Chinese Herb Polygonum Cuspidatum Research Articles

Emodin inhibiting epithelial-mesenchymal transition in pulmonary fibrosis through the c-MYC/miR-182-5p/ZEB2 axis.

Emodin is a natural anthraquinone compound, which is the main component found in the traditional Chinese herb Polygonum cuspidatum. The anti-fibrosis effects of Emodin have been reported. This study aimed to explore the specific mechanism of Emodin in the epithelial-mesenchymal transition (EMT) of pulmonary fibrosis. The pulmonary fibrosis mice models were constructed with bleomycin, the EMT models of alveolar epithelial cells were stimulated by TGF-β1, and Emodin was used for intervention. c-MYC and miR-182-5p were overexpressed or silenced by cell transfection. Our results demonstrated that Emodin attenuated pulmonary fibrosis induced by bleomycin in mice, and inhibited EMT, meanwhile downregulated c-MYC, upregulated miR-182-5p, and downregulated ZEB2 in vitro and vivo. Next, overexpression of c-MYC promoted EMT, while silencing c-MYC and overexpressing miR-182-5p inhibited EMT. Then, c-MYC negatively regulated the expression of miR-182-5p with a direct binding relationship. And miR-182-5p inhibited ZEB2 expression in a targeted manner. Finally, Emodin inhibited EMT that had been promoted by overexpression of c-MYC. In conclusion, Emodin could attenuate pulmonary fibrosis and EMT by regulating the c-MYC/miR-182-5p/ZEB2 axis, which might provide evidence for the application of Emodin in the treatment of pulmonary fibrosis.

Polydatin promotes the neuronal differentiation of bone marrow mesenchymal stem cells in vitro and in vivo: Involvement of Nrf2 signalling pathway.

Bone marrow mesenchymal stem cell (BMSC) transplantation represents a promising repair strategy following spinal cord injury (SCI), although the therapeutic effects are minimal due to their limited neural differentiation potential. Polydatin (PD), a key component of the Chinese herb Polygonum cuspidatum, exerts significant neuroprotective effects in various central nervous system disorders and protects BMSCs against oxidative injury. However, the effect of PD on the neuronal differentiation of BMSCs, and the underlying mechanisms remain inadequately understood. In this study, we induced neuronal differentiation of BMSCs in the presence of PD, and analysed the Nrf2 signalling and neuronal differentiation markers using routine molecular assays. We also established an in vivo model of SCI and assessed the locomotor function of the mice through hindlimb movements and electrophysiological measurements. Finally, tissue regeneration was evaluated by H&E staining, Nissl staining and transmission electron microscopy. PD (30 μmol/L) markedly facilitated BMSC differentiation into neuron‐like cells by activating the Nrf2 pathway and increased the expression of neuronal markers in the transplanted BMSCs at the injured spinal cord sites. Furthermore, compared with either monotherapy, the combination of PD and BMSC transplantation promoted axonal rehabilitation, attenuated glial scar formation and promoted axonal generation across the glial scar, thereby enhancing recovery of hindlimb locomotor function. Taken together, PD augments the neuronal differentiation of BMSCs via Nrf2 activation and improves functional recovery, indicating a promising new therapeutic approach against SCI.

Protective effects of polydatin on multiple organ ischemia-reperfusion injury.

Polydatin(PD), a natural active ingredient isolated from traditional Chinese herb Polygonum cuspidatum, is also found in daily foods such as grapes and red wine. It might play a potential therapeutic role in human health through its anti-inflammatory, anti-oxidant, anti-ischemia injury, anti-apoptosis, conditioning blood lipids and other effects, which makes it increasingly become a hotspot of research. Various studies have shown that PD has a protective effect in the ischemia-reperfusion injury of heart, lungs, kidneys, gastrointestinal tract, cerebra and other organs. However, the specific mechanism of action is less and not completely clear. In this study, we aim to review the protective mechanism of PD in the ischemia-reperfusion injury of various organs, and provide inspiration for future studies.

Polydatin Exerts an Antitumor Effect Through Regulating the miR-382/PD-L1 Axis in Colorectal Cancer.

Background: Colorectal cancer (CRC) is considered as one of the most lethal malignancies worldwide. However, the effective therapies remain limited. Polydatin, a main effective component of the Chinese herb Polygonum cuspidatum, has multiple antitumor activities; however, whether Polydatin has anti-CRC activity is not fully understood. Materials and Methods: CRC cell proliferation and apoptosis were measured after treatment of Polydatin using Cell Counting Kit-8 assay, colony formation assay, and flow cytometer assay. The expression of miR-382 and programmed cell death ligand 1 (PD-L1) were determined in CRC cell lines by quantitative real-time polymerase chain reaction and Western blot, respectively. Furthermore, dual-luciferase reporter assay was conducted to determine the target of miR-382. Moreover, loss-of-functional experiments were used to identify the effect of Polydatin on miR-382. Finally, tumor xenograft experiments were conducted to determine the effect of Polydatin in vivo. Results: As a result, Polydatin effectively inhibited cell proliferation and promoted cell apoptosis in CRC cell lines. PD-L1 was confirmed as a direct target of miR-382. Furthermore, Polydatin could suppress the expression of PD-L1 by upregulating miR-382. Moreover, Polydatin inhibits proliferation and promotes apoptosis of CRC cells by regulating miR-382 and suppressing CRC tumor growth in vivo. Conclusion: Polydatin inhibits CRC cell proliferation and promotes apoptosis by regulating miR-382/PD-L1 axis. Polydatin could be a potential compound to synthesize novel antitumor drugs.

Protective effects of polydatin in free and nanocapsulated form on changes caused by lipopolysaccharide in hippocampal organotypic cultures.

Polydatin (PD) is a compound, originally isolated from the root and rhizome of the Chinese herb Polygonum cuspidatum. To date, various biological properties of this compound, such as analgesic, anti-pyretic or diuretic effects, have been shown. Recently, anti-oxidant and anti-inflammatory properties have been widely postulated, yet PD instability and low bioavailability limit its beneficial actions. Therefore, it has been suggested that an encapsulation process may be a promising strategy for overcoming these limitations and increasing the therapeutic efficacy of PD. We examined the effects of PD in two forms, including free and in PD-loaded polymeric nanocapsules, on lipopolysaccharide (LPS)-induced changes in hippocampal organotypic cultures. Our results indicated that free and encapsulated PD diminished cell death processes and attenuated the secretion of pro-inflammatory cytokines induced by LPS administration. Additionally, PD in both forms strongly inhibited the production of nitric oxide and down-regulated the level of iNOS enzyme in LPS-stimulated hippocampal cultures. Taken together, our study showed that PD exerts anti-inflammatory and anti-oxidant properties in LPS-treated hippocampal organotypic cultures. Furthermore, we show that the encapsulation procedure preserved the features of the free form of this compound, and therefore, the polymeric nanocapsules containing PD may be used as a novel and promising delivery system in therapeutic strategies.

Antitumor Research of the Active Ingredients from Traditional Chinese Medical Plant Polygonum Cuspidatum.

In recent years, the utilization of Chinese native medicine and other plant extracts in the treatment of diseases has attracted extensive attention, especially in the area of malignant tumors. However, lots of herbal remedies active ingredients have not been found or have been discovered but not effectively developed and applied. Therefore, screening new Chinese medicine active components and determining their antitumor effects have become a new breakthrough in the prevention and treatment of tumor disease. In the past years, a large number of studies have demonstrated that Polygonum cuspidatum and its active components like resveratrol showed excellent antitumor activities, including our own antitumor studies about resveratrol in colorectal cancer. The purpose of this review is to summarize the research progress of Chinese herb Polygonum cuspidatum and its active components in tumor diseases and provide theoretical basis for further scientific experiments and clinical applications.

Polydatin protects learning and memory impairments in a rat model of vascular dementia

Polydatin is one of the most common encountered stilbenes of nature and a key component of the Chinese herb Polygonum cuspidatum. This study is to investigate the effects of polydatin on learning and memory impairments induced by chronic cerebral hypoperfusion in rats, as well as the potential mechanism. Both common carotid arteries and both vertebral arteries occlusion (four-vessel occlusion, 4-VO) induced severe cognitive deficits tested by water maze task, along with oxidative stress in hippocampus. Oral administration of polydatin for 30 days markedly attenuated cognitive deficits compared with the control (p<0.05). Biochemical determination revealed that polydatin decreased the production of malondialdehyde (MDA) and significantly increased the activities of superoxide dismutase (SOD) and catalase (CAT). Additionally, polydatin effectively alleviated the injuries of cultured neurons induced by oxygen-glucose deprivation (OGD). These results suggest that polydatin exhibit therapeutic potential for vascular dementia, which is most likely related, at least in part, to its anti-oxidant activity and the direct protection of neurons.

Antifatigue effects of polydatin from Chinese herb Polygonum Cuspidatum in swimming mice

This study evaluated the antifatigue polydatin from Chinese herb Polygonum Cuspidatum (PFPC) in ICR mice by swimming endurance test. Forty male mice were studied by being divided into 4 groups (ten for each group), as follows: Group I (control group, CG), Group â…i (low-dose group, LDG), Group â…¢ (medium-dose group, MDG) and Group â…£i€ i€ (high-dose group, HDG). The control group was given distilled water and the treatment groups were given various doses of PFPC (20, 40, 60 mg/kg) for 28 consecutive days, respectively. The result showed that PFPC had significant antifatigue effects in mice. It extended the swimming time, increased concentration of the hemoglobin (Hb), prevented the increase in lactate and blood urea nitrogen (BUN) concentrations. Key words: Polydatin, Polygonum cuspidatum, antifatigue.

Rapid Quantitative HPTLC Analysis, on One Plate, of Emodin, Resveratrol, and Polydatin in the Chinese Herb Polygonum cuspidatum

The rhizome of Polygonum cuspidatum is an important Chinese medicine used against infectious hepatitis, leucorrhagia, pruritus vulvae of the dampness-heat type, burns, snake bite, carbunculosis, amenorrhea, dysmenorrhea, trauma with blood stasis, and rheumatism, etc. Emodin, resveratrol, and polydatin are main active components of the rhizome. We report a simple densitometric HPTLC method for quantification of these compounds. The method was validated for precision, repeatability, and accuracy. The method was found to be precise, with RSD of 0.23, 0.25, and 0.32 (interday) and 0.45, 0.57, and 0.48 (intraday) for different concentrations of emodin, resveratrol, and polydatin, respectively. Instrument precision was 0.25, 0.23, and 0.34 (%CV) for emodin, resveratrol, and polydatin, respectively. The accuracy of the method was checked by measuring the recovery of the three compounds at three different levels; the average recoveries were 102.56%, 100.21%, and 100.27%, respectively. The amounts of emodin, resveratrol and polydatin in Polygonum cuspidatum, as estimated by the proposed method, were 4.96 mg g−1, 1.81 mg g−1, and 13.02 mg g−1. The HPTLC method proposed for estimation of emodin, resveratrol and polydatin was found to be simple, precise, specific, sensitive, and accurate and can be used for quality control of Polygonum cuspidatum.

Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure–activity relationships of 2-methoxystypandrone and its analogues

2-Methoxystypandrone, a naphthoquinone, was isolated from a Chinese herb Polygonum cuspidatum by bioassay guided fractionation using HRV 3C-protease assay. It showed an IC 50 value of 4.6 μM and is moderately selective. A new 10-step, total synthesis of 2-methoxystypandrone was accomplished in 45% overall yield using a Diels–Alder approach. Several analogues of this compound were prepared. Isolation, synthesis and HRV 3C-protease structure–activity relationships of these compounds have been described.