cells was evaluated by cytotoxicity assays, and the result revealed that DP, at final concentration of 16 microg/ml, is a potent antagonist for USA300-mediated cell damage. Importantly, those beneficial effects might partially correlate with hla and RNAIII suppression by DP, leading to the inhibition of alpha-toxin production in culture supernatant. Overall, these results suggest that DP could attenuate the virulence of USA300 by decreasing alpha-toxin production without inhibiting bacterial growth, and this compound may represent an ideal candidate for the development of anti-virulence agent combating S. aureus infection.

The angiogenic effect of dracorhodin perchlorate on human umbilical vein endothelial cells and its potential mechanism of action.[Pubmed:27357516]

Mol Med Rep. 2016 Aug;14(2):1667-72.

Hyperglycemia is the key clinical feature of diabetes, and may induce refractory wound lesions and impaired angiogenesis. Dracorhodin perchlorate (Dra) is the major ingredient of dragon's blood and it has been used as a medicine to treat chronic wounds, such as diabetic foot, since ancient times in many cultures. The current study aimed to investigate the effect of Dra on human umbilical vein endothelial cells (HUVECs) under highglucose (HG) stimulation and its potential mechanism. Dra was observed to increase the multiplication capacity of HUVECs both under low glucose (LG) and HG concentrations. Additionally, migration and tube formation in HUVECs was facilitated by Dra. The expression levels of Ras, mitogenactivated protein kinase (MAPK) and vascular endothelial growth factor, which are key components of the Ras/MAPK pathway, were upregulated following Dra treatment. The present study is the first report, to the best of our knowledge, of the effects of Dra on wound healing, and the association with the Ras/MAPK signaling pathway.

Dracorhodin perchlorate induces the apoptosis of glioma cells.[Pubmed:26846469]

Oncol Rep. 2016 Apr;35(4):2364-72.

Dracorhodin perchlorate (Dp), a synthetic analogue of the antimicrobial anthocyanin red pigment, has recently been shown to induce apoptotic cell death in various types of cancer cells. Yet, the inhibitory effect of Dp on human glioma cells remains uninvestigated. Therefore, in the present study, 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay and flow cytometry were used to detect cell viability and cell cycle progression in glioma U87MG and T98G cells, respectively. Annexin V-FITC/propidium iodide double staining and JC-1 staining were separately applied to determine cellular apoptosis and mitochondrial membrane potential damage in the cells. The expression levels of associated proteins involved in cell cycle progression and apoptosis were measured by western blotting. The activities of caspase9/-3 were determined by Caspase-Glo-9/3 assay. The results indicated that Dp treatment significantly inhibited cell proliferation in a dose- and time-dependent manner, and blocked cell cycle progression at the G1/S phase in the U87MG and T98G cells via the upregulation of p53 and p21 protein expression, and simultaneous downregulation of Cdc25A, Cdc2 and P-Cdc2 protein expression. Additionally, Dp treatment led to the loss of cellular mitochondrial membrane potential, and the release of cytochrome c, and strongly induced the occurence of apoptosis. Increased expression levels of Bim and Bax protein and the downregulated expression of Bcl-2 protein were observed. Caspase-9/-3 were activated and their activities were elevated after Dp treatment. These findings indicate that Dp inhibits cell proliferation, induces cell cycle arrest and apoptosis in glioma cells, and is a possible candidate for glioma treatment.

Dracorhodin perchlorate induces G1/G0 phase arrest and mitochondria-mediated apoptosis in SK-MES-1 human lung squamous carcinoma cells.[Pubmed:26171006]

Oncol Lett. 2015 Jul;10(1):240-246.

Dracorhodin perchlorate (DP) has recently been revealed to induce apoptosis in various types of cancer. However, the antitumor potential and molecular mechanisms of DP in human lung cancer have not been previously reported. Therefore, the present study aimed to investigate the effects of DP on cell viability, the cell cycle and apoptosis, using an MTT assay, flow cytometry and western blot studies. DP was identified to induce cellular and DNA morphological changes, and decreased the viability of SK-MES-1 human lung squamous carcinoma cells. DP significantly inhibited the growth of SK-MES-1 cells by inducing apoptosis and G1/G0 cell cycle arrest in a dose-dependent manner via activation of p53 (P<0.05). Furthermore, DP promoted the significant upregulation of B cell lymphoma-2 (Bcl-2)-activated X protein and significant downregulation of Bcl-2 (P<0.05), inducing dissipation of the mitochondrial membrane potential (MMP). In addition, caspase-3 was activated by DP via the cleavage of its substrate, proteolytic cleavage of poly(ADP-ribose) polymerase. DP also induced caspase-independent apoptosis by significantly increasing the protein expression of the apoptosis-inducing factor (P<0.05), which is localized in mitochondria under the physiological conditions and released into the cytoplasm when MMP is dissipated. Furthermore, the present study demonstrated that DP significantly increased the generation of reactive oxygen species (P<0.05). In conclusion, the current study revealed that DP is able to induce cell cycle arrest and apoptosis in SK-MES-1 cells via activation of the mitochondrial pathway, indicating that DP may be a potential leading compound for the development of future lung cancer therapeutic regimes.

Dracorhodin perchlorate induces apoptosis in primary fibroblasts from human skin hypertrophic scars via participation of caspase-3.[Pubmed:24525335]

Eur J Pharmacol. 2014 Apr 5;728:82-92.

Hypertrophic scar (HS) is an abnormally proliferative disorder characterized by excessive proliferation of fibroblasts and redundant deposition of extracellular matrix. An unbalance between fibroblast proliferation and apoptosis has been assumed to play an important role in HS formation. To explore the regulative effects of Dracorhodin perchlorate (Dp), one of the derivants of Dracorhodin that is a major constituent in the traditional Chinese medicine, on primary fibroblasts from human skin hypertrophic scars, 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay and flow cytometric analysis were respectively used to evaluate the inhibitory effect of Dp on the cells and to determine cell cycle distribution. Additionally, cellular apoptosis was separately detected with Hoechst 33258 staining and terminal deoxynucleotidyl transferase (TdT)-mediated dUTP nick end labeling (TUNEL) assay. The expression levels of caspase-3 mRNA and protein were respectively measured with reverse transcription-polymerase chain reaction and western blot analysis, and caspase-3 activity were determined using a colorimetric assay kit. The results showed that Dp significantly inhibited cell growth, and induced apoptosis in fibroblasts in a dose-and time-dependent manner, arresting cell cycle at G1 phase. Additionally, Dp slightly up-regulated caspase-3 mRNA expression in fibroblasts, but significantly down-regulated caspase-3 protein expression in a dose- and time-dependent manner, and concurrently elevated caspase-3 activity. Taken together, these data indicated that Dp could effectively inhibit cell proliferation, and induced cell cycle arrest and apoptosis in fibroblasts, at least partially via modulation of caspase-3 expression and its activity, which suggests that Dp is an effective and potential candidate to develop for HS treatment.

Dracorhodin perchlorate induced human breast cancer MCF-7 apoptosis through mitochondrial pathways.[Pubmed:23869191]

Int J Med Sci. 2013 Jul 7;10(9):1149-56.

OBJECTIVE: Dracorhodin perchlorate (DP) was a synthetic analogue of the antimicrobial anthocyanin red pigment Dracorhodin. It was reported that DP could induce apoptosis in human prostate cancer, human gastric tumor cells and human melanoma, but the cytotoxic effect of DP on human breast cancer was not investigated. This study would investigate whether DP was a candidate chemical of anti-human breast cancer. METHODS: The MTT assay reflected the number of viable cells through measuring the activity of cellular enzymes. Phase contrast microscopy visualized cell morphology. Fluorescence microscopy detected nuclear fragmentation after Hoechst 33258 staining. Flowcytometric analysis of Annexin V-PI staining and Rodamine 123 staining was used to detect cell apoptosis and mitochondrial membrane potential (MMP). Real time PCR detected mRNA level. Western blot examined protein expression. RESULTS: DP dose and time-dependently inhibited the growth of MCF-7 cells. DP inhibited MCF-7 cell growth through apoptosis. DP regulated the expression of Bcl-2 and Bax, which were mitochondrial pathway proteins, to decrease MMP, and DP promoted the transcription of Bax and inhibited Bcl-2. Apoptosis-inducing factor (AIF) and cytochrome c which localized in mitochondrial in physiological condition were released into cytoplasm when MMP was decreased. DP activated caspase-9, which was the downstream of mitochondrial pathway. Therefore DP decreased MMP to release AIF and cytochrome c into cytoplasm, further activating caspase 9, lastly led to apoptosis. CONCLUSION: Therefore DP was a candidate for anti-breast cancer, DP induced apoptosis of MCF-7 through mitochondrial pathway.

Dracorhodin, the main component in sanguis draconis, is a flavylium compound belonging to the anthocyanin family. Dracorhodin can induce vasodilatation.

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