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Gynura procumbens (Lour.) Merr. is a well-known plant used in folkloric medicine in tropical Asian countries. The plant is prevalently employed by traditional healers in the treatment of diabetes, cancer, hypertension, inflammation, fever, and skin disorders. Several scientific studies reported that Gynura procumbens possesses considerable therapeutic value for the development of emerging treatment options. The diverse pharmacological effects of this plant are attributed to its vast phytoconstituent content. Different chemical classes, including alkaloids, flavonoids, phenolics, steroids, proteins, and polysaccharides, have been isolated from this plant. In this review, we tried to explore the different aspects of Gynura procumbens as an established medicinal plant. The data gathered here give an indication that the plant Gynura procumbens is a good natural source of chemical compounds with different types of pharmacological actions, and these chemical compounds can be used as models for the development of de novo therapeutic agents.

Gynura procumbens (GP) is a herbal medicinal plant of South-East Asian origin, popularly recognised as ‘Sambung nyawa’. The plant has been used traditionally to treat various diseases including hypertension. The anti-hypertensive activity of this plant has also been scientifically proven both in vivo and in vitro yet the investigation on its mechanisms of actions remains limited. Our previous study has demonstrated the vasodilatory action of both aqueous and methanol GP extracts possibly via activation of the cholinergic pathway and that kaempferol 3-O-rutinoside is the active ingredient responsible in mediating this effect. Hence, in this study we further confirm the involvement of the cholinergic pathway by using several pharmacological interventions, focusing on the downstream mechanism of this pathway. Our results showed that in the presence of endothelium, GP extracts induced vasodilation via activation of the muscarinic M3 receptors. However, in the absence of endothelium, GP mediated vasodilation possibly via stimulation of other muscarinic receptors and/or involvement of nicotinic receptors, a speculation that needs further investigations. GP-induced relaxation was markedly inhibited by nitric oxide (NO) blocker, L -NAME, suggesting that GP elicited ACh endothelium-dependent relaxation by producing NO in rat aortic rings. In conclusion, these data demonstrate that the vasodilatory effect of GP extracts appears to be mediated via cholinergic pathway.

BACKGROUND Ethanolic extract of G. procumbens leaves has been previously shown to possess antihyperlipidemic effects. OBJECTIVE This study was designed to prepare caffeoylquinic acids rich and poor fractions of the ethanolic extract using resin column technology and compare their antihyperlipidemic and antioxidant potentials. RESULTS Among the treatment groups, caffeoylquinic acids rich fraction (F2) and chlorogenic acid (CA, one of the major caffeoylquinic acids) showed potent antihyperlipidemic effects, with significant reductions in total cholesterol (TC), triglycerides (TG), low-density lipoprotein-cholesterol (LDL-C), very low-density lipoprotein-cholesterol (VLDL-C), atherogenic index (AI) and coronary risk index (CRI) (p

The antioxidant and anti-inflammatory potentials of polyphenols contained in Gynura procumbens (GP) extract were systematically analyzed. Polyphenols in GP were analyzed for nine peaks using high-performance liquid chromatography (HPLC) combined with mass spectrometry (MS), and quantitatively determined through each standard. A total of nine polyphenolic compounds were identified in the samples and their MS data were tabulated. To determine the potential of bioactive ingredients targeting DPPH and COX-2, we analyzed them by ultrafiltration combined with LC. The results identified the major compounds exhibiting binding affinity for DPPH and COX-2. Caffeic acid, kynurenic acid, and chlorogenic acid showed excellent binding affinity to DPPH and COX-2, suggesting that they can be considered as major active compounds. Additionally, the anti-inflammatory effect of GP was confirmed in vitro. This study will not only be used to provide basic data for the application of GP to the food and pharmaceutical industries, but will also provide information on effective screening methods for other medicinal plants.

Four new polysaccharides (GPP-20, GPP-40, GPP-60 and GPP-80) were fractionated from Gynura procumbens leaves by 20%, 40%, 60% and 80% (v/v) ethanol, successively. Their physicochemical properties including the contents of neutral sugar, uronic acid and protein, as well as the monosaccharide composition were determined. In addition, the antioxidant activities of them were investigated via the reducing power assay and scavenging capacities of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals and hydroxyl free radicals, respectively. The results indicated that apart from neutral sugar, they all contained uronic acids and proteins in their structures, which were further proved by the UV-vis and FT-IR spectra. Monosaccharide composition analysis implied that they all belonged to heteropolysaccharides consisted of arabinose, galactose, glucose, xylose and galacturonic acid with different types and ratios. What's more, GPP-20, GPP-40 and GPP-80 always exhibited better antioxidant activities than GPP-60 among these three antioxidant assays in vitro.

Gynura procumbens (Lour.) Merr. is traditionally used as a raw material for making dumplings or steamed stuffed buns, and its fresh leaves are boiled with water for tea. Herein, we established an ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS) combined with characteristic ion filtration (CIF) strategy to rapidly screen active ingredients with antioxidant and anti-inflammatory properties in G. procumbens. This strategy involved screening the active part of G. procumbens using antioxidation and anti-inflammatory activity assays; discovering the active compounds by speculating on the active site's chemical composition by UHPLC-Q-TOF-MS/MS plus CIF; and verifying the active compounds' activities. The ethyl acetate extract (EEAF) of G. procumbens was the major active site. Eighty-one compounds were identified from the EEAF using UHPLC-Q-TOF-MS/MS plus CIF. Furthermore, polyphenols such as cynarine, isochlorogenic acids A and isochlorogenic acids C have excellent antioxidizing and anti-inflammatory activities. This study provides a practical strategy for rapid in vitro screening of the antioxidizing and anti-inflammatory activities of traditional vegetables and herbs and identification of active ingredients.

Ethnopharmacology relevance Gynura procumbens (Lour.) Merr. displayed cardio-protective effect that may prevent atherogenesis. The primary underlying pathological process of cardiovascular disease is atherosclerosis. Atherosclerotic lesion composed of macrophages, T cells and other immune cells which incorporated with cholesterol that infiltrates from the blood. Aim of the study: The present study was performed to determine underlying mechanism of G. procumbens ethanol extract and its fractions such as aqueous, chloroform, ethyl acetate and hexane affect macrophage derived foam cell formation. Materials and methods Lipid droplets accumulation in treated macrophages were visualized by Oil Red O staining while the total cholesterol present in the treated macrophages were measured using Cholestryl Ester quantification assay kit. Enzyme-Linked Immunosorbent Assay (ELISA) were used to detect TNF-α and IL-1β secretion in the supernatant of treated macrophages. Gene expression of Lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1) and ATP-binding cassette transporter A-1 (ABCA-1) in treated macrophages were analyzed using Real-Time Quantitative Polymerase Chain Reaction (RT-qPCR). Results G. procumbens ethanol extract and its fractions reduced lipid droplet accumulation and total cholesterol in oxLDL-treated macrophages together with significantly reduction of TNF-α and IL-1β secretions in supernatant oxLDL-treated macrophages. LOX-1 gene expression was significantly reduced when G. procumbens ethanol extract and its fractions were added in oxDL-treated macrophages. In contrast, G. procumbens ethanol extract and its fractions significantly increased the expression of ABCA-1 gene in oxLDL-treated macrophages. Conclusion In conclusion, G. procumbens ethanol extract and its fractions inhibit the formation of macrophage derived foam cell by reducing TNF-α and IL-1β expression, which usually highly expressed in atherosclerotic plaques, suppressing scavenger receptor LOX-1 gene that binds oxLDL but induced ABCA-1 gene that mediate lipid efflux from macrophages.

Plants from Gynura family was used in this study, namely,Gynura procumbensandGynura bicolor.Gynura procumbensis well known for its various medicinal properties such as antihyperglycaemic, antihyperlipidaemic, and antiulcerogenic; meanwhile,G. bicolorremains unexploited. Several nonenzymatic antioxidants methods were utilized to study the antioxidant capacity, which include ferric reducing antioxidant power (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, total flavonoid content, total phenolic content, and ascorbic acid content determination. DPPH assay revealsG. procumbensshoot as the lowest (66.885%) andG. procumbensroot as the highest (93.499%) DPPH radical inhibitor. In FRAP assay, reducing power was not detected inG. procumbensleaf callus (0.000 TEAC mg/g FW) wherebyG. procumbensroot exhibits the highest (1.103 TEAC mg/g FW) ferric reducing power. Total phenolic content and total flavonoid content exhibited similar trend for both the intact plants analysed. In all antioxidant assays,G. procumbenscallus culture exhibits very low antioxidant activity. However,G. procumbensroot exhibited highest phenolic content, flavonoid content, and ascorbic acid content with 4.957 TEAC mg/g FW, 543.529 QEµg/g FW, and 54.723 µg/g FW, respectively. This study reveals thatG. procumbensroot extract is a good source of natural antioxidant.

A randomized complete block (RCBD) study was designed to investigate the effects of cadmium (Cd) and copper (Cu) on the growth, bioaccumulation of the two heavy metals, metabolite content and antibacterial activities in Gyanura procumbens (Lour.) Merr. Nine treatments including (1) control (no Cd and Cu); (2) Cd 2 = cadmium 2 mg/L; (3) Cd 4 = cadmium 4 mg/L; (4) Cu 70 = copper 70 mg/L; (5) Cu 140 = copper 140 mg/L); (6) Cd 2 + Cu 70 = cadmium 2 mg/L + copper 70 mg/L); (7) Cd 2 + Cu 140 = cadmium 2 mg/L + copper 70 mg/L); (8) Cd 4 + Cu 70 = cadmium 4 mg/L+ copper 70 mg/L and (9) Cd 4 + Cu 140 = cadmium 4 mg/L + copper 140 mg/L) were evaluated in this experiment. It was found that the growth parameters (plant dry weight, total leaf area and basal diameter) were reduced with the exposure to increased concentrations of Cd and Cu and further decreased under interaction between Cd and Cu. Production of total phenolics, flavonoids and saponin was observed to be reduced under combined Cd and Cu treatment. The reduction in the production of plant secondary metabolites might be due to lower phenyl alanine lyase (PAL) activity under these conditions. Due to that, the 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant potential (FRAP) and antibacterial activities was also found to be reduced by the combined treatments. The current experiments show that the medicinal properties of G. procumbens are reduced by cadmium and copper contamination. The accumulation of heavy metal also was found to be higher than the safety level recommended by the WHO in the single and combined treatments of Cd and Cu. These results indicate that exposure of G. procumbens to Cd and Cu contaminated soil may potentially harm consumers due to bioaccumulation of metals and reduced efficacy of the herbal product.

Previous studies have investigated the cardiovascular activity of Gynura procumbens Merr. single-solvent extracts. The objective of this study was to evaluate the in vitro vasorelaxant properties and the underlying pharmacological mechanisms of serial extracts and fractions of Gynura procumbens (GP). The leaves of GP were serially extracted with petroleum ether, chloroform, methanol and water using the maceration method. Suspended aortic ring preparations were pre-contracted with phenylephrine (PE 1 µM), followed by cumulative addition of GP extracts (0.25–3 mg/mL). The petroleum ether extract (GPPE) was the most potent among the four extracts. Pre-incubation of endothelium-intact aorta with atropine (1 µM), indomethacin (10 µM), methylene blue (10 µM), propranolol (1 µM) and potassium channel blockers such as TEA (1 µM), glibenclamide (10 µM), 4-aminopyridine (1 µM) and barium chloride (10 mM) had no effect on GPPE-induced vasorelaxation. The vasorelaxant effect of GPPE was partly diminished by pretreatment of aortic rings preparations with l-NAME (10 µM) and even more so in endothelium-denuded aortic rings, indicating a minimal involvement of endothelium-dependent pathway in GPPE-induced vasorelaxation. The calcium-induced vasocontractions were antagonized significantly and concentration-dependently by GPPE in calcium free and high potassium medium. These results illustrate that Ca2+ antagonizing actions of GPPE in rat isolated aorta are comparable to that of verapamil and may be mainly responsible for its vasodilation effect. The antioxidant activity of GPPE supports its vasorelaxant effect by attenuating the production of deleterious free radicals and reactive oxygen species in the vasculature.

1. The present study investigated the effects of dietary supplementation with Gynura procumbens on egg yolk and serum cholesterol and triglycerides, excreta microflora, laying performance and egg quality. 2. A total of 160 Hy-Line Brown layers (45 weeks old) were randomly assigned into 4 treatments on the basis of laying performance. Each treatment had 4 replicates with 10 birds each. 3. Dietary treatments were basal diet supplemented with 0 (control), 2.5, 5.0 and 7.5 g/kg diet G. procumbens during 56-d feeding period. 4. Serum (d 21, 42 and 56) and egg yolk (d 28, 42 and 56) cholesterol and triglycerides concentrations were linearly reduced with increasing dietary concentrations of G. procumbens. 5. Increasing dietary concentrations of G. procumbens linearly reduced the excreta total anaerobic bacteria (d 28), Clostridium sp. and Escherichia coli (d 28 and 56) populations. 6. Overall egg production and egg mass were linearly increased, and overall feed efficiency was linearly improved with increase in dietary G. procumbens. 7. Dietary increasing concentrations of G. procumbens linearly improved egg yolk colour (d 28 and 56) and breaking strength of eggs (d 56). 8. The results obtained in the present experiment indicate that dietary supplementation with G. procumbens could reduce the egg yolk cholesterol, suppresses harmful excreta microflora and improves layers performance.

Ethnopharmacological relevance: Gynura procumbens is commonly used as a traditional medicinal plant in Malaysia for treatment of many diseases. To investigate the chemopreventive properties of Gynura procumbens on azoxymethane (AOM)-induced aberrant crypt foci (ACF) in rats. Methods: Five groups of adult male rats were used in this experiment. Normal/control group; the rats were injected subcutaneously with 15 mg/kg of sterile normal saline once a week for two weeks, and orally administered with 10% Tween 20 (5 mL/kg). Carcinogen and treatment groups; the rats were injected subcutaneously each with 15 mg/kg body weight AOM once a week for 2 weeks and were continued to be fed for two months, respectively with 10% Tween 20, 500 and 250 mg/kg body weight plant extracts. Reference group; the rats were injected subcutaneously with 15 mg/kg body weight AOM once a week for 2 weeks, and injected intraperitoneally with fluorouracil 35 mg/kg body weight for five consecutive days. Result: Total ACF detected in methylene blue stained whole mounts of rat colon were 21, 23and 130 in rats fed with 500, 250 mg/kg body weight treatment and carcinogen groups, respectively. Treatment with high and low doses of the plant extract led to83.6% and 82.2% decrease in the total crypts in the groups fed 500 mg/kg and 250 mg/kg Gynura procumbens respectively compared to carcinogen group. Immunohistochemical staining of ACF showed suppressed azoxymethane induced colonic cell proliferation and Bcl-2 expression. Glutathione-S-transfarase and superoxide dismutase activities were higher in treated rats compared to carcinogen groups. Conclusion: Gynura procumbens reduced the incidence of AOM induced ACF. The findings showed that Gynura procumbens may have antiproliferative and antioxidative properties. Moreover, Gynura procumbens possesses the medicinal properties to prevent colon cancer.

Conventional fluorescent lamps that are used in tissue culture are costly light sources, exhibiting excessive wavelength emission-bandwidth that must be replaced by alternative, less costly, and much lower power-consuming energy sources. The use of Light-Emitting Diodes (LEDs) is the best option due to their potential role as elicitors of secondary metabolite production in many plant models. Gynura procumbens (G. procumbens) is widely used for treating various diseases. Here, leaf explants were cultivated in MS medium that was supplemented with 0.5 mg/L of naphthaleneacetic acid (NAA) and 2.0 mg/L of benzylaminopurine (BAP) for 30 days under white, blue, and red LEDs. Secondary metabolites were analyzed by High Performance Liquid Chromatography (HPLC) and Liquid Chromatography-Mass Spectrometry (LC-MS). Blue LEDs elicited the highest antioxidant activity, total flavonoid, and phenolic content. Furthermore, the content of cyanidin-monoglucosides significantly increased under blue light.

Ethnopharmacological relevance Gynura procumbens is applied topically for the treatment of traumatic injuries in South China. Materials and methods This study was conducted to identify the active ingredients in the essential oils from Gynura procumbens (GPEO) by Gas Chromatography-Mass Spectrometer (GC–MS) and to elucidate the mechanisms underlying the anti-inflammatory and antinociceptive effects in vivo and in vitro. Results A reduction in dswelling and pain were observed in mice treated with GPEO or its active ingredients (α-pinene, 3-carene, and limonene) compared with mice treated with a solvent control. GPEO or its three active ingredients had potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. All three ingredients inhibited nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, which could be responsible for the anti-inflammatory effect of GPEO. However, only 3-carene produced an antinociceptive effect. Conclusion Consistent with the traditional usage in Southern China, GPEO may serve as a promising potent external therapeutic agent for the treatment of chronic pain.

Gynura procumbens (Lour.) Merr. is a traditionally used medicinal plant to decrease cholesterol level, reduce high blood pressure, control diabetics, and for treatment of cancer. In our present study, a proteomic approach was applied to study the proteome of the plant that had never analyzed before. We have identified 92 abundantly expressed proteins from the leaves of G. procumbens (Lour.) Merr. Amongst the identified proteins was miraculin, a taste-masking agent with high commercial value. Miraculin made up ∼0.1% of the total protein extracted; the finding of miraculin gave a great commercial value to G. procumbens (Lour.) Merr. as miraculin's natural source is limited while the production of recombinant miraculin faced challenges of not being able to exhibit the taste-masking effect as in the natural miraculin. We believe the discovery of miraculin in G. procumbens (Lour.) Merr., provides commercial feasibility of miraculin in view of the availability of G. procumbens (Lour.) Merr. that grow wildly and easily in tropical climate.

INTRODUCTION: Gynura procumbens has been shown to decrease blood pressure via inhibition of the angiotensin‐converting enzyme. However, other mechanisms that may contribute to the hypotensive effect have not been studied. OBJECTIVES: To investigate the cardiovascular effects of a butanolic fraction of Gynura procumbens in rats. METHODS: Anaesthetized rats were given intravenous bolus injections of butanolic fraction at doses of 2.5–20 mg/kg in vivo. The effect of butanolic fraction on vascular reactivity was recorded in isolated rat aortic rings in vitro. RESULTS: Intravenous administrations of butanolic fraction elicited significant (p

Gynura procumbens (Lour.) Merr (family Compositae) is cultivated in Southeast Asia, especially Indonesia, Malaysia and Thailand, for medicinal purposes. This study evaluated the in vivo hypoglycemic properties of the water extract of G. procumbens following 14 days of treatment and in vitro in RIN-5F cells. Glucose absorption from the intestines and its glucose uptake in abdominal skeletal muscle were assessed. The antidiabetic effect of water extract of G. procumbens leaves was investigated in streptozotocin-induced diabetic rats. The intraperitoneal glucose tolerance test (IPGTT) was performed in diabetic rats treated with G. procumbens water extract for 14 days. In the IPGTT, blood was collected for insulin and blood glucose measurement. After the IPGTT, the pancreases were collected for immunohistochemical study of β-cells of the islets of Langerhans. The possible antidiabetic mechanisms of G. procumbens were assessed through in vitro RIN-5F cell study, intestinal glucose absorption and glucose uptake by muscle. The results showed that G. procumbens significantly decreased blood glucose levels after 14 days of treatment and improved outcome of the IPGTT. However, G. procumbens did not show a significant effect on insulin level either in the in vivo test or the in vitro RIN-5F cell culture study. G. procumbens also showed minimal effects on β-cells of the islets of Langerhans in the pancreas. However, G. procumbens only significantly increased glucose uptake by muscle tissues. From the findings we can conclude that G. procumbens water extract exerted its hypoglycemic effect by promoting glucose uptake by muscles.

Gynura procumbens (Lour.) Merr. is an evergreen edible vine in southern China. The antioxidant activity and metabolites of chlorogenic acid dimer from Gynura procumbens (Lour.) Merr. were evaluated by the model of in vitro digestion and in vivo metabolomics approach, respectively. Moreover, metabolites of chlorogenic acid dimer in blood and urine of Sprague-Dawley rats were determined by HPLC-ESI-QTOF-MS/MS. In vitro digestion results suggested the antioxidant activity of the purified chlorogenic acid dimer was significantly enhanced after simulated digestion. Meanwhile, in vivo metabolism results showed that 7 and 20 new metabolites were observed in blood and urine, respectively, suggesting that hydrolysis along with methylation, glucuronidation and other reactions may all happen when the chlorogenic acid dimer entered the digestive and metabolic systems, which inducing and exhibiting various biological activities through metabolism. PRACTICAL APPLICATIONS: Gynura procumbens (Lour.) Merr. (GPM) is an evergreen edible vine with the effects of anticancer, anti-inflammatory, antiviral, depressurization, and antioxidation. As a health care vegetable, it is not usually eaten in daily life. Our current study shows that chlorogenic acid dimer extracted from GPM has a significant enhanced antioxidant ability after gastro-intestinal digestion in vitro, and their metabolites in vivo of urine is far more than that of blood, which may indicate that the chlorogenic acid dimer can be fully absorbed and decomposed through the gastro-intestinal digestion and metabolism. Thus, GPM could be used as a functional food ingredient for antioxidant enhancement to promote the economic value. The research also provides theoretical data for the intensive processing and utilization of GPM, as well as for the relative research on digestion and metabolism of edible plants.

Aims of the study Gynura procumbens (Merr.), which is known as “Sambung nyawa”, is widely used in South East Asian countries in the traditional treatment of many ailments. However, there is little toxicological information available regarding safety following repeated exposure. The present investigation describes the toxicity of a methanol extract of Gynura procumbens leaves in rats. Materials and methods For acute toxicity studies, a methanol extract of Gynura procumbens was orally administered to Sprague–Dawley rats (female and male) at a dose range of 1000–5000 mg/kg. For sub-chronic toxicity studies, the rats were orally administered the methanol extract of Gynura procumbens at the doses of 125, 250, and 500 mg/(kg day) for a period of 13 weeks. The animals were sacrificed, followed by examination of their organs and blood serum. Results and conclusions Administration of the methanol extract from Gynura procumbens leaves at 1000–5000 mg/kg did not produce mortality or significant changes in the general behaviour, body weight, or organ gross appearance of rats. There were no significant differences in the general condition, growth, organ weights, haematological parameters, clinical chemistry values, or gross and microscopic appearance of the organs from the treatment groups as compared to the control group. Therefore, the NOAEL for the Gynura procumbens methanol extract is 500 mg/(kg day) administered orally for 13 weeks.

Aqueous extracts of Gynura procumbens (Lour.) Merr. were orally administered to spontaneously hypertensive (SHR) rats for 4 weeks, and antihypertensive effects were determined. Oral administration of 500 mg/kg of G. procumbens (Lour.) Merr. extract (GPE) resulted in significantly lower blood pressure in SHR rats compared with SHR rats not given GPE (P < .05). Furthermore, GPE-administered rats had significantly lower serum lactate dehydrogenase, creatine phosphate kinase, and increased nitric oxide (NO), a known vasodilator, compared with the non–GPE-administered SHR group (P < .05). These results suggest that oral administration of aqueous GPE may be useful for prevention and treatment of hypertension through increasing NO production in blood vessels.

To study the antidiabetic activity of Gynura procumbens (G. procumbens) used in the traditional management of diabetes in Southern Asia.G. procumbens leaves were extracted sequentially with graded percentage of ethanol in water (95%, 75%, 50%, 25% and 0%), and the extracts were tested for antidiabetic activity using acute (7 h), subcutaneous glucose tolerance test and sub-chronic (14 d) test in non-diabetic and streptozotocin-induced diabetic rats. The extracts were further subjected to phytochemical studies.In acute dose (1 g/kg), the extracts significantly lowered fasting blood glucose (FBG) in streptozotocin-induced diabetic rats (P0.05). However, the FBG-lowering effect of the 25% extract compared to the other extracts, was rapid (47% after 2 h) and the highest: 53%, 53% and 60% in the 3rd, 5th, and 7th h, respectively (P0.05), comparable only to the effect of metformin. Furthermore, the extracts suppressed peak FBG in subcutaneous glucose tolerance test, but only the 0% and 25% extracts, and metformin sustained the decrease until the 90th min (P0.05). Moreover, in the 14 days study, the 25% extract exerted the highest FBG-lowering effect, namely 49.38% and 65.43% on days 7 and 14, respectively (P0.05), similar to the effect of metformin (46.26% and 65.42%). Total flavanoid and phenolic contents in the extracts were found to decrease with increase in polarity of extraction solvents. The composition of reference compounds (chlorogenic acid, rutin, astragalin and kaempferol-3-O-rutinoside) followed a similar trend.G. procumbens contains antidiabetic principles, most extracted in 25% ethanol. Interaction among active components appears to determine the antidiabetic efficacy, achieved likely by a metformin-like mechanism.

Background Previous studies of Gynura procumbens (G. procumbens) have shown that partially purified fractions of the leaves are capable of lowering the blood pressure of rats by inhibiting angiotensin-converting enzymic activity and causing vasodilatation. The objectives of this study were therefore to further purify the active compounds that exhibited selective effects on blood vessels, determine the mechanism of actions, and to qualitatively analyse the putative compounds present. Methods The butanolic fraction (BU) of the crude ethanolic extract was purified using column chromatography to obtain several sub-fractions of different polarities. The in vitro effects of BU and the sub-fractions on vascular tension were subsequently determined using isolated rat thoracic aortic rings. The most potent sub-fraction (F1) alone was then investigated for its mechanisms of the vasorelaxant activity. In another experiment, thin-layer chromatography was used to qualitatively analyse the active compounds found in F1. Results The BU and the sub-fractions ranging from 10-7 to 10-2 g/ml significantly (p -4 – 1 x 10-2 M) in calcium-free with high concentration of potassium as well as in calcium- and potassium-free Krebs-Henseleit solutions. Contractions induced by noradrenaline and caffeine were not affected by F1. The vasorelaxing effect caused by F1 was significantly attenuated with preincubation of potassium channel blockers (glibenclamide and 4-aminopyridine) and prostacyclin inhibitor (indomethacin) while it was not affected by preincubation with tetraethylammonium, l-nitro-arginine methyl esther, propanolol, atropine, oxadiazolo quinoxalin one and methylene blue. The qualitative phytochemical analysis of F1 indicated the presence of flavonoids. Conclusion These results confirm previous findings that G. procumbens causes vasodilatory effects by blocking calcium channels. In addition, the present study further demonstrates that the vasodilatory effect of G. procumbens may also be due to the opening of potassium channels and the stimulation of prostacyclin production. The putative compounds are probably flavonoids in nature.

Previous studies showed that Gynura procumbens reduced blood pressure by blocking calcium channels and inhibiting the angiotensin-converting enzyme activity. The present experiments were to further explore the effects and mechanisms of a purer aqueous fraction (FA-I) of G. procumbens on angiotensin I (Ang I)-induced and angiotensin II (Ang II)-induced contraction of aortic rings and also on the bradykinin (BK) effect on cardiovascular system. Rat aortic rings suspended in organ chambers were used to investigate the vascular reactivity of FA-I. Effect of FA-I on BK was studied by in vitro and in vivo methods. Results show that FA-I significantly (P < 0.05) decreased the contraction evoked by Ang I and Ang II. In the presence of indomethacin (10 µM) or N-nitro-L-arginine methyl ester (0.1 µM), the inhibitory effect of FA-I on Ang II-induced contraction of aortic rings was reduced. Besides, FA-I potentiated the vasorelaxant effect and enhanced the blood pressure-lowering effect of BK. In conclusion, FA-I reduced the contraction evoked by Ang II probably via the endothelium-dependent pathways, which involve activation of the release of nitric oxide and prostaglandins. The inhibition of angiotensin-converting enzyme activity by FA-I may contribute to the potentiation of the effects of BK on cardiovascular system.

Ethnopharmacological relevance Gynura procumbens Merr. (Asteraceae) has been used as a traditional remedy for various skin diseases in certain areas of Southeast Asia. Aim of the study In order to evaluate the protective activity of Gynura procumbens extract on skin photoaging and elucidate its mode of action. Materials and methods Matrix-metalloproteinase (MMP)-1 and -9 expressions were induced by UV-B irradiation in human primary dermal fibroblasts. MMP-1 expression level was measured by enzyme-linked immunosorbent assay (ELISA) and Western blot analysis. Zymography was employed for evaluating the enzymatic activity of MMP-9. Anti-inflammatory activity and anti-oxidative capacity of the extract were evaluated by ELISA and dichlorodihydrofluorescein diacetate (DCF-DA) assay. Results The ethanolic extract of Gynura procumbens inhibited MMP-1 expression up to 70% compare to negative control group. The enzymatic activity of MMP-9 was inhibited around 73% by the treatment of 20 μg/mL of the extract. The extract markedly reduced the production of reactive oxygen species (ROS). Gynura procumbens extract showed an inhibitory effect on releasing pro-inflammatory cytokines (IL-6 and IL-8) in human HaCat keratinocyte. Conclusion The ethanolic extract of Gynura procumbens inhibited MMP-1 and MMP-9 expressions induced by UV-B irradiation via inhibition of pro-inflammatory cytokine mediator release and ROS production.

Gynura procumbens is used in Thai folk medicine to treat topical inflammation, rheumatism, and viral ailments. In the present work, attempts were made to verify the folk medicinal claim that the crude ethanolic extract of G. procumbens has antiinflammatory action and to relate the activity to particular fractions using a croton oil-induced mouse ear inflammation model. The original ethanolic extract of G. procumbens was partitioned between water and ethyl acetate. The residues were subjected to antiinflammatory evaluation. While the water extract did not show any antiinflammatory activity, the administration of the original organic extract significantly inhibited the increase in ear thickness in response to croton oil (n = 5). The activity of 0.75 mg/ear original organic extract showed similar antiinflammatory activity (inhibition 65.2%) to that of 6 mg/ear hydrocortisone 21-hemisuccinate sodium salt (inhibition 64.8%). The organic extract was then fractionated with a series of solvents in order of increasing polarity. Each fraction was dried, dissolved in acetone and monitored using the same bioassay. These experiments showed that the hexane and toluene fractions showed significant inhibitions of 44.6% and 34.8%, respectively. These two fractions had similar activities to 4 mg/ear of hydrocortisone (inhibition 35.0%). The possible chemical constituents in the extracts and fractions were investigated using thin layer chromatography and specific color reagents. These tests showed that steroids might be one class of antiinflammatory compounds in this plant.

Gynura procumbens (Lour.) Merr. belongs to the Asteraceae Family. The plant is a well-known traditional herb in South East Asia and it is widely used to treat inflammation, kidney discomfort, high cholesterol level, diabetic, cancer and high blood pressure. Our earlier study showed the presence of valuable plant defense proteins, such as peroxidase, thaumatin-like proteins and miraculin in the leaf of G. procumbens. However, the effects of these defense proteins on cancers have never been determined previously. In the present study, we investigated the bioactivity of gel filtration fractionated proteins of G. procumbens leaf extract. The active protein fraction, SN-F11/12, was found to inhibit the growth of a breast cancer cell line, MDA-MB-231, at an EC50 value of 3.8 µg/mL. The mRNA expressions of proliferation markers, Ki67 and PCNA, were reduced significantly in the MDA-MB-23 cells treated with SN-F11/12. The expression of invasion marker, CCL2, was also found reduced in the treated MDA-MB-231 cells. All these findings highlight the anti-cancer property of SN-F11/12, therefore, the proteins in this fraction can be a potential chemotherapeutic agent for breast cancer treatment.

There is currently a great deal of research interest in utilizing plant compounds against human diseases, including hypertension. The present study investigated the effects of different extracts and fractions from leaves of Gynura procumbens Merr. on rat atrial contraction in vitro. Isolated left and right atria, mounted in a 20-ml organ bath, were allowed to equilibrate for 15 min before the application of the extracts or fractions. The extracts (petroleum-ether extract (PE) and methanol extract (ME)) and the fractions (chloroform fraction (CHL), ethyl-acetate fraction (EA), n-butanol fraction (NB) and water fraction (WA) of the methanol extract) were tested at three concentrations (0.25, 0.5 and 1.0 mg/ml), with a β-adrenergic agonist (isoprenaline) as a control. All data on contraction responses were log-transformed and analyzed. When exposed to the different extracts, both atria tended to exhibit greater contractive responses with the NB whereas cardiac contractions had a tendency to be reduced with most other extracts. For a given extract, the contraction responses were particularly greater at 0.5 mg/ml for the right atrium and at 1 mg/ml for the left atrium. Further analysis focusing on the NB fraction revealed that positive inotropism was greater in left atria exposed to highly-concentrated F2 and F3 sub-fractions. Taken together, our results suggest that NB extracts and fractions from the G. procumbens-leaf methanol extract have positive inotropic activities and, hence, can be considered as an alternative/traditional medicine against increased blood pressure in humans or can be used in strategies aimed at finding antihypertensive biomolecules from an accessible source.