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Ginsenoside Rg_3, an active component of traditional Chinese medicine(TCM), was used as the substitute for cholesterol as the membrane material to prepare the ginsenoside Rg_3-based liposomes loaded with dihydroartemisinin and paclitaxel. The effect of the prepared drug-loading liposomes on triple-negative breast cancer in vitro was evaluated. Liposomes were prepared with the thin film hydration method, and the preparation process was optimized by single factor experiments. The physicochemical properties(e.g., particle size, Zeta potential, and stability) of the liposomes were characterized. The release behaviors of drugs in different media(pH 5.0 and pH 7.4) were evaluated. The antitumor activities of the liposomes were determined by CCK-8 on MDA-MB-231 and 4T1 cells. The cell scratch test was carried out to evaluate the effect of the liposomes on the migration of MDA-MB-231 and 4T1 cells. Further, the targeting ability of liposomes and the mechanism of lysosome escape were investigated. Finally, H9c2 cells were used to evaluate the potential cardiotoxicity of the preparation. The liposomes prepared were spheroid, with uniform particle size distribution, the ave-rage particle size of(107.81±0.01) nm, and the Zeta potential of(2.78±0.66) mV. The encapsulation efficiency of dihydroartemisinin and paclitaxel was 57.76%±1.38% and 99.66%±0.07%, respectively, and the total drug loading was 4.46%±0.71%. The accumulated release of dihydroartemisinin and paclitaxel from the liposomes at pH 5.0 was better than that at pH 7.4, and the liposomes could be stored at low temperature for seven days with good stability. Twenty-four hours after administration, the inhibition rates of the ginsenoside Rg_3-based liposomes loaded with dihydroartemisinin(70 μmol·L~(-1)) and paclitaxel on MDA-MB-231 and 4T1 cells were higher than those of the positive control(adriamycin) and free drugs(P<0.01). Compared with free drugs, liposomes inhibited the migration of MDA-MB-231 and 4T1 cells(P<0.05). Liposomes demonstrated active targeting and lysosome escape. In particular, liposomes showed lower toxicity to H9c2 cells than free drugs(P<0.05), which indicated that the preparation had the potential to reduce cardiotoxicity. The findings prove that ginsenoside Rg_3 characterized by the combination of drug and excipient is an ideal substitute for lipids in liposomes and promoted the development of innovative TCM drugs for treating cancer.
Subject(s)
Humans , Paclitaxel/pharmacology , Liposomes/chemistry , Ginsenosides/therapeutic use , Triple Negative Breast Neoplasms/drug therapy , Cardiotoxicity/drug therapy , Cell Line, TumorABSTRACT
Objective: The aim of this study is to probe in the inhibitory effects of ginsenoside Rg3 on the expression of hypoxia-induced factor-1α (HIF-1α) and vascular endothelial growth factor (VEGF) in human gastric cancer cells. Materials and Methods: Human gastric cancer BGC823 cells were divided into the control group and experiment group, and expression levels of HIF-1α and VEGF were detected by immunocytochemistry and Western blot after cells were cultured under hypoxia for different durations. Results: Under hypoxia, expression of HIF-1α and VEGF in human gastric cancer BGC823 cells showed an increasing trend, and that was remarkably lower in experiment group than in the control group after applying Rg3, which was obvious at 12 and 24 h (P < 0.05). Conclusion: Rg3 can inhibit expression of HIF-1α and VEGF in human gastric cancer cells and may influence abdominal implantation metastasis of gastric cancer through inhibiting its expression
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Ginsenoside Rg_3 is widely used in clinical practice as an anti-tumor adjuvant drug, but its application is limited due to its poor oral absorption. In this study, we intended to construct a ginsenoside Rg_3 nanostructured lipid carrier modified by the pullulan(PUL-Rg_3-NLC) to improve the adhesion properties of ginsenoside Rg_3, promote the drug uptake and improve the anti-tumor efficacy. PUL-Rg_3-NLC was characterized by morphology, particle size and Zeta potential. In vivo adhesion characteristics were evaluated by oral gavage tests, and the results were verified from multiple perspectives in combination with in vitro uptake behavior and in vitro pharmacodynamics. The results showed that PUL-Rg_3-NLC, with a particle size of(102±1.89) nm, was characterized by gastric adhesion and could be retained in gastric tissues for a long time, and its uptake by BGC-823 cells was promoted mainly through the pathway mediated by the caveolin-mediated endocytosis. In vitro MTT, cell apoptosis, wound-healing assay and invasion assay all showed some anti-tumor effects. Therefore, PUL-Rg_3-NLC can significantly promote the adhesion of Rg_3 in the stomach, promote the uptake of drugs by gastric cancer cells, and improve the anti-tumor effect. This study can provide some reference for the adjuvant treatment of gastric cancer.
Subject(s)
Drug Carriers , Ginsenosides , Glucans , Lipids , Nanostructures , Particle SizeABSTRACT
Objective@#To evaluate the efficacy of ginsenoside Rg3(GRg3) in the treatment of acute radiation proctitis in rat models.@*Methods@#On the 7th day after 21.5 Gy irradiation, 100 rats were divided into the control group (normal saline, n=20), GRg3 group (gavage of 20 mg/kg, 40 mg/kg and 80 mg/kg GRg3, n=20 for each dose) and Smecta mixture enema group (n=20). After 2 weeks, all rats were anesthetized with chloral hydrate (3 ml/kg) and approximately 5 ml of blood sample was collected from the abdominal aorta prior to sacrifice. The rectal tissues were taken and prepared for detection of Bax and NF-κB contents and HE staining to observe the pathological changes of the rectal tissues. After the blood samples were centrifuged, the supernatants were collected for ELISA to detect the serum levels of IL-2, IL-6, TNF-α and MPO in each group.@*Results@#In the GRg3 group, the serum inflammatory cytokines, serum MPO concentration and the concentration of Bax and NF-κB in the intestinal tissues of rats were decreased along with the increasing dose of GRg3. These parameters in the high-dose GRg3 group were significantly lower than those in the saline group (all P<0.05), whereas did not significantly differ from those in the Smecta mixture enema group (all P>0.05), suggesting that GRg3 exerted good therapeutic effect on acute radiation proctitis in rat models.@*Conclusions@#GRg3 can significantly reduce the concentration of inflammatory cytokines, Bax and NF-κB in the intestinal tissues of rat models with acute radiation proctitis, which is more efficacious than the normal saline. GRg3 can be used to treat acute radiation proctitis in rat models.
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Objective To investigate the effect of ginsenoside Rg3 on immune checkpoint PD-L1 in Lewis cells (LLC) and to explore the related mechanism. Methods The effects of ginsenoside Rg3 on the proliferation of LLC were observed by MTT assay and cell long-term dynamic monitoring. LLC cells treated with 20 ng/mL IFN-γ were used to construct experimental model with high expression of PD-L1 in vitro. The effect of ginsenoside Rg3 on expression of PD-L1 was detected by flow cytometry and immunofluorescence. The effect of ginsenoside Rg3 on the protein expression of PI3K/Akt/mTOR pathway was verified by Western blotting. Results Ginsenoside Rg3 at 16, 32, 64, and 128 μmol/L significantly inhibited the proliferation of LLC (P < 0.01) and reduced the expression of PD-L1 induced by IFN-γ (P < 0.05). Ginsenoside Rg3 at 32 and 64 μmol/L significantly decreased the protein expression of PI3K and mTOR (P < 0.01), and ginsenoside Rg3 at 16, 32, and 64 μmol/L significantly inhibited the phosphorylation of Akt proteins (P < 0.05). Conclusion Ginsenoside Rg3 significantly inhibited the expression of PD-L1 in LLC cells by inhibiting PI3K/Akt/mTOR pathway. Ginsenoside Rg3 blocked the tumor cells escaping immune response by PD-L1 over-expression, enhanced the immune response of T cells, and inhibited the growth of non-small cell lung cancer cells.
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Immune escape is an important mechanism for the development of tumors. Re-activating the anti-tumor immune response is a key measure for the treatment of malignant tumors. Ginsenoside Rg3 (G-Rg3) is a sterol compound isolated from Panax ginseng. It can improve the anti-tumor immune response of human by up-regulating the autoantigenicity and immunogenicity of tumor cells, enhancing the function of immune effector cells and immune active molecules, and regulating the local immune microenvironment. However, the clinical application of G-Rg3 is limited due to its poor water solubility and low bioavailability. Improved drug delivery systems are the key to solving this problem. Therefore, this paper summarizes the research progress of G-Rg3 on tumor immunoregulation and its nano-drug delivery systems, in order to provide reference for the in-depth study and clinical application of G-Rg3.
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Objective: To study the chemical constituents of ginsenosides from the flower buds of Panax ginseng. Methods: The compounds were isolated and purified by Diaion HP-20, MCI gel, silica gel, and semi-preparative HPLC. The structures were elucidated based on NMR and MS data. Results: Four compounds were isolated from the extract of P. ginseng flower buds, and identified as 6’-acetyl-ginsenoside F1 (1), 12α-hydroxyl-ginsneoside Rd (2), 20(S)-ginsenoside Rg3 (3), and 5,6-didehydro-20(S)- ginsenoside Rg3 (4). Conclusion: Compound 4 is a novel ginsenoside, compounds 1 and 2 are new natural products.
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@#Objective: To investigate the effects of ginsenoside Rg3 on the formation of vasculogenic mimicry (VM) in gastric cancer cell line SGC7901 and its molecular mechanism. Methods: MTT assay was used to detect the effect of different concentrations of Rg3 on the proliferation of SGC7901 cells. SGC7901 cells were grouped as follows: BML-284 group, XAV-939 group, Rg3 group, Rg3+ BML-284 group and blank group. Transwell chamber assay was used to detect cell invasion and migration; the formation of VM was observed by tube formation assay; the secretion of MMP-9 and MMP2 was detected by ELISA; the mRNA expressions of GSK-3β and Wnt2B were detected by qPCR; the expression of β-Catenin protein in cells was analyzed by WB; and nuclear entry of β-Catenin was examined by Immunofluorescence. Results: Ginsenoside Rg3 inhibited the proliferation of SGC7901 cells in a time- and concentrationdependent manner; compared with the blank group, 40 mg/L Rg3 significantly inhibited the invasion and migration of SGC7901 cells (both P<0.05) and VM formation (P<0.05); in the meanwhile, the expressions of intracellular GSK-3β, Wnt2B mRNA and β-catenin protein, as well as the nuclear entry of β-catenin were significantly inhibited (all P<0.05). The invasion, migration and VM formation of SGC7901 cells in Rg3+BML-284 group were not significantly different from those in the blank group (all P>0.05). Conclusion: Rg3 can inhibit cell invasion, migration and VM formation in SGC7901 cells by inhibiting the activation of Wnt/β-Catenin pathway.
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@# Objective: To investigate the effect of ginsenoside Rg3 combined with TRAIL on the apoptosis of lung cancer H358 cells and its possible mechanism. Methods: After the completion of cell culture, H538 cells were treated with TRAIL (0, 50, 100, 200 ng/ ml ) or Rg3 (0, 25, 50, 100 μmol/L) for 48 h, and the cells were grouped according to different treatments, namely control group, 50 μmol/LRg3 group, 100 ng/ml TRAILgroup and 50 μmol/LRg3+100 ng/ml TRAILgroup. The effects of Rg3 and/or TRAILon the proliferation of H358 cells were detected by MTT assay. The effects of Rg3 and/or TRAIL on the morphological changes of H358 cells were observed by DAPI staining. Theapoptosis of H358 cells in each group was detected by flow cytometry. The effects of Rg3 and/or TRAIL on the expressions of death receptor 5 (DR5) and caspase-8 in H358 cells were detected by WB. Results: Compared with the other groups, the proliferation of lung cancer H358 cells was significantly inhibited, while the apoptosis was significantly elevated in the 50 μmol/LRg3+100 ng/ml TRAILgroup (P<0.05).After color developing, cells in 50 μmol/LRg3+100 ng/ml TRAILgroup had nuclear shrinkage, chromatin condensation, increased fluorescence intensity, and late morphological changes such as saturation fragmentation. Compared with the other groups, the expression levels of DR5 and caspase-3 ,8 in the cells of 50 μmol/L Rg3+100 ng/ml TRAIL group were significantly increased (P<0.05). Conclusion: Ginsenoside Rg3 combined with TRAIL can synergistically inhibit the proliferation and induce apoptosis of lung cancer H358 cells. The mechanism may be related to the up-regulation of DR5 and caspase-8 by ginsenoside Rg3.
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Aim: To explore the repair mechanism of ginsenoside Rg3 in treating the impaired diabetic wound from improving the vulnerability of diabetic skin of rats. Methods: Male SD rats (n = 32) were injected intraperitoneally streptozotocin to induce hyperglycemia, except for the rats of control group (n = 8). Diabetic rats were randomly divided into model group (equal volume of saline), aminoguanidine group (10 mg · kg-1), ginsenoside Rg3 high dose (15 mg · kg-1) and low group (5 mg · kg-1). After four weeks of oral gavage treatment, full-thickness wound was established. On 21st day after injury, wound samples were collected to observe the pathological changes in wound; the thickness of epidermis and dermis was measured by HE staining; and the epidermal cell proliferation cycle was analysed by flow cytometry; the expression of CD31 in wound tissues was detected by immunohistochemical and image analytical methods. Results: Ginsenoside Rg3 groups showed significantly more fibroblasts, necrotic tissue drops and advanced epithelial, and thickening of epidermis and dermis (P < 0. 01). Model group showed significant increase in G0/G1 phase ratio of epidermal cell cycle (P <0. 01), while reduction in G2/M and S period ratios (P < 0. 01). However, G0/G1 period ratio decreased, while G2/M and S period ratios rose in aminoguanidine group, ginsenoside Rg3 high dose and low dose groups. The decrease of G0/G1 period ratio (P < 0. 05) and increase in G2/M (P <0. 05) and S period ratios (P <0. 01) was found to be significant. The expressions of CD31 in model group was lower than those in control group (P<0. 01). Whereas, it was higher in ginsenoside Rg3 high dose group and aminoguanidine group (P < 0. 05). Conclusions: Ginsenoside Rg3 can effectively promote the repair and healing of impaired diabetic wound. The various mechanisms of repair might be through improving skin pathology, regulating epidermal cell proliferation cycle and promoting angiogenesis.
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Objective: To explore the solid fermentation process of Panax ginseng by Monascus purpureus, which can transfer some major ginsenoside into rare ginsenoside Rg3 with stronger biological activity. Methods: The static dark culture method was used to perform microbial fermentation; Vanilline-glacial acetic acid method was used to detect the total saponins before and after fermentation, and the ginsenoside Rg3 was detected by HPLC. Results: The optimum process parameters of Monascus purpureus fermentation was fermentation 6 d, fermentation temperature 32 ℃, pH 7.0, and water content of substrate 50%. After 6 d of fermentation, the content of total saponins in fermentation products increased by 40%, and the content of ginsenoside Rg3 was 6.047 mg/g, which was 2.3 times as much as that of non-fermented P. ginseng. According to the change of monomer saponin content along with the fermentation time, it was deduced that the transformation path was Rb1 (Rb2)→Rd→Rh2→Rg3. Conclusion: The solid fermentation process of Monascus purpureus established in this study is reasonable, which not only lays a foundation for the directional production of rare saponins Rg3 but provides a theoretical support for preparing rare ginsenoside in vitro.
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Objective: To investigate the effects of ginsenoside Rg3 on intimal proliferation and apoptosis of vascular smooth muscle cells after vascular injury in rats. Methods: Forty Sprague Dawley rats were divided into four groups randomly including Sham operation group, model group, ginsenoside Rg3 low-dose group (5 mg/kg), and ginsenoside Rg3 high-dose group (10 mg/kg). The carotid artery intima injury model was established by inflation balloons. From the next day after modeling, the rats were treated with ginsenoside Rg3 by ig administation in ginsenoside Rg3 groups, and rats in Sham operation group and model group were administered with same amount of normal saline. The injured common carotid arteries were harvested after 14 d and morphological changes of injured arteries were observed by HE staining. Terminal deoxynucleotidyl transferase-mediated nick end labeling (TUNEL) was used to detect the apoptosis of smooth muscle cells; Western blotting and qRT-PCR were used to detect the expression of Fas and anti-apoptotic gene Bcl-2. Results: Compared with the Sham operation group, the vascular neointima of rats in model group was significantly thicker, and the ratio of intima/media area and the apoptosis rate of neointimal hyperplasia were significantly increased. The expression of apoptosis-related gene Fas and anti-apoptotic gene Bcl-2 was significantly increased. Compared with model group, ginsenoside Rg3 (5 and 10 mg/kg) significantly alleviated vascular intimal hyperplasia, the intima/media area ratio and the expression of Bcl-2 was significantly decreased, and the apoptosis rate of smooth muscle cells in the neointimal area and the expression of Fas in injured vessels were significantly increased. Conclusion: Ginsenoside Rg3 can reduce the vascular neointimal hyperplasia induced by balloon injury with the possible underlying mechanism to promote the apoptosis of smooth muscle cells.
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Objective To prepare and characterize tri-components nanostructure lipid carrier of Ginseng Radix modified with hyaluronic acid (HA-OUR-NLC). Methods Nanostructured lipid carriers (NLC) was used to wrap mount three difficult soluble active ingredients in Ginseng Radix including oleanolic acid (OA), ursolic acid (UA), and ginsenoside Rg3. Then using hyaluronic acid (HA) as the target factor, NLC was modified by charge-adsorption. The dynamic dialysis method was used to test the release. The cellular uptake and cytotoxicity of HA-OUR-NLC on SMMC-7721 cells were investigated by flow cytometry instrument and MTT assay respectively. Results OUR-NLC was prepared by ultrasonic dispersion of solvent using NLC as carrier material and CTAB as emulsifier, and its appearance was light blue opalescence. Then HA-OUR-NLC was successfully prepared by charge-sorption method with round shape and uniform distribution. In vitro release showed that it had a sustained release effect. Cell uptake experiments showed that HA-OUR-NLC can be taken up by SMMC-7721 cells. MTT assay results showed that HA-OUR-NLC had inhibitory effect on SMMC-7721 cell proliferation. Conclusion HA-OUR-NLC prepared by solvent ultrasonic dispersion not only has good physical and chemical properties, but also has a certain sustained release effect.
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Objective To analyze the content changes of six kinds of ginsenosides Re, Rg1, Rb1, Rg3, Rh1, and Rh2 after pulping of mountain cultivated ginseng. Methods The HPLC-UV method was performed on an Innoval ODS-2 chromatographic column (250 mm × 4.6 mm, 5 μm), gradient elution of acetonitrile and water with column temperature 30 ℃, at a flow rate of 1.0 mL/min, and detected at 203 nm with injection volume as 20.0 μL. Results The content of six kinds of ginsenosides Re, Rg1, Rb1, Rg3, Rh1 and Rh2 were changed from 0.651, 0.506, 0.363, 0.014, 0.023, 0.031 mg/g to 0.517, 0.413, 0.105, 0.122, 0.214, 0.098 mg/g after pulping of mountain cultivated ginseng. The calibration curve was liner within 2.5-100 mg/L for ginsenoside Re, Rg1, Rb1, Rg3, Rh1, and Rh2, respectively, with the correlation r2 > 0.999 5 and perfect precision, stability, and repeatability. The average recoveries ranged from 95% to 105%, and RSD values varied from 1.25% to 3.5%. Conclusion The content of six kinds of ginsenosides Re, Rg1, Rb1, Rg3, Rh1, and Rh2 in mountain cultivated ginseng were changed after the pulping. The content of ginsenoside Re, Rg1, and Rb1 was reduced and rare ginsenoside Rg3, Rh1, and Rh2 was increased by 8.7 times, 9.3 times, and 3.2 times respectively after the pulping. The HPLC method for simultaneous determination of six kinds of ginsenosides has good accuracy and reliability and can provide scientific basis for the quality evaluation of mountain cultivated ginseng pulp.
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@#Objective: To investigate Ginsenoside Rg3 interfering the expression of CaM through PI3K/AKT signaling pathway to affect the biological activity of gastric cancer BGC-823 cells. Methods: After the culture and passage of gastric cancer BGC-823 cells, Western blotting was used to detect the expression of p-AKT and CaM protein in gastric cancer BGC-823 cells treated with IGF-1 and/ or Rg3; The effect of IGF-1 and/or Rg3 on the proliferation of BGC-823 cells was detected by MTT assay; The effect of IGF-1 and/or Rg3 on the invasion of BGC-823 cells was detected by Transwell assay; Effect of IGF-1 and/or Rg3 on apoptosis of BGC-823 cells was detected by Flow Cytometry. Results: Western blotting results showed that the expression of p-AKT and CaM protein increased in BGC-823 cells with the prolongation of IGF-1 treatment (all P<0.05); Compared with the blank control group, Rg3 significantly inhibited the proliferation of BGC-823 cells, while IGF-1 and IGF-1+Rg3 significantly promoted the cell proliferation (all P<0.05); Compared with the blank control group, Rg3 significantly reduced the invasion of BGC-823 cells, while IGF-1 and IGF-1+Rg3 significantly promoted the invasion of BGC-823 cells (all P<0.05);Flow cytometry showed that compared with the blank control group, Rg3 significantly promoted the apoptosis of BGC-823 cells, while IGF-1 and IGF-1+Rg3 significantly inhibited the apoptosis of BGC-823 cells (all P< 0.05). Conclusion: Ginsenoside Rg3 inhibits the expression of CaM by blocking PI3K/AKT signaling pathway, thereby promoting the apoptosis of gastric cancer BGC-823 cells.
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OBJECTIVE: To study the effects of ginsenoside Rg3 on NF-κBp65 and its related inflammatory factors after carotid balloon injury in rats. METHODS: Sprague Dawley(SD) rats(n=40) were divided into 4 groups randomlysham operationgroup, model group, ginsenoside Rg3 5 mg·kg-1 and ginsenoside Rg3 10 mg·kg-1. 2.0 mm×12 mm Ballon catheters were used to establish the carotid artery intima injury model. On next day after modeling, all animals in model group were administered intragastrically with relative saline and different concentration of ginsenoside Rg3 for 14 d. After 14 d, the morphological changes of the injured arteries were observed by HE staining. The expression of NF-κBp65 in vascular tissue was detected by Western blot; Tumor necrosis factor-α(TNF-α), interleukin-1β(IL-1β) and IL-6 were detected by RT-PCR and Elisa. RESULTS: Compared with the sham-operation group, the neointimal in model group was significantly thicker(P<0.01). while the expression levels of IL-1β, IL-6, TNF-α and NF-κBp65 were increased in model group(P<0.01). The vascular intimal hyperplasia was alleviated distinctly(P<0.01) and the protein expression of NF-κBp65 in vascular tissue was significantly decreased(P<0.01) compared with model group. the expression level of IL-1β, IL-6 and TNF-α was significantly lower in intervention group(P<0.01). CONCLUSION: Ginsenoside Rg3 could reduce the vascular neointimal hyperplasia and inflammation induced by balloon injury, which may be related to its inhibitory role of the transcription factor NF-κB signaling pathway.
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Objective To explore the effects of Ginsenoside Rg3 on oxidative stress and apoptosis in rats with diabetic kidney disease (DKD) induced by STZ.Methods DKD model induced by injection of STZ were randomly divided into 4 groups:diabetic kidney disease group(DKD),low,middle,and high dose Rg3 treated group (L-Rg,M-Rg,H-Rg).Normal rats were selected as control group (NC).Then the Rg3 treated groups were daily administrated with Rg3 (2,5,10 mg/kg) for 10 weeks,while the other two groups were given distilled water.Urinary protein was tested after collecting urine for 24 hours.The fasting plasma glucose (FPG),blood urea nitrogen (BUN),creatinine (Scr),and activity of oxidative stress markers such as GSH-Px,MDA,and SOD in serum were measured.The pathological changes of the kidney were evaluated by HE staining.Cell apoptosis was detected by TUNEL method,and expression of apoptosis related proteins Bax and Bcl-2 were detected by Western blotting.Results After Rg3 intervention,the general status and renal function such as BUN and Scr were significantly improved,24 h urinary protein decreased,serum SOD activity was enhanced,while the content of MDA decreased,apoptosis rate and expression of Bax decreased,and Bcl-2 increased.Conclusion Ginsenoside Rg3 has a protective effect on renal injury in diabetic rats,which may be related to the enhancement of the antioxidase activity in serum,and the inhibition of the apoptosis of renal cells.
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Ginsenoside Rg3,the active ingredient of ginseng with obvious anti-tumor effect,can effectively inhibit the growth of lung cancer,gastric cancer,liver cancer,colon cancer and breast cancer,and improve the immunity. However,ginsenoside Rg3 has poor water solubility with slow absorption and rapid elimination,which leads to low plasma concentration and low bioavailability. Thus,how to overcome its low solubility and improve its bioavailability has become an important research area. In this paper ,the dos-age forms of ginsenoside Rg3 are reviewed by consulting relevant publications.
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Objective To investigate the chemical constituents of the rhizomes of Ligusticum chuanxiong and discuss the significance of first discovery of ginsenosides from the plant. Methods The compounds were isolated and repeatedly purified by column chromatographies such as macroperous resin, Sephadex LH-20, silica gel, and preparative TLC as well as semi-preparative RP-HPLC. Their structures were elucidated by physicochemical properties, NMR, and MS spectral analyses. Results Three ginsenoside compounds were isolated from the n-butanol extracts of rhizomes of L. chuanxiong, and their structures were identified as (20S)-ginsenoside Rh1 (1), (20R)-ginsenoside Rh1 (2), and (20R)-ginsenoside Rg3 (3). Conclusion Ginsenosides are isolated from the genus Ligusticum (Umbelliferae) for the first time, it is of great significance for clarifying pharmacodynamic material basis of the rhizomes of L. chuanxiong. These results also provide the reference data for further verifying the relevance of plant evolution and traditional efficacy between L. chuanxiong and Panax ginseng.
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Objective To observe the inhibitory effect of ginsenoside RG3 on choroidal neovascularization in vitro and in vivo.Methods MTT assay was used to evaluate the inhibitory effect of ginsenoside RG3 on human umbilical vein endothelial cells (HUVEC) proliferation in vitro,and HUVEC were divided into normal group,in which the cells were cultured in DMEM/F-12 medium containing 10％ fetal bovine serum,control group with its medium containing 2 g · L-1 dimethyl sulfoxide (DMSO) and different concentrations of ginsenoside RG3 administration group (12.5 μmol · L-1,25.0 imol · L-1,50.0 μmol · L-1,100.0 μmol · L-1).Then the absorbance value was measured after 6 h.Then,a small amount of HUVEC was collected again and divided into control group with its medium containing 2 g · L-1 DMSO and 100.0 μrnol · L-1 ginsenoside RG3 group for detecting the inhibitory effect of ginsenoside RG3 on tubular formation and vascular endothelial growth factor (VEGF) protein expression by Western blots.In vivo,20 male C57BL/6J mice were collected and randomly divided into control group and ginsenoside RG3 group.After 2 weeks,followed by establishment of model with a semiconductor laser,fundus fluorescein angiography was performed on the 1 st day and 21 st days after treatment.Results MTT results showed that absorbance value of the normal group,control group,12.5 μnol · L-1,25.0 μmol · L-1,50.0 μmol · L-1,100.0 μmol · L-1 ginsenoside RG3 group was 0.43 +0.17,0.43 ±0.05,0.33 +0.02,0.24 +0.02,0.18 ±0.01,0.15 ±0.01 accordingly,and there was no significant difference between the control group and the normal group (all P ＞ 0.05),but the difference between the other group and control group was statistically significant (all P ＜ 0.05).Tubular formation assay showed that the number of tubular formation in the control group and 100.0 μmol · L-1 ginsenoside RG3 group was 72.5 + 5.56 and 11.33 ± 3.71,respectively,and the difference was statistically significant (P ＜ 0.01).Western blots showed that the relative expression of VEGF in 100.0 μmol · L-1 ginsenoside RG3 group (0.14 ±0.01) was significantly lower than that in the control group (0.46 ±0.01),and the difference was statistically significant (P ＜0.01).In vivo fundus fluorescein anglography showed that the fluorescein leakage area of ginsenoside RG3 group was lower than that of the control group.Conclusion Ginsenosid RG3 can inhibit the formation of choroidal neovascularization by inhibiting the expression of VEGF in vitro and in vivo.