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In a bid to make the use of functional food easier in the management and prevention of diseases, product development and fortification from/with functional foods have become the recent focus of research. This study, therefore, sought to exploit the recent trend in the brewing industry on the production of non-alcoholic beers by investigating the possibility of having a non-alcoholic beer flavored with bitter leaf, a known plant widely reported to have a strong hypoglycemic effect, as against the traditional use of hops, and the effect of the produced beer on the glycemic indices and various diabetic biochemical parameters that serve as biomarkers for type-2 diabetes (T2D). The glycemic indices, as well as the inhibitory potentials of bitter leaf-flavored Non-alcoholic wheat beer (NAWB) in ratios of 100%HP, 100%BL, 75:25BL, 50:50BL, and 25:75BL, on enzymes linked to a high-fat diet/streptozocin (HFD/STZ)-induced T2D albino Wistar rats were investigated. There were no significant difference (p .05) between the starch (1.72-1.77 mg/100 mL), amylose (0.22-0.24 mg/100 mL), and amylopectin (1.49-1.53 mg/100 mL) contents of the various samples. The Glycemic Index (GI) of the samples ranged from 36 to 73 with 75:25Bl and 50:50BL have the lowest (36) values. The samples reduced blood glucose levels and inhibited pancreatic α-amylase, lipase, and intestinal α-glucosidase activity. The inhibitory potentials of these beer samples on α-amylase and α-glucosidase as well as their ability to reduce blood glucose levels in diabetic rats thus making the bitter leaf flavored NAWB a suitable healthy beverage for better glycemic control in diabetics. PRACTICAL APPLICATIONS: This study revealed the potential of producing non-alcoholic wheat beer flavored with bitter leaves as a possible substitute for hops. The potential inherent in bitter leaf in the management of type 2 diabetes can thus be made available through a far-reaching beverage medium such as non-alcoholic beer to help in the treatment/management of T2D. The results of this research could be an eye-opener to the possible utilization of bitter leaf and by extension other plants that have been reported in the management of T2D. The use of the bitter leaf as a substitute for hops in the production of non-alcoholic beer in the brewing industry could help in a health-oriented campaign for safe drinks that could be helpful in the control of blood glucose levels of diabetic patients.

Objective This study aims to investigate antidiabetic activity of several Vernonia amygdalina extracts to study their potential use in medicine. Methods Aqueous and ethanol extracts were obtained by maceration and Soxhlet extraction from roots and leaves of V. amygdalina. The extracts were tested as inhibitors of α-glucosidase activity and of advanced glycation end products (AGEs) formation. Further, radical scavenging activity was examined detecting the oxygen radical absorbance capacity, while the potential cytotoxicity of extracts was estimated with MTT assay. Key findings In aqueous and ethanol extracts, several polyphenolic compounds were identified; in detail, (-)-catechin and luteolin were found in leaf extracts, while caffeic acid, chlorogenic acid and the terpenoid vernodalol were recognized in root extracts. Regarding antidiabetic activity, the aqueous root extracts efficiently inhibited α-glucosidase activity in a concentration-dependent manner (IC50 = 5.6 µg/ml and 39.8 µg/ml, respectively of macerated and Soxhlet extracts), whereas those obtained from leaves exhibited lower potency. Furthermore, AGEs formation was reduced by all V. amygdalina extracts starting from 10 µg/ml. Conclusions The aqueous extracts of V. amygdalina roots obtained by maceration and Soxhlet extraction show remarkable anti-α-glucosidase activity, and all extracts have favourable antiglycation and antioxidant activities.

Secondary metabolites produced by endophytic fungi are an important source of biologically active compounds. The current research was focused on the biological activities of ethyl acetate extracts of fungi, isolated and identified from

When tested in the acetic acid-induced writhing and formalin-induced paw-licking tests, the ethanol extract of Vernonia patula (VP) aerial parts showed significant antinociceptive activity. In neuropharmacological tests, it also significantly delayed the onset of sleep, increased the duration of sleeping time, and significantly reduced the locomotor activity and exploratory behaviour of mice. Five phenolic compounds, namely gallic acid, vanillic acid, caffeic acid, quercetin and kaempferol, were detected in VP following HPLC-DAD analysis. The presence of these phenolic compounds in VP provides some support for the observed antinociceptive and sedative effects. A computational study was performed to predict the binding affinity of gallic acid, vanillic acid, caffeic acid, quercetin and kaempferol towards the cannabinoid type 1 (CB1) receptor. Caffeic and vanillic acid showed the highest probable ligand efficiency indices towards the CB1 target. Vanillic acid displayed the best blood brain barrier penetration prediction score. These findings provide some evidence for the traditional use of VP to treat pain.

Uncontrolled inflammation causes health problems. Extracellular signal-regulated kinase (ERK) phosphorylates signal transducer and activator of transcription 3 (STAT3) at Ser727, resulting in inflammation. The leaf of Vernonia amygdalina (VA) is a medicinal herb for managing inflammation-associated diseases. Oral administration or topical application of VA leaf extract exerts anti-inflammatory effects in rat models. However, the anti-inflammatory mechanisms of the herb are not fully understood.In this study, we aimed to investigate the involvement of ERK/STAT3 (Ser727) signaling in the anti-inflammatory effects of an ethanolic extract of VA leaves.Extracts of VA leaves were prepared with different concentrations of ethanol. A LPS-stimulated RAW264.7 cell model was used for in vitro assays, and a TPA (12-O-tetradecanoylphorbol-13-acetate)-induced ear edema mouse model was employed for in vivo assays. The 95% ethanol extract of VA leaves (VAE) exerted the strongest inhibitory effect on nitric oxide (NO) production in LPS-stimulated macrophages; thus it was selected for use in this study. Hematoxylin and eosin (HE) staining was used to examine pathological conditions of mouse ear tissues. Griess reagent was employed to examine NO generation in cell cultures. Immunoblotting and ELISA were used to examine protein levels, and RT-qPCR was employed to examine mRNA levels.Topical application of VAE ameliorated mouse ear edema induced by TPA. VAE suppressed the phosphorylation of ERK (Thr202/Tyr204) and STAT3 (Ser727); and decreased protein levels of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin (IL)-6, IL-1β and tumor necrosis factor-α (TNF-α) in the mouse ear tissues and in LPS-stimulated RAW 264.7 cells. VAE also inhibited NO production, and lowered mRNA levels of IL-6, IL-1β and TNF-α in the macrophages.VAE ameliorates TPA-induced mouse ear edema. Suppression of ERK/STAT3 (Ser727) signaling is involved in VAE's anti-inflammatory effects. These novel data provide further pharmacological justifications for the medicinal use of VA in treating inflammation-associated diseases, and lay the groundwork for developing VAE into a new anti-inflammatory agent.

Background Lipotropic molecules are effective therapeutic targets to counteract non-alcoholic fatty liver disease (NAFLD). Lipotropic compounds are capable of removing fat from the liver and/or manage the reduction of the synthesis or deposition of lipids in the liver. The objective of this study was to evaluate the lipotropic effects of the aqueous extract of leaves of Vernonia guineensis (AEVG) on rats fed high fat diet. Methods Twenty male rats with an average mass of 235 g were allow acclimatize for seven days, following which they were divided into four groups of five animals each. The test group was treated with high fat diet (HFD) and AEVG at 400 mg/kgBW, while positive control group received HFD and Fenofibrate at 100 mg/kgBW. The normal control group received a normal diet; and the negative control group received HFD. After 14 days of treatment, animals were sacrificed, blood and organs (liver, heart and kidneys), as well as the faeces were collected for the preparation of plasma and homogenates respectively. Some markers of lipid profil (total cholesterol, triglycerides, HDL-c, LDL-c,) and markers of toxicity (AST, ALT, γ-GT, creatinine) were evaluated. Results The results obtained showed that a HFD at the hepatic level led to the accumulation of lipids (triglycerides (TG) and total cholesterol (TC)) and had adverse effects on hepatic function by promoting cytolysis. At the plasma level, HFD induced hyperlipidemia. Administration of AEVG at 400 mg/kgBW improved the blood lipid profile and reduced the storage of TG and cholesterol in the liver. AEVG also promoted fecal cholesterol excretion and reduced atherogenic indices which include Total Cholesterol/High-Density Lipoprotein cholesterol (TC/HDL-c) and Low-Density Lipoprotein cholesterol/High-Density Lipoprotein cholesterol (LDL-c/HDL-c). The extract exhibited hepato-protective activity (anticholestasis) and improved glomerular filtration. Conclusion These findings suggest that AEVG possesses lipotropic effects confirming its probable use in the management of non-alcoholic fatty liver disease and its cardiometabolic complications. This virtue could be exploited for local pharmaceutical development.

BackgroundVernonia anthelmintica (L.) willdis a traditional urgur herb in China for a long history. Its alcohol extract (AVE) has been proved to promote hair follicle growth in C57BL/6 mice. We conducted this study to investigate the hair-growth effects of AVE in stressed mice and its possible mechanism of action.MethodsThe hair-follicle growth effects of AVE were examined by in vivo and in vitro study. We exposed C57BL/6 male mice to chronic restraint stress to induce murine hair follicle growth inhibition. The effects of AVE were examined by histological analysis, immunofluorescence for Ki67 and cytokeratin 19 immunoreactivity, western blot assay in tyrosinase and related proteins expressions and immunofluorescence for nerve fibers. In organ culture of mouse vibrissae follicles, we used substance P as a catagen-inducing factor of hair follicle growth, and measured the elongation of hair shafts and expression of neurokinin-1 receptor protein by application of AVE.ResultsOur results showed that AVE counteract murine hair follicle growth inhibition caused by chronic restraint stress via inducing the conversion of telogen to anagen and inhibiting catagen premature, increasing bulb keratinocytes and bulge stem cells proliferation, promoting melanogenesis, and reducing the numbers of substance P and calcitonin gene-related peptide nerve fibers. Furthermore, AVE also counteracted murine hair follicle growth inhibition caused by substance P in organ culture.ConclusionThese results suggest that AVE counteract stress-induced hair follicle growth inhibition in C57BL/6 mice in vivo and in vitro, and may be an effective new candidate for treatment of stress-induced hair loss.

A bioactive component, 2',3,4,4'-tetrahydrochalcone (RY3-a) was first isolated from Vernohia anthelmintica (L.) willd seeds, and a set of its analogs, RY3-a-1-RY3-a-15 and RY3-c were designed and synthesized. Biological activity assays showed that RY3-c exhibited better melanogenesis and antioxidant activity and lower toxicity in comparison with RY3-a and butin. Further study tests showed that RY3-c exhibited better melanogenesis activity compared with the positive control 8-methoxypsoralan (8-MOP) in a vitiligo mouse model, suggesting that RY3-c is a good candidate antivitiligo agent. Mechanistic studies showed that RY3-c could repair cell damage induced by excessive oxidative stress and may exert melanin synthesis activity in the mouse melanoma B16F10 cell line by activating the mitogen-activated protein kinase (MAPK) pathway and the upregulation of c-kit.

Background: Both young and old leaves of Vernonia amygdalina (VA) are traditionally used to treat inflammation, pain and fever. However, the efficacy of young and old leaves for treating these ailments have not been compared till date. Aim: To ascertain the effect of young and old leaves of VA in managing inflammation, pain and fever. Methods: Both quantitative and qualitative phytochemical screening of ethanol extracts of young (EthYL) and old (EthOL) leaves of VA were performed. The anti-inflammatory activity of orally administered EthYL and EthOL (50–200 mg/kg) and Diclofenac (10 mg/kg) were evaluated in carrageenan-induced inflammation model in rats. Antipyretic activity of EthYL, EthOL and Aspirin (25 mg/kg) were assessed in the Baker’s yeast-induced pyrexia model. Anti-allodynic effect of both extracts were evaluated by inserting inflamed paws of rats in cold water. Antinociceptive property of the extracts were assessed using tail withdrawal and formalin-induced nociception test. Histopathological examination of the paws was performed, in addition to formalin test to understand the possible mechanism of action of the extracts. Negative control rats received 2 ml/kg normal saline in all tests. Results: The amount of flavonoids, alkaloids, tannins, and phenolics were significantly (p

The ethyl acetate, ethanol, and aqueous extracts sequentially obtained from the leaves of Vernonia amygdalina were investigated for their antidiabetic and antioxidant protective effect in oxidative hepatic injury. The extracts showed significant (p < .05) free radical scavenging and reducing power activities. They significantly (p < .05) elevated reduced glutathione level, superoxide dismutase, and catalase activities, with concomitant depletion of malondialdehyde level. The ethanol and aqueous extracts caused a removal of oxidative-included chemical functional group at 1,500-1,200 (amide II)/cm region, with the inclusion of a functional group at 3,000-2,800 (carboxylic acid)/cm region. The extracts significantly (p < .05) inhibited the activities of α-glucosidase and α-amylase and stimulated glucose uptake in rat muscles. Gas chromatography-mass spectrometric (GC-MS) analysis revealed phytol as the predominant compound, with ethanol having the highest concentration. Based on the IC50 values, the ethanol extract exhibited the best activities, followed by the ethyl acetate extract, while the aqueous extract was the least. These results suggest the antioxidative and antidiabetic properties of V. amygdalina as evident by their modulation of antioxidant biomarkers and oxidative-induced chemistry changes and stimulate muscle glucose uptake. PRACTICAL APPLICATIONS: Vernonia amygdalina (bitter leaf) is amongst the common leafy vegetables in West Africa reported for its various medicinal and nutritional properties. It is utilized as a food ingredient as well as supplement for the treatment and management of type 2 diabetes. The ability of its extracts to stimulate glucose uptake and protect against diabetic-induced changes in the chemical functional groups of the liver gives more credence to its reported antidiabetic properties. Being a common leafy vegetable, V. amygdalina can be a cheap source of nutraceutical for the treatment and management of type 2 diabetes and its complications.

Vernolide-A and vernodaline are sesquiterpene lactones isolated from genera of Vernonia. Vernolide-A and vernodaline have shown promising therapeutic properties, including antibacterial, antihelminth, and antioxidant activities. Recently, the anticancer properties of these sesquiterpene lactones have been investigated with the elucidation of effects on cell proliferation, metastasis, angiogenesis, and apoptosis. The antiproliferation and antimetastatic activities arise from targeting extracellular signal-regulated kinase 1 (ERK-1), extracellular signal-regulated kinase 2 (ERK-2), nuclear factor-κB (NF-κB), signal transducer and activator of transcription 3 (STAT3), matrix metalloproteinase 2 (MMP-2), and matrix metalloproteinase 9 (MMP9). The induction of apoptosis is due to the enhancement of caspase 9, caspase 3, while inhibition of Bcl-2 and Bcl-xL results in the release of cytochrome c into the cytosol. The activity of vernolide-A and vernodaline is hypothesized to be due to thiol reactivity through the α-methylene-γ-lactone group of sesquiterpene lactones. This review will give a brief summary of the anticancer activity of vernolide-A and vernodaline and provide information on the underlying molecular mechanisms.

The present study aimed to evaluate the antileishmanial effect, the mechanisms of action and the association with miltefosine of Vernonia brasiliana essential oil against Leishmania infantum promastigotes. This essential oil was obtained by hydrodistillation and its chemical composition was determined by gas chromatography-mass spectrometry (GC–MS). The antileishmanial activity against L. infantum promastigotes and cytotoxicity on DH82 cells were evaluated by MTT colorimetric assay. Ultrastructural alterations were evaluated by transmission electron microscopy. Changes in mitochondrial membrane potential, in the production of reactive oxygen species, and analysis of apoptotic events were determined by flow cytometry. The association between the essential oil and miltefosine was evaluated using the modified isobologram method. The most abundant component of the essential oil was β-caryophyllene (21.47 %). Anti-Leishmania assays indicated an IC50 of 39.01 ± 1.080 μg/mL for promastigote forms after 72 h of treatment. The cytotoxic concentration for DH82 cells was 63.13 ± 1.211 μg/mL after 24 h of treatment. The effect against L. infantum was proven through the ultrastructural changes caused by the oil, such as kinetoplast and mitochondrial swelling, vesicles in the flagellar pocket, discontinuity of the nuclear membrane, nuclear fragmentation and condensation, and loss of organelles. It was observed that the oil leads to a decrease in the mitochondrial membrane potential (35.10 %, p = 0.0031), increased reactive oxygen species production, and cell death by late apoptosis (17.60 %, p = 0.020). The combination of the essential oil and miltefosine exhibited an antagonistic effect. This study evidences the antileishmanial action of V. brasiliana essential oil against L. infantum promastigotes.

Vernonia [Vernonia galamensis (Cass.) Less.] (Asterales: Asteraceae) was examined as a potential trap crop for the cotton (Gossypium hirsutum L., Malvales: Malvaceae) arthropod complex. Four rows of vernonia were embedded within a 96-row cotton field. The abundance of true bug pests, true bug predators, and spiders were determined by whole-plant and sweep net sampling procedures during the early, middle, and late phases of the cotton-growing season. The census data showed that the arthropods had a strong preference for the vernonia trap crop throughout the cotton-growing season. The movement of the arthropods from the trap crop into cotton was also measured using the protein immunomarking technique as a mark–capture procedure. The arthropods inhabiting the vernonia trap crop were marked directly in the field with a broadcast spray application of egg albumin (protein) during each phase of the study. In turn, the captured specimens were examined for the presence of the mark by an egg albumin-specific enzyme-linked immunosorbent assay. Very few marked specimens were captured beyond the vernonia trap crop 1, 3, and 6 d after each marking event. The arthropods’ strong attraction and fidelity to vernonia indicate that it could serve as a trap crop for cotton pests and a refuge for natural enemies.

In this study, we synthesised the zinc oxide nanoparticles from

Introduction Sitophilus zeamais infestation is among the major setbacks to sustainable maize farming and availability. It causes an estimated annual loss of 5–10% and 20–30% of the total maize grains loss in the temperate and tropical zones, respectively. Although synthetic pesticides are quick and effective in managing crop pests, their overuse and misuse is discouraged due to their detrimental effects on human and environment. Natural pesticidal products that are extracted from plants are particularly gaining importance as an alternative to synthetic pesticides. They are available, easily biodegraded and have low toxicity to nontarget organisms. Most botanical pesticides act on insects by repelling them away from the crops in the field or in the stores. Therefore, this study aimed to determine repellency potential of organic leaf extracts of Tithonia diversifolia and Vernonia lasiopus on S. zeamais. Materials and methods. The phytochemical profile of T. diversifolia and V. lasiopus was determined using GC-MS. Laboratory-based experiments were carried out using area preference method to assess the efficacy of the extracts against weevils for a test period of 5 h. Six groups of experiments were set up with ten S. zeamais in each test: positive control (Actellic), negative control (solvent only), and four different experimental extract concentrations (25, 50, 75, and 100%). Results The results indicated that T. diversifolia and V. lasiopus leaf extracts possess potent repellency effect on weevils. All the extracts simply discouraged S. zeamais from the treated areas recording significantly good levels of repellent activities between 26 and 96%. Furthermore, the GC-MS analysis manifested the presence of bioactive compound in the extracts which are associated with the repellency effects. Conclusion The study scientifically confirms the traditional use of the T. diversifolia and V. lasiopus and provides important platform for further study on the extracts as bioresource of botanical repellent.

Nine components (C1-C9) were isolated from chloroform fraction of fractionated methanol extracts of

This study emphasized on the neuroprotective properties of bitter leaf alkaloid-rich extract (BLAE) using transgenic fruit fly (

Objective The aim of this study was to investigate the antiplasmodial effects of the crude aqueous, methanol and chloroform extracts of the leaves of Vernonia adoensis in Plasmodium berghei infected Swiss albino mice using Peters’ 4-day suppressive test. Results The number of mice used for the toxicity test was 20 (5/group) and for each extract and control groups 5 mice per group was used. The aqueous, methanol and chloroform extracts of V. adoensis leaves indicated statistically significant (P

Vitiligo is a depigmentation disorder of the skin. It is primarily caused by the destruction of melanocytes or obstruction of the melanin synthesis pathway. Melanin is a type of skin pigment that determines skin color. The seeds of Vernonia anthelmintica (L.) Willd (Kaliziri) are used for treating skin diseases including vitiligo in traditional Uyghur medicine. 1,5‑Dicaffeoylquinic acid (1,5‑diCQA) is a natural polyphenolic compound widely distributed in plants and extracted from Kaliziri seeds. Therefore, in the present study, the effect of 1,5‑diCQA on melanin synthesis in B16 cell was evaluated, and its molecular mechanism was explored. The results indicated that 1,5‑diCQA treatment of B16 cells stimulated an increase of intracellular melanin level and tyrosinase (TYR) activity without cytotoxicity. Reverse transcription quantitative polymerase chain reaction results also indicated that 1,5‑diCQA may markedly improve the protein expression and RNA transcription of microphthalmia‑associated transcription factor (MITF), melanogenic enzyme Tyr, tyrosinase‑related protein 1 (TRP 1) and tyrosinase‑related protein 2 (TRP 2). Additional results identified that 1,5‑diCQA may promote the phosphorylation of p38 mitogen‑activated protein kinase (p38 MAPK) and extracellular signal‑regulated kinase (ERK) MAPK. Notably, the increased levels of intracellular melanin synthesis and tyrosinase expression induced by 1,5‑diCQA treatment were significantly attenuated by the protein kinase A (PKA) inhibitor H‑89. Intracellular cyclic adenosine monophosphate (cAMP) concentration and phosphorylation of cAMP‑response element binding protein was increased following 1,5‑diCQA treatment. These results indicated that 1,5‑diCQA stimulated melanogenesis via the MAPK and cAMP/PKA signaling pathways in B16 cells, which has potential therapeutic implications for vitiligo.

Vernonia cinerea (V cinerea) is a plant distributed in grassy areas in Southeast Asia and has several pharmacological effects, including antidiabetic activity. However, the information available regarding the effect of V cinerea on insulin resistance in high-fat diet (HFD)–induced obese mice is not yet determined. We hypothesized that V cinerea water extract (VC) improves insulin sensitivity in HFD-induced obese mice by modulating both phosphatidylinositol-3-kinase (PI3K) and adenosine monophosphate–activated protein kinase (AMPK) pathways in liver, skeletal muscle, and adipose tissue. Obesity was induced in mice from the Institute for Cancer Research by feeding an HFD 188.28 kJ (45 kcal % lard fat) for 12 weeks. During the last 6 weeks of the HFD, obese mice were treated with VC (250 and 500 mg/kg). We found that VC at both doses significantly reduced the hyperglycemia, hyperinsulinemia, hyperleptinemia, and hyperlipidemia. Obese mice treated with VC could increase serum adiponectin but reduce the proinflammatory cytokines, tumor necrosis factor–α, and monocyte chemoattractant protein–1. The extracts decreased triglyceride storage in liver and skeletal muscle of obese mice. The average size of fat cells was smaller in VC-treated groups than that of the HFD group. The protein expressions of PI3K and AMPK pathways in liver, skeletal muscle, and adipose tissue were upregulated (increased phosphorylation of PI3K, protein kinase B, AMPK, and acetyl-CoA carboxylase) by VC treatment. Furthermore, the glucose transporter 4 was increased in muscle and adipose tissue in obese mice treated with VC. These data indicate that VC treatment stimulates phosphorylation of PI3K and AMPK pathways in liver, muscle, and adipose tissue. Stimulating these pathways may improve impaired glucose and lipid homeostasis in an HFD-induced obesity mouse model. Based on these findings, it appears that VC has potential as a functional food or therapeutic agent in management of insulin resistance related diseases, such as type 2 diabetes mellitus.

Phytochemical investigation of ethanol extracts from two Taiwanese collections of Vernonia cinerea resulted in the isolation of eighteen hirsutinolide-type sesquiterpenoids, including seven new ones designated as vernolides E – K (1–7). All structures were determined by a combination of detailed spectroscopic analyses (NMR and MS) and comparison with reported data. In an in vitro anti-inflammatory assay, compounds 3, 7, 9, 11, and 14 exhibited strong inhibitory activities toward NO production by LPS-induced RAW264.7 macrophages, with IC50 values of 1.18, 0.85, 0.66, 0.71 and 0.45 µM, respectively, without affecting cellular viability at 40 µM. Preliminary structure-activity relationships indicate that the ester groups at C-8 and C-13 may enhance inhibition of NO production.

Background Obesity is a growing public health problem arising from energy imbalance. The effect of 10% dietary incorporation of Vernonia amygdalina (VA) leaves into high-fat diets on some biological markers of adiposity and dyslipidaemia was investigated. Methods Experimental diets consisted of the following n CD (control diet); HFD (high-fat diet); and HFD- VA (HFD containing 10% Vernonia amygdalina leaves) supplementation. Fifteen male Wistar rats were randomly divided into three groups of five animals each. After twelve weeks of feeding, serum lipid profile, blood glucose concentrations, body weight, adiposity index, feed intake, fecal loss and relative organ weight were investigated. Results Vernonia amygdalina (VA) inhibited HFD-induced weight gain and adiposity in rats. HFD-induced obese rats showed a significant increase in the levels of serum TG and TC compared to rats on a normal diet. However, the levels of serum TG, TC, LDL-C in HFDVA rats reduced significantly relative to the levels in HFD rats. Our results indicate that HFDVA reversed fatty infiltration leading to decreased body weight and fat tissue mass in the rats. Conclusions These results suggested that incorporation of Vernonia amygdalina into high-fat diets may have therapeutic potentials for obesity and related metabolic disorders. Further studies to explore its possibility as an alternative pharmacologic agent to treat obesity are warranted.

Background Vitiligo is a long-term skin disease characterized by the loss of pigment in the skin. The current therapeutic approaches are limited. Although the anti-vitiligo mechanisms of Vernonia anthelmintica (L.) remain ambiguous, the herb has been broadly used in Uyghur hospitals to treat vitiligo. The overall objective of the present study aims to identify the potential lead compounds from Vernonia anthelmintica (L.) in the treatment of vitiligo via an oral route as well as the melanogenic mechanisms in the systematic approaches in silico of admetSAR and substructure-drug-target network-based inference (SDTNBI). Results The results showed that the top 5 active compounds with a relatively higher bioavailability that interacted with 23 therapeutic targets were identified in Vernonia anthelmintica (L.) using admetSAR and SDTNBI methods. Among these compounds, Isorhamnetin and Kaempferide, which are methyl-flavonoids, performed 1st and 2nd. Isorhamnetin and Kaempferide significantly increased the expression of melanin-biosynthetic genes (MC1R, MITF, TYR, TYRP1 and DCT) and the tyrosinase activity in B16F10 cells. Isorhamnetin and Kaempferide significantly increased the mRNA-expression of melanin-biosynthetic genes (MC1R, MITF, TYR, TYRP1 and DCT), the protein level of MITF and the tyrosinase activity. Based on the SDTNBI method and experimental verification, Isorhamnetin and Kaempferide effectively increased melanogenesis by targeting the MC1R-MITF signaling pathway, MAPK signaling pathway, PPAR signaling pathway (PPARA, PPARD, PPARG), arachidonic acid metabolism pathway (ALOX12, ALOX15, CBR1) and serotonergic synapses (ALOX12, ALOX15) in the treatment of vitiligo from a network perspective. Conclusion We identified the melanogenic activity of the methyl-flavonoids Isorhamnetin and Kaempferide, which were successfully predicted in a network pharmacological analysis of Vernonia anthelmintica (L.) by admetSAR and SDTNBI methods. Electronic supplementary material The online version of this article (10.1186/s12918-017-0486-1) contains supplementary material, which is available to authorized users.

Objective Diabetes mellitus (DM) is known to be associated with increase of oxidative stress products. The direction of effect of any treatment on these products could therefore be a reliable measure of its efficacy on DM. So the aim of this study was to investigate the activity of insulin, Ocimum gratissimum L. (OG) and Vernonia amygdalina L. (VA) on oxidative stress products. Methods Thirty-six female Wistar rats weighing 150–200 g were randomly divided into six groups of six rats each. Thirty rats were induced for type 1 DM (DM1) with a single intraperitoneal administration of 65 mg/kg body weight of streptozotocin. Group 1 was normal control and was administered distilled water while Group 2 served as DM1 control group; Groups 3, 4, 5 and 6 were diabetic rats treated with 208 mg/kg OG (DM1 + OG), 52 mg/kg VA (DM1 + VA), 208 mg/kg OG + 52 mg/kg VA (DM1+OG +VA) and 0.16 IU insulin (DM1 + insulin) respectively. Determination of methemoglobin and sulfhemoglobin was achieved by the absorption spectrum principle. Red blood cell (RBC) catalase was assayed by continuous spectrophotometric method. Results The RBC catalase concentration was significantly decreased in the DM1 and DM1+VA groups when compared with the normal control. DM1 + OG significantly increased RBC-catalase when compared to DM1. The methemoglobin concentration was significantly reduced in the DM1, DM1 + VA, DM1 + OG + VA and DM1 + insulin groups when compared to the normal control group. The sulfhemoglobin concentration was significantly increased in the diabetic control and the diabetic treated groups when compared to the normal control. DM1 + OG reduced the sulfhemoglobin concentration when compared to DM1. The blood glucose concentration of all the diabetic groups was significantly raised compared to normal control. OG, VA and insulin significantly reduced the blood glucose concentration with the efficacy of OG and VA higher than insulin. Conclusion Adverse alteration of oxidative indices were observed in type 1 DM model. Treatment with OG and insulin showed potent antioxidant activity, while the hypoglycemic efficacy of OG and VA were higher than insulin.

Species of the Vernonia genius are widely distributed across the world. In traditional communities, they are commonly used in popular medicine for the treatment of inflammatory diseases. The objective of the present study was to evaluate the anti-inflammatory activity of Vernonia polysphaera Baker hydroalcoholic extract. A λ-carrageenan-induced paw edema and peritonitis model was established in BALB/c mice. The in vitro activity of the extract was measured on LPS-stimulated RAW 264.7 cells. There was no toxic effect on mice or on the cells treated with the extract. Animals treated with V. polysphaera extract demonstrated inhibition of paw edema in comparison with the untreated animals at all the analyzed doses. In peritonitis, treatment with the extract at a dose of 500 mg/kg resulted in a lower total leukocyte count in the peritoneal fluid and blood and lower levels of IL-1β, IL-6, TNF-α and PGE-2 than the control group. Cells treated with 50 and 100 μg/mL of the extract exhibited lower levels of nitrite and pro-inflammatory cytokine production and lower COX-2, NF-κB expression. The V. polysphaera extract demonstrated an anti-inflammatory effect, interfering with cell migration, reducing pro-inflammatory cytokine levels and COX-2 expression and consequent interference with PGE-2, as well as inhibiting NF-κB transcription.

Twelve sesquiterpene lactones were isolated from the whole plants of

Honey is a nutritive fluid product of bees with an array of pharmacological/medicinal effects. As a natural product from honeybees, honey is regarded to be safe and free from any contaminants. Cassava tuber (Manihot esculenta)-based meal, Vernonia amygdalina (bitter leaf soup), and honey are common local cuisine in Nigeria. This is a human health risk assessment of heavy metals associated with the consumption of honey (Apis mellifera scutellata), cassava (Manihot esculenta), and bitter leaf (Vernonia amygdalina) in Enugu State, Nigeria. Concentrations of lead (Pb), Cd, As, Cu, Ni, Mn, Fe, Cr, and Fe in honey, soil, Manihot esculenta, and Vernonia amygdalina were determined using an atomic absorption spectrophotometer (AAS). The principal component analysis (PCA) was performed as a factor reduction technique among 12 factors (3 locations against 4 sources of heavy metals). The mean concentration of metals in honey, soil, Manihot esculenta, and Vernonia amygdalina ranged from 0.001 to 4.28 mg kg-1, from 0.0026 to 170.52 mg kg-1, from 0.012 to 80.63 mg kg-1, and from 0.0016 to 126.48 mg kg-1, respectively. Pb showed the highest carcinogenic risk with values of 3.18E-04-1.43E-01 in Vernonia amygdalina and 1.69E-04-3.47E-04 in Manihot esculenta for adults and children, respectively. In honey, Cd showed the highest carcinogenic risk with values of 1.26E-02-1.07E-01. About 51.5% of total cancer risk (TCR) was below 1E-04. Consumption of honey, Vernonia amygdalina, and Manihot esculenta in some urban parts of Enugu may pose some adverse health effects.

To investigate a possible methodology of exploiting herbal medicine and design polytherapy for the treatment of skin depigmentation disorder, we have made use of Vernonia anthelmintica (L.) Willd., a traditional Chinese herbal medicine that has been proven to be effective in treating vitiligo. Here, we report that the extract of Vernonia anthelmintica (L.) Willd. effectively enhances melanogenesis responses in B16F10. In its compound library, we found three ingredients (butin, caffeic acid and luteolin) also have the activity of promoting melanogenesis in vivo and in vitro. They can reduce the accumulation of ROS induced by hydrogen peroxide and inflammatory response induced by sublethal concentrations of copper sulfate in wild type and green fluorescent protein (GFP)-labeled leukocytes zebrafish larvae. The overall objective of the present study aims to identify which compatibility proportions of the medicines may be more effective in promoting pigmentation. We utilized the D-optimal response surface methodology to optimize the ratio among three molecules. Combining three indicators of promoting melanogenesis, anti-inflammatory and antioxidant capacities, we get the best effect of butin, caffeic acid and luteolin at the ratio (butin:caffeic acid:luteolin = 7.38:28.30:64.32) on zebrafish. Moreover, the effect of melanin content recovery in the best combination is stronger than that of the monomer, which suggests that the three compounds have a synergistic effect on inducing melanogenesis. After simply verifying the result, we performed in situ hybridization on whole-mount zebrafish embryos to further explore the effects of multi-drugs combination on the proliferation and differentiation of melanocytes and the expression of genes (tyr, mitfa, dct, kit) related to melanin synthesis. In conclusion, the above three compatible compounds can significantly enhance melanogenesis and improve depigmentation in vivo.

The present study investigated the effects of Vernonia cinerea (VC) on the reproductive function in streptozotocin (STZ)-induced diabetic male rats. Six-week-old male Sprague-Dawley rats were randomly divided into four groups: group 1, normal control rats; group 2, diabetic untreated rats; group 3, diabetic rats treated with VC (10 mg/kg); and group 4, diabetic rats treated with VC (40 mg/kg). Diabetes mellitus (DM) was induced by intraperitoneal injection of STZ (60 mg/kg). All animals were treated for 30 consecutive days. Body weight, blood glucose, food intake, epididymal sperm parameters, testicular microstructure and serum testosterone levels were evaluated. VC treatment significantly restored the sperm motility and testosterone concentration, and decreased the testicular histopathological changes in DM rats. Moreover, high-dose VC exhibited an antidibetic activity and significantly improved the sperm count. In conclusion, we found, for the first time, that administration of VC significantly restored the testicular function and testosterone concentration in diabetic male rats.

Vernonia plantaginoides (Less.) Hieron, previously known as Vernonia squarrosa, is a rhizomatous subshrub with purple flowers that is prevalent in the natural grassland of Uruguay, Argentina, and southern Brazil. We report an outbreak of V. plantaginoides ( yuyo moro) intoxication in sheep in Treinta y Tres Department, northeastern Uruguay. A total of 54 of 463 (12%) recently weaned lambs died 2–7 days after entering a natural pasture that had been invaded by sprouting V. plantaginoides. The first cases were found dead. Affected lambs showed marked jaundice, edema of the face, ears, and eyelids, and severe photodermatitis. At the autopsies of 3 lambs, the carcass was yellow, the liver was enlarged with a marked acinar pattern (“nutmeg liver”), and hemorrhages were observed on serous membranes. Microscopic lesions were characterized by diffuse periacinar hepatocellular necrosis and cholemic nephrosis. Three female lambs were experimentally dosed with the aerial parts of V. plantaginoides collected immediately after the outbreak. The lamb that was dosed once with 40 g/kg body weight died after 36 h with severe hepatic necrosis. The lamb dosed with 20 g/kg daily for 4 days showed clinical signs and microscopic lesions in the liver with multiple apoptotic hepatocytes in the periacinar zone. The third lamb, dosed with 30, 17, and 15 g/kg daily over 3 days, respectively, showed transient clinical signs and a rise in liver enzymes, but recovered, and no lesions were found postmortem. These results demonstrate that V. plantaginoides was responsible for severe field outbreaks of poisoning in sheep in Uruguay.

Metals reduction into submicro/nano size through bhasma preparations for therapeutic use is well established in ancient traditional system of Indian medicines i.e. Ayurveda. Recently, nanotechnology has drawn the attention of researchers to develeope various size and shape nanoparicles / composite for number of applications.In this article, we report the enrichment of lactone enriched fraction (LEF) by liquid-liquid portioning of Vernonia cinerea metabolic extract and sysnthesis of mediated nano-gold composite (LEF-AuNPs) in single step process. The morphological characteristic based on transmission electron microscope (TEM) image analysis showed that LEF-AuNPs were predominantly nanopolygons and nanobots in shapes ranging from 50-200 nm in size. Abundance of phytochemicals in both LEF and LEF-AuNPs was dissimilar. In LEF, montanol- a diterpenoid, while in LEF-AuNPs, neophytadiene- a phytanes was the major compound. HPLC profile of relatively polar compounds also varied drastically. In-vitro biocompatibility, cytotoxicity [MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) based assay] and storage stabilitiy of LEF-AuNPs were evaluated. The moderate ability of LEF-AuNPs to restrict parasitaemia, extended mean survival time of mice infected with Plasmodium berghei and lack of any evident toxicity provides new opportunities for the safe delivery and applications of such nanocomposites in malaria therapy.

Ethnopharmacological relevance Vernonia patula (Dryand.) Merr. and Leucas chinensis (Retz.) R. Brown have anti-inflammatory properties and are popularly used as complementary and alternative medicine in Asia. Aim of the study To investigate the underlying molecular mechanism and active chemicals in the ethanol extracts of V. patula (VP) and L. chinensis (LC). Materials and methods The inhibitory activities of VP and LC on lipopolysaccharide (LPS)-stimulated nitric oxide (NO) and interleukin-6 (IL-6) production were investigated in RAW264.7 macrophages and BV2 microglia. Downregulation of pro-inflammatory genes and upregulation of Nrf2 (NF-E2 p45-related factor 2)-ARE (antioxidant response element) pathway were investigated using RT-Q-PCR and Western blotting. Direct antioxidant capacities were measured using free radical scavenging and Folin-Ciocalteu assays. The flavonoids and triterpenes in VP and LC were identified by HPLC-ESI-MS. Results VP and LC inhibited NO and IL-6 production and suppressed iNOS, IL-6, IL-1β and CCL2 gene expression. VP and LC were potent direct antioxidants and effective indirect antioxidants assayed by Nrf2 activation and induction of heme oxygenase (HO)-1, glutamate-cysteine ligase modifier subunit (GCLM) and NAD(P)H quinone oxidoreductase 1 (NQO1). Three flavonoids including apigenin (1), luteolin (2) and chryseriol (3), and one triterpene betulinic acid (4) were found in VP; while compounds 1–4 and oleanolic acid (5) were in LC. Conclusion Anti-inflammatory and antioxidant activities of VP and LC may be in great part attributed to the identified Nrf2 activating compounds, which induce expression of Phase II enzymes and attenuate the upregulation of pro-inflammatory genes., Graphical abstract Image 1

Ethnopharmacological relevance Sesquiterpene lactones are organic compounds derived mainly from plants that exhibit anti-inflammatory and antitumor activities being one of the key mechanism of action of NF-kB pathway and synthesis of cytokines such as IL-1 and TNF- α. Aim of the study The overall objective of the present study was to evaluate the anti-inflammatory action of a sesquiterpene lactone diacethylpiptocarphol (DPC) from Vernonia scorpioides (Lam.) Pers. and parthenolide (PTH) in Balb-c mice with DSS-induced colitis. Materials and methods The anti-inflammatory effects of Intraperitonial administration of DPC (5 mg/kg/day) were evaluated in Balb/c mice with DSS-induced colitis, and further the body weight measurement, TNF-α and TGF-β level was determined. Results After intraperitoneal treatment for one week, DSS-induced colitis was significantly reduced in mice treated with either of both sesquiterpenes lactones, as witnessed by reduced cellular infiltration, tissue damage, TNF-α production, and enhanced production of TGF-β. Conclusions Sesquiterpene lactone DPC, isolated from Vernonia scorpioides showed anti-inflammatory activity, in this experimental model of colitis the sesquiterpene lactones DPC and PTH exhibit equal anti-inflammatory activity.

Ethnopharmacological relevance Vernonia anthelmintica (L.) Willd. (Asteraceae; Purple Fleabane) has a long history of traditional use for the management of several disorders related to skin, central nervous system, kidney, gynecology, gastrointestinal, metabolism, and general health. The review aims to provide updated systematic information on ethnomedicinal uses, phytochemistry, pharmacological uses, toxicity studies, and patented formulations of V. anthelmintica. This review will not only help to identify the research gaps but also provide information to the scientific community for future research requisites. Material and methods Empirical searches were conducted on the medicinal plant via significant search engines like Google Scholar, Scopus-Elsevier, Medline, SciFinder, Web of Science, Directory of Open Access Journal (DOAJ) from inception until June 2018. Besides, references from local literature, books, and non-English journals were also included. Results Scientific reports revealed that V. anthelmintica is a popular medicinal plant used in local and traditional medicine to manage various disorders. Phytochemical studies have identified 193 chemical constituents amongst which steroids form the most abundant class, followed by terpenes. Crude extracts and isolated compounds exhibited various pharmacological activities such as anti-vitiligo, anti-diabetic, anti-inflammatory, antipsoriatic, neuroprotective, hepatoprotective, analgesic, antipyretic, antioxidant, antiparasitic, antimicrobial, antiproliferative, immunomodulatory and also helped in managing pulmonary fibrosis and promoting the synthesis of estrogen. Approximately 45 chemical constituents were found to be biologically active. There are only three toxicity reports and 37 patents available on V. anthelmintica. Conclusion The review suggests that V. anthelmintica act as a promising source for drug development. The potential uses of V. anthelmintica are owing to the presence of phenolic acids, steroids, fatty acids, and terpenes in its composition. However, further studies are needed to explore the exact mechanism of action, pharmacokinetics, chronic toxicological studies, safe dose consumption, and possible interactions with other herbs.

Vernonia amygdalina (VA) is a medicinal tropical herb for diabetes and malaria and believed to be beneficial for joint pains. The antiosteorthritis effects of VA leaf in cartilage explant assays and on postmenopausal osteoarthritis (OA) rat model were investigated. The VA reduced the proteoglycan and nitric oxide release from the cartilage explants with interleukin 1β (IL-1β) stimulation. For the preclinical investigation, ovariectomized (OVX) female rats were grouped (n = 8) into nontreated OA, OA + diclofenac (5 mg/kg), OA + VA extract (150 and 300 mg/kg), and healthy sham control. Monosodium iodoacetate was injected into the knee joints to accelerate OA development. After 8 weeks, the macroscopic, microscopic, and histological images showed that the OA rats treated with VA 300 mg/kg and diclofenac had significantly reduced cartilage erosions and osteophytes unlike the control OA rats. The extract significantly down-regulated the inflammatory prostaglandin E2, nuclear factor κβ, IL-1β, ADAMTS-5, collagen type 10α1, and caspase3 in the OVX-OA rats. It up-regulated the anti-inflammatory IL-10 and collagen type 2α1 mRNA expressions, besides reducing serum collagenases (MMP-3 and MMP-13) and collagen type II degradation biomarker (CTX-II) levels in these rats. The VA (containing various caffeoyl-quinic acids, flavanone-O-rutinoside, luteolin, apigenin derivative and vernonioside D) suppressed inflammation, pain, collagenases as well as cartilage degradation, and improved cartilage matrix synthesis to prevent OA.

In this study Vernonia amygdalina. Delile stem and leaves were evaluated for anti-cancer and antibacterial actions against selected microorganisms. The crude plant extracts were extracted using methanol and fractionated into ethyl acetate, hexane, aqueous and crude extracts. Cancer inducing agent Carbon tetrachloride (CCl4) was introduced into Wistar mice and screened with crude extracts of Vernonia amygdalina. Delile to evaluate the anti-cancer properties of the extracts. The effect of CCl

This study investigated the inhibitory effects of active component isolated from flavonoid fraction of Vernonia cinerea (FVC), lupeol on selenite induced cataract formation. Previous reports suggest that phytochemicals or natural plant products retard the process of cataractogenesis by scavenging free oxygen radicals. Hence, the present study sought to assess the potential of lupeol on in vivo selenite induced cataract models. Lupeol, a pentacyclic triterpenoid, was isolated from the ethyl acetate fraction of methanolic extract of Vernonia cinerea, follows standard chromatographic techniques. Structural elucidation of the compound was carried out using (1)H NMR, (13)C NMR, Mass spectrometry together with other complementary techniques (UV and IR). From these, the isolated compound was identified as Lupeol (3'-hydroxylup-20(29)-ene). The antioxidant activity was comparatively studied using DPPH radical scavenging and FRAP assay. Lupeol exhibited higher DPPH radical scavenging activity as well as reducing power assay. In this study, cataract was induced by a single subcutaneous injection of sodium selenite (4 μg/g body weight) on rat pups. Lupeol was administered orally from 8th day upto 21st day at a concentration 25 μg/g body weight. Cataract was visualized on 16th day with the help of an ophthalmoscope and later on with the naked eye. On the 30th day, rats were euthanized by sodium pentothal injection, lenses were excised and the biochemical parameters such as activity of superoxide dismutase (SOD), catalase (CAT), Glutathione peroxidase (GPx), Glutathione reductase (GR), Glutathione-S-transferase (GST), Ca(2+) ATPase, glutathione content (GSH), reactive oxygen species (ROS), lipid peroxidation products (malondialdehyde) were estimated and found effective in the treatment of cataract by lupeol.

Ethnopharmacological relevance Vernonia anthelmintica has been utilized conventionally as an ingredient in Ayurveda and traditional Uighur medicine for management of various skin ailments, and scientific data's have substantiated its use in treating vitiligo, dermatosis and leucoderma. The present investigation was focused to evaluate the antipsoriatic activity of V. anthelmintica fruit extracts and fractions. Materials and methods Ointment containing dichloromethane (DCM) and methanol (MeOH) extracts at topical dose of 2.5% and 5% (w/w) was evaluated using mouse tail model of psoriasis. Bioactivity-guided fractionation (F1-F7) of most active extract was carried out and fractions were again subjected to mouse tail model. Further the activity of bioactive fraction was confirmed in HaCaT (human keratinocyte) cell line using MTT (3-(4,5-dimethylthiazol-2-yl)− 2,5-diphenyltetrazolium bromide) assay and its chemical characterization was done via gas chromatography mass spectrometry (GC-MS). Results The dichloromethane extract (5%, w/w) showed statistically significant (* p Conclusion Ameliorative effect of V. anthelmintica in psoriasis might be attributed to the presence of essential fatty acids and thus corroborates its traditional use in the treatment of skin ailments.

In the endeavor to obtain new antitrypanosomal agents, particularly sesquiterpene lactones, from Kenyan plants of the family Asteraceae, Vernonia cinerascens Sch. Bip. was investigated. Bioactivity-guided fractionation and isolation in conjunction with LC/MS-based dereplication has led to the identification of vernodalol (1) and isolation of vernodalin (2), 11β,13-dihydrovernodalin (3), 11β,13-dihydrovernolide (4), vernolide (5), 11β,13-dihydrohydroxyvernolide (6), hydroxyvernolide (7), and a new germacrolide type sesquiterpene lactone vernocinerascolide (8) from the dichloromethane extract of V. cinerascens leaves. Compounds 3-8 were characterized by extensive analysis of their 1D and 2D NMR spectroscopic and HR/MS spectrometric data. All the compounds were evaluated for their in vitro biological activity against bloodstream forms of Trypanosoma brucei rhodesiense and for cytotoxicity against the mammalian cell line L6. Vernodalin (2) was the most active compound with an IC50 value of 0.16 µM and a selectivity index of 35. Its closely related congener 11β,13-dihydrovernodalin (3) registered an IC50 value of 1.1 µM and a selectivity index of 4.2.

Made available in DSpace on 2018-12-11T17:11:03Z (GMT). No. of bitstreams: 0 Previous issue date: 2017-12-17 Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) The composition of the essential oil (EO) from leaves of Vernonia polyanthes and the evaluation of its leishmanicidal potential are reported here for the first time. The oil obtained by hydrodistillation was analysed by combination of GC and GC/MS. Thirty-five compounds were identified, representing 91.8% of the oil composition. The oil consists primarily of monoterpenes (37.1%), sesquiterpenes (26.3%) and oxygenated sesquiterpenes (23.9%), myrcene (34.3%), zerumbone (15.8%), bicyclogermacrene (8.9%), α-humulene (4.8%) and germacrene D (4.3%) being the major constituents. Activity against Leishmania infantum was determined using the tetrazolium dye (MTT) colorimetric method. The oil, as well as zerumbone, one of its major constituents, showed significant leishmanicidal activity, with IC50 values of 19.4 and 9.0 μg/ml, respectively. Cytotoxicity in macrophages cells was evaluated using the MTT colorimetric assay. The EO showed the CC50

The young leaves of Vernonia amygdalina are often utilized as vegetable and for medicinal purpose compared to the old leaves. This study was designed to evaluate and compare the antidiabetic effects between ethanolic leaf extracts of old and young V. amygdalina on streptozotocin (STZ) induced diabetic rat for four weeks. Preliminary screening of both young and old ethanolic extracts revealed the presence of the same phytochemicals except flavonoids which was only present in the old V. amygdalina. Difference in antioxidant power between the young and old leaf extracts was statistically significant (p0.05). Both leaf extracts produced a significant (p0.05) antihyperglycaemic effect. Also results from treated rats revealed increasing effect in some haematological parameters. Similarly, the higher dose (300 mg/kg) of both extracts significantly (p0.05) reduced serum ALT, AST, and ALP levels as compared to the diabetic control rats. Results also showed significant (p0.05) decrease in LDL-C and VLDL-C in the extract-treated rats with a corresponding increase in HDL-C, as compared to the diabetic control rats. Moreover histopathological analysis revealed ameliorative effect of pathological insults induced by the STZ in the pancreas, liver, and spleen, most significantly the regeneration of the beta cells of the islets of Langerhans in treated rats.

Objective This study investigated the acute and subacute toxicity of whole-plant aqueous extract of Vernonia mespilifolia Less. (AEVM) in rats for evaluating its safety profile. Methods AEVM for the acute (2000 and 5000 mg/kg) and subacute (200, 400 and 600 mg/kg) toxicity studies was administered orally to rats according the guidelines 425 and 407 of Organization for Economic Cooperation and Development, respectively. Food and water intake as well as body and organ weight of animals were recorded. Signs of toxicity were assessed, and hematological, biochemical and histopathological analyses were performed. Results In the acute toxicity study, a single dose of the aqueous extract at 2000 or 5000 mg/kg caused no mortality in the animals, suggesting that the median lethal dose is greater than 5000 mg/kg. In the subacute toxicity study, administration of the extract for 28 d, at all doses, caused no significant changes in the body weights or organ weights of rats in the treated groups when compared with the control group. In addition, hematological and biochemical parameters also revealed no toxic effects of the extract on rats. Histological sections of the heart, liver and kidney from test animals showed no signs of degeneration. Conclusion These results showed that AEVM at dosage levels up to 600 mg/kg is nontoxic and could also offer protection on some body tissues. AEVM could, therefore, be considered safe.

Tectona grandis (teak) and Vernonia amygdalina (bitter leaf) are plants used in traditional medicine in West Africa. In this study, we tested ethanolic and hydro-ethanolic extracts of bark and leaves of T. grandis and ethanolic extract of leaves of V. amygdalina for their inhibitory effect on Toxoplasma gondii, a protozoan parasite responsible for toxoplasmosis. Ethanolic extract of V. amygdalina leaves had proportional contents of phenols, tannins, flavonoids, and polysaccharides. This extract presented the highest efficacy against T. gondii, the lowest cytotoxicity to mammalian cells, but moderate anti-oxidant activity compared to other plant extracts. Ethanolic extract of T. grandis bark also had elevated anti-T. gondii activity, low cytotoxicity on mammalian cells, and one of the highest anti-oxidant activities. However, the phytochemical content of this extract was not very different from the hydro-ethanolic extract, which had no anti-T. gondii activity. In addition, ethanolic extract of V. amygdalina leaves, but not of T. grandis bark, significantly increased the production of TNF-α and NO by antigen-presenting cells. Both extracts had the tendency to decrease expression of major histocompatibility complex molecules at the surface of antigen-presenting cells, while they did not modulate the percentage of apoptotic cells. A study of signalling pathways would help to determine the mechanisms of action of these plant extracts.Les extraits de Tectona grandis et de Vernonia amygdalina ont des propriétés anti-Toxoplasma et pro-inflammatoires in vitro.Tectona grandis (teck) et Vernonia amygdalina sont des plantes utilisées dans la médecine traditionnelle en Afrique de l’Ouest. Dans cette étude, l’effet inhibiteur d’extraits éthanoliques et hydro-éthanoliques d’écorce et de feuilles de T. grandis et de l’extrait éthanolique des feuilles de V. amygdalina a été étudié sur Toxoplasma gondii, un parasite protozoaire responsable de la toxoplasmose. L’extrait éthanolique des feuilles de V. amygdalina avait des quantités équivalentes de phénols, tanins, flavonoïdes et polysaccharides. Cet extrait présentait la plus grande efficacité contre T. gondii, la plus faible cytotoxicité vis-à-vis de cellules de mammifères, mais une activité anti-oxydante moyenne comparée aux autres extraits de plantes. L’extrait éthanolique d’écorce de T. grandis avait aussi une activité anti-T. gondii élevée, une faible cytotoxicité vis-à-vis des cellules de mammifères et l’une des activités anti-oxydantes les plus élevées. Cependant, le contenu phytochimique de cet extrait n’était pas très différent de l’extrait hydro-éthanolique qui n’avait pas d’activité anti-T. gondii. De plus, l’extrait éthanolique des feuilles de V. amygdalina, mais pas de l’écorce de T. grandis, augmentait significativement la production de TNF-α et de NO par les cellules présentatrices d’antigènes. Les deux extraits avaient tendance à diminuer l’expression des molécules du complexe majeur d’histocompatibilité à la surface des cellules présentatrices d’antigènes alors qu’ils ne modulaient pas le pourcentage de cellules apoptotiques. L’étude des voies de signalisation permettrait de comprendre les mécanismes d’action de ces extraits de plantes.

Context: Vernonia amygdalina Del. (VA) (Asteraceae) is commonly used to treat hypertension in Malaysia. Objective: This study investigates the vasorelaxant mechanism of VA ethanol extract (VAE) and analyzes its tri-step FTIR spectroscopy fingerprint. Materials and methods: Dried VA leaves were extracted with ethanol through maceration and concentrated using rotary evaporator before freeze-dried. The vasorelaxant activity and the underlying mechanisms of VAE using the cumulative concentration (0.01–2.55 mg/mL at 20-min intervals) were evaluated on aortic rings isolated from Sprague Dawley rats in the presence of antagonists. Results: The tri-step FTIR spectroscopy showed that VAE contains alkaloids, flavonoids, and saponins. VAE caused the relaxation of pre-contracted aortic rings in the presence and absence of endothelium with EC50 of 0.057 ± 0.006 and 0.430 ± 0.196 mg/mL, respectively. In the presence of Nω-nitro-l-arginine methyl ester (EC50 0.971 ± 0.459 mg/mL), methylene blue (EC50 1.203 ± 0.426 mg/mL), indomethacin (EC50 2.128 ± 1.218 mg/mL), atropine (EC50 0.470 ± 0.325 mg/mL), and propranolol (EC50 0.314 ± 0.032 mg/mL), relaxation stimulated by VAE was significantly reduced. VAE acted on potassium channels, with its vasorelaxation effects significantly reduced by tetraethylammonium, 4-aminopyridine, barium chloride, and glibenclamide (EC50 0.548 ± 0.184, 0.158 ± 0.012, 0.847 ± 0.342, and 0.304 ± 0.075 mg/mL, respectively). VAE was also found to be active in reducing Ca2+ released from the sarcoplasmic reticulum and blocking calcium channels. Conclusions: The vasorelaxation effect of VAE involves upregulation of NO/cGMP and PGI2 signalling pathways, and modulation of calcium/potassium channels, and muscarinic and β2-adrenergic receptor levels.

Seeds of Vernonia anthelmintica in the form of Ethanol seed extract of Vernonia anthelmintica (EEVA), Hexane extract of Vernonia anthelmintica (HEVA) and water decoction of Vernonia anthelmintica (WDVA) were evaluated for their in-vivo anti-Inflammatory potential in carrageenan induced rat paw model. The results were compared to anti-inflammatory activity of standard drug (ibuprofen) and untreated groups. In-vitro evaluation of antioxidant potential of EEVA and HEVA were also conducted by "DPPH scavenging assay". The results of present study depicts that HEVA and EEVA in higher dose possess a strong anti-inflammatory potential as compared to standard anti-inflammatory drugs, whereas WDVA showed milder anti-inflammatory potential. DPPH assay has revealed strong anti-oxidant potential of EEVC with the percentage Radical Scavenging activity (%RSA) of 89.709 at concentrations of 500 ul as compared to standard drugs gallic acid (23.436±0.43) and acetyl salicylic acid (111.44±0.7) at concentrations of 95.95 μM. The other extract HEVC has shown to have insignificant %RSA at the concentration of 500μl. Hence the present study revealed that selected extracts of Vernonia anthelmintica exhibited significant in-vitro antioxidant and in-vivo anti-inflammatory potential.

Background: Vernonia amygdalina, commonly called bitter-leaf, is widely consumed in many parts of Africa, and Nigeria, in particular. The leaf extract has been reported to have antimicrobial, anti-plasmodial, anti-helminthic, as well as prebiotic properties, but its immuno-modulatory effects have not been well-studied, neither have the prebiotics been identified. This study evaluated the immuno-modulatory properties of the aqueous leaf extract and identified the prebiotic components. Methods: The immuno-modulatory potential was evaluated by monitoring the effects of oral administration of the extract on immunological, haematological and lipid profiles of Rattus norvegicus, while the prebiotic components were identified by thin layer chromatography (TLC), following liquid-liquid fractionation of the extract. Results: Consumption of the extract caused significant increases in CD4+-, white blood cell-, total lymphocyte- and high density lipid (HDL) counts; decreases in low density lipid (LDL) and triglycerides and no significant effect on haemoglobin (Hb) and packed cell volume (PCV) in the blood of test animals. The water-soluble fraction of the extract contained most of the phyto-constituents of the extract and Thin Layer Chromatographic analysis of the fraction revealed the presence of fructo-oligosaccharide and galacto-oligosaccharide prebiotics. Conclusion: The results from this study have shown that the aqueous leaf extract of V. amygdalina has positive immune-modulatory and haematologic effects and contains some important prebiotic compounds.

Despite the widespread use of Vernonia anthelmintica seeds in traditional medicine, the need to establish the safety of the Vernonia anthelmintica is required to ascertain the safe use of this herbal medicine. The aim of the present study is to establish the acute toxicity profile of different extracts of Vernonia anthelmintica. Hexane and ethanol extract of Vernonia Anthelmintica has been studied for its brine shrimp lethality potential. Water decoction (WDVA), Hexane (HEVA) and Ethanol (EEVA) extracts of Vernonia anthelmintica has also been evaluated for their in-vivo acute oral toxicity in mice by Lorke's method. Phytochemistry of all three extracts was also evaluated for the presence of their secondary metabolites. All three extracts showed the presence of flavonoids and terpenoids, while alkaloids, tannins and fixed oils were present in HEVA and EEVA. Furthermore EEVA also showed presence of carbohydrates and HEVA also showed the presence of cardiac glycosides. Ethanol and hexane extracts of Vernonia anthelmintica showed a positive cytotoxicity in brine shrimp lethality test at 24 hours with LC50 104.16 (224.0-48.05)μg/ml and 216.11μg/ml (378.2-128.7) respectively as compared to standard drug etoposide LC50 7.46μg/ml. The oral LD50 for EEVA, HEVA and WDVA in mice by Lorke's method was greater than 5000mg/kg. The result of brine shrimp lethality test clearly exhibited the presence of bioactive compounds with cytotoxic potential; however seems to be safe for oral use since LD50 was higher than 5000mg/kg and thus safety of acute dosing in vivo practices is justified.