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Abstract: Ethnopharmacological relevance: The use of African chewing sticks in maintaining oral health is widely practiced in African countries. It has been reported that chewing stick users have a lower rate of dental caries and a better general oral health than non-users. It is generally thought that the beneficial effect of chewing stick is attributed to the mechanical cleansing effect and antimicrobial substances present in the stick. However, the active antimicrobial substances remain uncharacterized. Aim of the study: To provide a scientific basis for the anti-caries effect of African chewing sticks, the authors purify an active antibacterial compound from Garcinia kola Heckel, a Nigerian chewing stick and examined the antibacterial activity of this compound against the cariogenic bacterium Streptococcus mutans. Materials and methods: Methanol extract was prepared from Garcinia kola and was further fractionated by solvent extractions. Silica gel chromatography was used to purify the antibacterial compound from the active fraction. The identity of the purified compound was determined by NMR analysis. The antibacterial activity of the purified compound was examined by standard microbiological assays. Results: The antibacterial activity was found in the ether fraction and the active compound was isolated and determined to be a biflavonoid named GB1. GB1 was active against Streptococcus mutans and other oral bacteria with minimum inhibitory concentration (MIC) values of 32–64μg/ml. The basis for the antibacterial effect of GB1 was investigated using Streptococcus mutans as the target. At 256μg/ml, GB1 exhibited some bacteriocidal activity against Streptococcus mutans and induced the aggregation of Streptococcus mutans. GB1 has no apparent effects on protein synthesis and DNA synthesis but inhibited glucose uptake and utilization by Streptococcus mutans suggesting that GB1 exerts its antibacterial effect by inhibiting metabolism. GB1 also inhibited the formation of water-insoluble glucan by the extracellular glucosyltransferases from Streptococcus mutans in a dose-dependent manner. Streptococcus mutans did not develop resistance to GB1 upon subculturing in the presence of sub-MIC level of the biflavonoid. Conclusion: The antibacterial effect and glucan synthesis-inhibition property of this biflavonoid may account for some of the beneficial effects reported in the chewing stick users. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: The use of African chewing sticks in maintaining oral health is widely practiced in African countries. It has been reported that chewing stick users have a lower rate of dental caries and a better general oral health than non-users. It is generally thought that the beneficial effect of chewing stick is attributed to the mechanical cleansing effect and antimicrobial substances present in the stick. However, the active antimicrobial substances remain uncharacterized. Aim of the study: To provide a scientific basis for the anti-caries effect of African chewing sticks, the authors purify an active antibacterial compound from Garcinia kola Heckel, a Nigerian chewing stick and examined the antibacterial activity of this compound against the cariogenic bacterium Streptococcus mutans. Materials and methods: Methanol extract was prepared from Garcinia kola and was further fractionated by solvent extractions. Silica gel chromatography was used to purify the antibacterial compound from the active fraction. The identity of the purified compound was determined by NMR analysis. The antibacterial activity of the purified compound was examined by standard microbiological assays. Results: The antibacterial activity was found in the ether fraction and the active compound was isolated and determined to be a biflavonoid named GB1. GB1 was active against Streptococcus mutans and other oral bacteria with minimum inhibitory concentration (MIC) values of 32–64μg/ml. The basis for the antibacterial effect of GB1 was investigated using Streptococcus mutans as the target. At 256μg/ml, GB1 exhibited some bacteriocidal activity against Streptococcus mutans and induced the aggregation of Streptococcus mutans. GB1 has no apparent effects on protein synthesis and DNA synthesis but inhibited glucose uptake and utilization by Streptococcus mutans suggesting that GB1 exerts its antibacterial effect by inhibiting metabolism. GB1 also inhibited the formation of water-insoluble glucan by the extracellular glucosyltransferases from Streptococcus mutans in a dose-dependent manner. Streptococcus mutans did not develop resistance to GB1 upon subculturing in the presence of sub-MIC level of the biflavonoid. Conclusion: The antibacterial effect and glucan synthesis-inhibition property of this biflavonoid may account for some of the beneficial effects reported in the chewing stick users. [Copyright &y& Elsevier]

Abstract: Crude extracts and three purified tannins from Geum japonicum Thunberg (Rosaceae) were examined for relaxant effects in isolated rat thoracic aorta and for hypotensive effects in anesthetized normotensive and hypertensive rats. The acetone extract and the butyl alcohol extract of Geum japonicum at a cumulative concentration of 30μg/ml potently relaxed phenylephrine-precontracted aortic rings by 73±5% and 80±7%, respectively, without affecting the resting tension of these vessels. Removal of the vascular endothelium, inhibition of nitric oxide (NO) synthase with N ω -nitro-l-arginine (l-NA) or inhibition of cGMP biosynthesis with methylene blue all abolished the vasorelaxant effects of the Geum japonicum extracts. Addition of l-arginine, the substrate for NO biosynthesis, reversed the inhibitory effects of l-NA. Similar vasorelaxant effects of 82±10%, 61±8% and 82±14%, were observed with the purified tannins, penta-O-galloyl-β-glucoside, casuariin and 5-desgalloylstachyurin, respectively, at a cumulative concentration of 10μM. Intravenous injection of the butyl alcohol extract of Geum japonicum at a cumulative dose of 2.5mg/kg into both hypertensive and normotensive rats resulted in a marked reduction in the mean arterial blood pressure by 46±6% and 34±7%, respectively, which was abolished by prior injection of l-NA. Therefore, these results suggest that tannins may be responsible for the vasorelaxant and hypotensive effects of Geum japonicum, mediated via endogenous NO and subsequent cGMP formation. The data suggest that extracts of Geum japonicum may have potential use as new anti-hypertensive agents for lowering arterial blood pressure in hypertensive patients. [Copyright &y& Elsevier]

Garcinia oligantha Merr. is an ethnomedicine plant mainly distributed in Guangdong and Hainan, China. It has the effects of heat-clearing and detoxicating, which has been used by local ethnic minorities to treat a variety of diseases, including inflammation, internal heat, toothache and scald. This review summarizes and discusses the progress of the chemical compounds and biological activities of G. oligantha that have been studied in recent years to provide the direction for the prospective research and applications of G. oligantha. The relevant literature about G. oligantha was accessible from ancient Chinese medical books and records, theses, as well as major scientific databases such as Google Scholar, PubMed, Web of Science, ScienceDirect, SciFinder, Baidu Scholar and China National Knowledge Infrastructure (CNKI). To date, more than 150 chemical compounds were isolated from this plant, including xanthones, volatile oil, fatty acid, benzofurane derivative and biphenyl compounds. Xanthones are the main bioactive compounds that exhibit diverse biological effects, such as antitumor, analgesic, anti-inflammatory, antioxidative, neuroprotective, antimalarial and antibacterial effects, which are consistent with its traditional uses as a folk medicine. Modern pharmacological studies show that these compounds participate in a variety of signaling pathways underlying different pathophysiologies, making them a valuable medicinal resource. G. oligantha is an ethnomedicine with a long history. However, due to regional and cultural constraints, the popularisation and use of ethnomedicine are still limited. Modern pharmacological and chemical research suggest that G. oligantha contains a variety of bioactive compounds and showed diverse biological functions, which is worthy of comprehensive and in-depth research. This review summarizes and discusses the recent progress in studies on G. oligantha , looking forward to promote further research and sustainable development of folk medicinal plants. [Display omitted] [ABSTRACT FROM AUTHOR]

Chronic kidney disease can be caused by numerous diseases including obesity and hyperuricemia (HUA). Obesity may exacerbate the renal injury caused by HUA. Red ginseng, a steamed products of Panax ginseng Meyer root, is known for its remarkable efficacy in improving metabolic syndrome, such as maintaining lipid metabolic balance. However, the role of red ginseng on hyperuricemia-induced renal injury in obese cases remains unclear. This study aimed to investigate the action of red ginseng extract (RGE) on lipotoxicity-induced renal injury in HUA mice. A high-fat diet (HFD)-induced obesity model was employed to initially investigate the effects of RGE on body weight, TC, OGTT, renal lipid droplets, and renal function indices such as uric acid, creatinine, and urea nitrogen. Renal structural improvement was demonstrated by H&E staining. Subsequently, an animal model combining obesity and HUA was established to further study the impact of RGE on OAT1 and ACC1 expression levels. The mechanisms underlying renal injury regulation by RGE were postulated on the basis of RNA sequencing, which was verified by immunohistochemical (including F4/80, Ki67, TGF-β1, α-SMA, and E-cadherin), Masson, and Sirius red staining. RGE modulated HFD-induced weight gain, glucose metabolism, and abnormalities of uric acid, urea nitrogen, and creatinine. RGE alleviated the more severe renal histopathological changes induced by obesity combined with HUA, with down-regulated the protein levels of ACC1, F4/80, Ki67, TGF-β1, and α-SMA, and up-regulated OAT1 and E-cadherin. RGE has ameliorative effects on chronic kidney disease caused by obesity combined with HUA by maintaining lipid balance and reducing renal inflammation and fibrosis. [Display omitted] • RGE improved metabolic disorders and renal injury induced by obesity and obesity combination with hyperuricemia. • RGE ameliorated obesity-induced lipid accumulation in the kidney. • RGE improved renal inflammation and fibrosis exacerbated by lipotoxicity. [ABSTRACT FROM AUTHOR]

Prunella vulgaris L. (PVL) is a perennial herb belonging to the Labiate family, first recorded in the "Shen Nong's Classic of the Materia Medica". PVL can enter the liver and gallbladder channel to show its function in clearing the liver fire, dispersing nodules, dissolving swelling, and improving vision. The traditional use of PVL is to protect liver function and has clinical applications in liver diseases therapy. The modern pharmacological studies have been shown to possess potential hepatoprotection, but its underlying mechanisms against alcoholic liver disease (ALD) in mice remains to be elucidated. This study aimed to explore the protective effect and potential mechanism of PVL on alcohol induced liver injury. We used Lieber-DeCarli ethanol liquid diet fed Male C57BL/6 mice for four weeks plus a single binge (NIAAA modified model) to establish an ALD model and explored the protective effects of PVL extract against ALD. Western blot, Flow cytometry and RT-qPCR methods were used to detect lipid metabolism disorders and the inflammatory response induced by macrophages in ALD mice, and the gut microbiota composition changes were detected by 16s rRNA to reveal the potential mechanism of PVL against ALD. In ALD mice, PVL can ameliorate excessive alcohol intake-induced liver injury and lipid metabolism disorders associated with improvement of gut microbiota dysbiosis and intestinal barrier damage. PVL reduced the translocation of endotoxin, which subsequently inhibits hepatic inflammation mediated by the TLR4/MyD88 signaling pathway. These findings demonstrated the protective potential of PVL against gut dysbiosis and endotoxin leakage in ALD mice, which provides a theoretical basis for PVL against liver diseases. [Display omitted] • PVL ameliorated liver injury in ALD mice. • PVL modulated gut dysbiosis in ALD mice. • PVL ameliorated intestinal barrier dysfunction in ALD mice. • PVL alleviated hepatic inflammation in ALD mice. [ABSTRACT FROM AUTHOR]

A widely used traditional prescription, Yi-Gan San (YGS) is a remedy for neurodegenerative disorders. The formulation consists of seven Chinese medicinal materials in specific proportions, namely Uncariae Ramulus cum Uncis (Uncaria rhynchophylla (Miq.) Miq. ex Havil.), Bupleuri Radix (Bupleurum chinense DC.), Angelicae Sinensis Radix (Angelica sinensis (Oliv.) Diels), Chuanxiong Rhizoma (Ligusticum wallichii Franch.), Poria (Poria cocos (Schw.) Wolf), Atractylodis Macrocephalae Rhizoma (Atractylodes macrocephala Koidz.) and Glycyrrhizae Radix et Rhizoma (Glycyrrhiza uralensis Fisch.). Using YGS has been shown to alleviate various behavioural and psychological symptoms of dementia (BPSD). The goal of this review is to give up-to-date information about the traditional uses, chemistry, pharmacology and clinical efficacy of YGS based on the scientific literature and to learn the current focus and provide references in the next step. The database search room was accessed using the search terms "Yi-Gan San" and "Yokukansan" to obtain results from resources such as Web of Science, PubMed, Google Scholar and Sci Finder Scholar. We not only consulted the literature of fellow authors for this review but also explored classical medical books. YGS has been used to cure neurosis, sleeplessness, night weeping and restlessness in infants. Its chemical components primarily consist of triterpenes, flavonoids, phenolics, lactones, alkaloids and other types of compounds. These active ingredients displayed diverse pharmacological activities to ameliorate BPSD by regulating serotonergic, glutamatergic, cholinergic, dopaminergic, adrenergic, and GABAergic neurotransmission. In addition, YGS showed neuroprotective, antistress, and anti-inflammatory effects. The majority of cases of neurodegenerative disorders are treated with YGS, including Alzheimer's disease and dementia with Lewy bodies. Based on previous studies, YGS has been used as a traditional prescription in East Asia, such as Japan, Korea and China, and it has diverse chemical compounds and multiple pharmacological activities. Nevertheless, few experimental studies have focused on chemical and quantitative YGS studies, suggesting that further comprehensive research on its chemicals and quality assessments is critical for future evaluations of drug efficacy. [Display omitted] • Traditional uses, chemical compounds, pharmacological activities and clinical studies of Yi-Gan San (YGS) were concluded. • The research status about the traditional uses of YGS was presented in this review. • All know chemical constituents isolated from YGS and their chemical structures were proposed in this review. • The research on pharmacological effects and underlying mechanisms of YGS were summarized. • The clinical curative effects of YGS were outlined in detail. [ABSTRACT FROM AUTHOR]

Leonurus japonicus Houtt., also known as motherwort, is a traditional Chinese medicine that was first identified in Shennong Bencao Jing , the first and essential pharmacy monograph in China. L. japonicus has been regarded as a good gynecological medicine since ancient times. It has been widely used in clinical settings for treatment of gynecological diseases and postnatal rehabilitation with good efficacy and low adverse effects. The main purpose of this study was to determine the angiogenic and wound healing effects of total alkaloid fraction from L. japonicus Houtt. (TALH) in vivo and in vitro. In addition, the main bioactive components of total alkaloids were to be identified and analyzed in this study. First, the UHPLC/Q-TOF-MS method was used to identify and quantify the major components in the TALH extract. The wound healing activity was evaluated in vivo using a rat full-thickness cutaneous wound model. Histological study of wound healing in rat model was performed via immunohistochemistry and immunofluorescence. Cell proliferation was determined by MTT assay. Wound healing and transwell assays were used for detection of cell migration. The effect on tube formation was determined by tube formation assay in HUVECs. Western blot and RT-PCR were used to detect the expressions of relative proteins and genes respectively. Knock-down of SRC by siRNA was done to verify the crucial role of SRC in promotion of angiogenesis induced by TALH. Seven characteristic peaks were recognized in the UHPLC/Q-TOF-MS spectrum, while four of the main components were quantified. The wound model in rats showed that treatment of TALH promoted wound healing by stimulating cellular proliferation and collagen deposition. In vitro experiments showed that co-treatment of TALH and VEGF increased cell proliferation, migration and tube formation in HUVECs. Mechanistic studies suggested that the co-treatment increased gene expressions of SRC, MEK1/2 and ERK1/2, as well as the phosphorylation levels of these proteins. Furthermore, the effect of co-treatment was attenuated after SRC knockdown, suggesting that SRC plays an important role in angiogenesis and wound healing induced by TALH and VEGF co-treatment. Our results showed that TALH was one of the main active components of L. japonicus that promoted angiogenesis and wound healing by regulating the SRC/MEK/ERK pathway. Our study provided scientific basis for better clinical application of L. japonicas. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Polygonum chinense Linn., a folk medicine, has long been used for the treatment of diarrhea and enteritis in southwestern China. However, the components responsible for its anti-diarrheal activity are still poorly understood. Aim of the study: To determine anti-diarrheal activities of Polygonum chinense L. and to identify its active components through bioactivity-guided isolation technique. Materials and methods: Animals were orally administered with the extract of Polygonum chinense L. The anti-diarrheal effects of 75% ethanol extract, four fractions with different polarities from 75% ethanol extract, different eluates collected from Diaion HP-20 macroporous resin chromatography, ellagic acid and corilagin, were examined based on mouse models of castor oil- and magnesium sulfate-induced diarrhea. Results: The results showed that the 75% ethanol extract of Polygonum chinense L. exhibited significant anti-diarrheal activities in a dose-dependent manner in two mouse models. Through in vivo bioactivity-guided fractionation processes, n-butanol and aqueous fractions were found to exhibit prominent anti-diarrheal activities, and two major compounds, ellagic acid and corilagin, from these active fractions were found to possess anti-diarrheal effects. Conclusion: Present study provides evidence of the utilization of Polygonum chinense L. for diarrhea, and ellagic acid and corilagin are two components contributing to the anti-diarrheal effect. [Copyright &y& Elsevier]

Abstract: QFGJS is an herbal preparation, and its pronounced effectiveness in treating adjuvant-induced arthritis (AIA) has been previously demonstrated. We herein aimed to confirm its anti-arthritic effect on collagen-induced arthritis (CIA) in rats. CIA was established in female Wistar rats with intradermal injection of type II bovine collagen at the base of the tail of animals. CIA rats were treated daily with oral administration of different doses of QFGJS beginning on the day of the induction of arthritis (day 0, the prophylactic treatment) or on the day after the onset of arthritis (day 13, the therapeutic treatment) until day 30. The results showed that prophylactic treatment with QFGJS significantly suppressed the onset of arthritis, and therapeutic treatment with QFGJS markedly reduced paw swelling and ESR levels even in the established CIA. Radiologic and histopathologic changes in the arthritic joints were also significantly reduced in the QFGJS-treated versus vehicle-treated rats. Moreover, the serum levels of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 were markedly lowered in the QFGJS-treated rats. Hence, our studies demonstrate the quality, safety, and effectiveness of QFGJS as an anti-arthritic agent, which makes QFGJS a strong candidate for further clinical trials on rheumatoid arthritis (RA) patients. [Copyright &y& Elsevier]

Abstract: The root tubers of Stemona tuberosa, Stemona japonica and Stemona sessilifolia are recognized by the Pharmacopoeia of the People''s Republic of China as authentic sources of the herb Radix Stemonae (Baibu). Careful anatomical analyses of these three species, whose identities were confirmed by flowering and fruiting samples, revealed that the root tubers of Stemona tuberosa could be distinguished from those of the other two species by the presence of scattered fibers in the cortex and pith and by the absence of thickened striations on the surface of velamen cells. HPLC analyses demonstrated that the total alkaloid profiles could be grouped into four types represented as the major component by stenine-type Stemona alkaloids such as tuberostemonine (4) and neotuberostemonine (3), or by non-stenine types such as croomine (1) and stemoninine (2). Nevertheless, all these samples demonstrated different degrees of antitussive properties in guinea pigs. These results suggested that non-stenine-type of Stemona alkaloids also contributed to the antitussive properties. The variations in chemical profiles among herb samples add difficulty in ensuring quality control in botanical products. [Copyright &y& Elsevier]

Abstract: Paeoniflorin and sinomenine, derived from the root of Paeonia lactiflora Pall. (family Ranunculaceae) and the stem of Sinomenium acutum Rehder & Wilson (family Menispermaceae), respectively, have been, and are currently, widely used for treatment of rheumatic and arthritic diseases in China and Japan. Our previous studies demonstrated that sinomenine could significantly improve the bioavailability of paeoniflorin in rats, but the underlying mechanisms remain unknown. The present study aims to investigate the intestinal kinetic absorptive characteristics of paeoniflorin as well as the absorptive behavior influenced by co-administration of sinomenine using an in vitro everted rat gut sac model. The results showed a good linear correlation between the paeoniflorin absorption in sac contents and the incubation time from 0 to 90min. However, the concentration dependence showed that a non-linear correlation exists between the paeoniflorin absorption and its concentrations from 10 to 160μM, and the absorption was saturated at about 80μM of the drug. Sinomenine at 16 and 136μM concentrations could significantly enhance the absorption of paeoniflorin (20μM) by 1.5- and 2.5-fold, respectively. Moreover, two well-known P-glycoprotein inhibitors, verapamil and quinidine, could significantly elevate the absorption of paeoniflorin by 2.1- and 1.5-fold, respectively. Furthermore, sinomenine in a pattern, which influenced paeoniflorin''s absorption, manifested as similar to that of P-glycoprotein inhibitors. In conclusion, sinomenine significantly enhance the intestinal absorption of paeoniflorin, subsequently improve the bioavailability of paeoniflorin. The mechanism underlying the improvement of paeoniflorin''s bioavailability was proposed that sinomenine could decrease the efflux transport of paeoniflorin by P-glycoprotein. [Copyright &y& Elsevier]

Abstract: Paeonia lactiflora Pall. (Ranunculaceae) root and Sinomenium acutum Rehder and Wilson (Menispermaceae) stem are two herbs widely used in Chinese medicine to treat rheumatoid arthritis. While, in theory, either herb could be used alone, in practice, Chinese medicine practitioners prescribe them together. Studies on pharmacokinetic interaction between the active constituents of these two herbs (paeoniflorin and sinomenine, respectively) provide empirical evidence to support their clinical practice. A single dose of paeoniflorin (150mg/kg) alone and with sinomenine hydrochloride (90mg/kg) was administered by gastric gavage to unrestrained conscious male Sprague–Dawley rats (n =6, 250–300g). Blood samples were collected periodically via a jugular vein before and after dosing from 10min to 12h. A high-performance liquid chromatographic (HPLC) assay was developed to determine the plasma concentrations of paeoniflorin. Non-compartmental pharmacokinetic profiles were constructed by using the software PK Solutions 2.0. The pharmacokinetic parameters were compared using unpaired Student t-test. After co-administration of sinomenine, the peak plasma concentration of paeoniflorin was elevated (P <0.01), the peak time was delayed (P <0.01), the AUC0–t was increased (P <0.001), the mean residence time (MRT) was prolonged (P <0.01), the C L was decreased (P <0.01) and the V d was reduced (P <0.05). These results indicate that sinomenine hydrochloride at 90mg/kg significantly improved the bioavailability of paeoniflorin in rats. [Copyright &y& Elsevier]

Forty-four medicinal herbs were tested for antiviral activities against respiratory syncytial virus (RSV) by means of the cytopathologic effect (CPE) assay. Twenty-seven of the 44 medicinal herbs showed potent or moderate antiviral activities against RSV with 50% inhibition concentration (IC50) ranging from 6.3 to 52.1 μg/ml, and with selectivity index (SI) ranging from 2.0 to 32.1. Further purification of the active extracts from Sophora flavescens Ait. and Scutellaria baicalensis Georgi led to the identification of anagyrine (2), oxymatrine (7), sophoranol (10), wogonin (12), and oroxylin A (13) as the potent anti-RSV components. [Copyright &y& Elsevier]

Circulating tumor cells (CTCs) play an important role in tumor metastasis and may be a target for metastasis prevention. The traditional Chinese medicine Jinfukang functions to improve immunity, prevent metastasis, and prolong lung cancer patient survival periods. Yet, whether Jinfukang prevents metastasis by regulating immune cells to clearance CTCs is still unknown. To explore the anti-metastasis mechanism of Jinfukang from the perspective of regulating NK cells to clear CTCs. CTC-TJH-01 cell was treated with Jinfukang. Cytokine chip was used to detect cytokines in cell culture supernatant. Lymphocyte recruitment assay was detected by Transwell and flow cytometry. Protein expression was analysis by Western blot. LDH kit was used to detect cytotoxicity. NOD-SCID mice used for tail vein injection to study lung metastasis. Jinfukang could promote the expression and secretion of the chemokine CX3CL1 by CTCs. In addition, Jinfukang could promote the recruitment of natural killer (NK) cells by CTCs and significantly increase the cytotoxic effect of NK cells on CTCs. Moreover, Jinfukang could upregulate the expression of FasL and promote the secretion of TNF-α by NK cells and that NK cells could induce the apoptosis of CTCs through the Fas/FasL signaling pathway. Finally, we confirmed that Jinfukang could promote NK cells to kill CTCs and then inhibit lung cancer metastasis in vivo. The above effects of Jinfukang could be partially reversed by an anti-CX3CL1 mAb. These results suggest that Jinfukang may prevent lung cancer metastasis by enhancing the clearance of CTCs in the peripheral blood by NK cells, providing evidence for the anti-metastasis effect of Jinfukang. [Display omitted] [ABSTRACT FROM AUTHOR]