Isolation, characterization and anti-inflammatory activity of compounds from the Vernonia amygdalina.

The need to explore the abundance of natural products cannot be overemphasized particularly in the management of various disease conditions. In traditional medical practice, Vernonia amygdalina has been widely adopted in the management of various inflammatory disorders. The objective of this investigation was to isolate the bioactive principles from the stem-bark and root of V. amygdalina and assess the anti-inflammatory (in vitro) activity of both the crude extracts and the isolated compounds. Following extraction with the methanol, the extract was subjected to gravity column chromatography and the resultant fractions was further purified to obtained pure compounds. The structural elucidation of the compounds were based on data obtained from 1H to 13C nuclear magnetic resonance (NMR) spectroscopies as well as fourier transform infrared (FT-IR). Using diclofenac as a control drug, the albumin denaturation assay was used to determine the in vitro anti-inflammatory activity of the extracts and isolates. Three distinct compounds characterized are vernoamyoside D, luteolin-7-α-o-glucuronide, and vernotolaside, a new glycoside. When compared to diclofenac, which has an IC50 of 167.8 µg/mL, luteolin-7-α-o-glucuronide, vernoamyoside D, and vernotolaside all showed significant inhibitions with respective IC50 values 549.8, 379.5, and 201.7 µg/mL. Vernotolaside is reported for the first time from the root. The assertion that the plant is used in traditional medicine for the management of inflammatory disorder is somewhat validated by the confirmation of the existence of the compounds with the biochemical actions. Further validation of the isolated compounds would be required in animal studies.

Telfairia occidentalis mitigates dextran sodium sulfate-induced ulcerative colitis in rats via suppression of oxidative stress, lipid peroxidation, and inflammation.

Ulcerative colitis (UC), a subcategory of inflammatory bowel diseases, affects more than 2 million people globally. This study sought to investigate the curative ability of aqueous leaf extract of Telfairia occidentalis (ATO) on dextran sodium sulfate (DSS)-mediated colitis in rats. UC was induced by 5% of DSS in drinking water, and the curative ability of ATO was assessed at 200 mg/kg by oral administration for 10 days. The effect of ATO was deduced on anti-inflammatory, preclinical features [disease activity index (DAI)], redox assays, and alterations both microscopic and macroscopic of the colonic mucosa. DSS mediated inflammation in colons of rats with a significant increase in nitric oxide, myeloperoxidase, IL-1ß, IL-6, and TNF-α levels compared with a control group. Lipid peroxidation was also induced following exposure of rats to DSS. There is a marked decrease in antioxidant enzymes activities in DSS group. However, treatment with ATO markedly inhibited the colonic inflammation by reversing the elevated levels of inflammatory markers. Furthermore, ATO suppressed the lipid peroxidation chain reaction by reducing the level of malondialdehyde and hydrogen peroxide. ATO attenuates DSS-induced oxidative stress by increase the level of GSH and enhancing the activities of the cytoprotective enzymes (catalase, glutathione-S-transferase, and superoxide dismutase). Taken together, ATO reduced DAI score, inhibited inflammation, suppressed lipid peroxidation, attenuated oxidative stress, and enhanced the antioxidant enzymes activities. These therapeutic effects of ATO might be due to its phytochemicals as showed in gas chromatography-mass spectroscopy results. The findings of this study indicate that aqueous leaf extract of T. occidentalis has could be a drug candidate for the treatment of UC. PRACTICAL APPLICATIONS: The study focused on the curative ability of aqueous leaf extract of Telfairia occidentalis on dextran sodium sulfate (DSS) mediated colitis in rats. The extract elicits beneficial effects against colitis via its ability to reduce mucosal inflammation, suppress lipid peroxidation, attenuate oxidative stress, enhance the antioxidant enzymes activities, and reduce both infiltration of inflammatory cells and mucosal damage in colon. This study provides scientific evidence to the therapeutic ability of aqueous leaf extract of T. occidentalis in the treatment of DSS-induced ulcerative colitis and could be a drug candidate for the treatment of inflammatory bowel diseases in humans.

A systematic review on COVID-19 pandemic with special emphasis on curative potentials of Nigeria based medicinal plants.

Despite the frightening mortality rate associated with COVID-19, there is no known approved drug to effectively combat the pandemic. COVID-19 clinical manifestations include fever, fatigue, cough, shortness of breath, and other complications. At present, there is no known effective treatment or vaccine that can mitigate/inhibit SARS-CoV-2. Available clinical intervention for COVID-19 is only palliative and limited to support. Thus, there is an exigent need for effective and non-invasive treatment. This article evaluates the possible mechanism of actions of SARS-CoV-2 and present Nigeria based medicinal plants which have pharmacological and biological activities that can mitigate the hallmarks of the pathogenesis of COVID-19. SARS-CoV-2 mode of actions includes hyper-inflammation characterized by a severe and fatal hyper-cytokinaemia with multi-organ failure; immunosuppression; reduction of angiotensin-converting enzyme 2 (ACE2) to enhance pulmonary vascular permeability causing damage to the alveoli; and further activated by open reading frame (ORF)3a, ORF3b, and ORF7a via c-Jun N- terminal kinase (JNK) pathway which induces lung damage. These mechanisms of action of SARS-CoV-2 can be mitigated by a combination therapy of medicinal herbs based on their pharmacological activities. Since the clinical manifestations of COVID-19 are multifactorial with co-morbidities, we strongly recommend the use of combined therapy such that two or more herbs with specific therapeutic actions are administered to combat the mediators of the disease.

Hibiscus sabdariffa calyx palliates insulin resistance, hyperglycemia, dyslipidemia and oxidative rout in fructose-induced metabolic syndrome rats.

BACKGROUND: The effect of Hibiscus sabdariffa calyx extract was evaluated in high-fructose-induced metabolic syndrome rats. Insulin resistance, hyperglycemia, dyslipidemia and oxidative rout were induced in rats using high-fructose diet. High-fructose diet-fed rats were administered 100 and 200 mg kg(-1) body weight of H. sabdariffa extract for 3 weeks, starting from week 7 of high-fructose diet treatment. RESULTS: High-fructose diet significantly (P < 0.05) increased the serum levels of blood glucose, insulin, total cholesterol (TC), triacylglycerol (TAG), low-density lipoprotein cholesterol (LDLc) and very-low-density lipoprotein cholesterol (VLDLc), with a concomitant reduction in high-density lipoprotein cholesterol (HDLc). These alterations were significantly ameliorated by the extract. High-fructose diet-mediated decreases in the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GSH-red) and glucose 6-phosphate dehydrogenase (Glc 6-PD) were significantly (P < 0.05) attenuated. Altered levels of reduced glutathione (GSH) and glutathione disulfide (GSSG) were significantly (P < 0.05) restored to normal. High-fructose diet-mediated increases in the concentrations of malondialdehyde, conjugated dienes, lipid hydroperoxides, protein carbonyl and percentage fragmented DNA were significantly (P < 0.05) lowered by the Hibiscus extract. CONCLUSION: Overall, aqueous extract of H. sabdariffa palliates insulin resistance, hyperglycemia, dyslipidemia and oxidative rout in high-fructose-induced metabolic syndrome rats.

Antidiarrhoeal Activity of Musa paradisiaca Sap in Wistar Rats.

The folkloric claim of Musa paradisiaca sap in the management of diarrhoea is yet to be substantiated or refuted with scientific data. Therefore, the aim of the current study was to screen the sap of M. paradisiaca for both its secondary metabolites and antidiarrhoeal activity at 0.25, 0.50, and 1.00 mL in rats. Secondary metabolites were screened using standard methods while the antidiarrhoeal activity was done by adopting the castor oil-induced diarrhoeal, castor oil-induced enteropooling, and gastrointestinal motility models. The sap contained flavonoids, phenolics, saponins, alkaloids, tannins, and steroids while cardiac glycosides, anthraquinones, triterpenes, cardenolides, and dienolides were not detected. In the castor oil-induced diarrhoeal model, the sap significantly (P < 0.05) prolonged the onset time of diarrhoea, decreased the number, fresh weight, and water content of feaces, and increased the inhibition of defecations. Na(+)-K(+)-ATPase activity in the small intestine increased significantly whereas nitric oxide content decreased. The decreases in the masses and volumes of intestinal fluid by the sap were accompanied by increase in inhibition of intestinal fluid content in the enteropooling model. The sap decreased the charcoal meal transit in the gastrointestinal motility model. In all the models, the 1.00 mL of the sap produced changes that compared well with the reference drugs. Overall, the antidiarrhoeal activity of Musa paradisiaca sap attributed to the presence of alkaloids, phenolics, flavonoids, and/or saponins which may involve, among others, enhancing fluid and electrolyte absorption through de novo synthesis of the sodium potassium ATPase and/or reduced nitric oxide levels.

Lophirones B and C extenuate AFB1-mediated oxidative onslaught on cellular proteins, lipids, and DNA through Nrf-2 expression.

The capability of lophirones B and C to extenuate aflatoxin B1 (AFB1)-mediated onslaught on cellular proteins, lipids, and DNA was investigated for 6 weeks. Lophirones B and C significantly (P < 0.05) increase the expression and specific activity of cytoprotective enzymes (glutathione-S-trans-ferase, nioctinamide adenine dicludeotide:quinone oxidoreductase-1, epoxide hydrolase, and uridyl glucuronosyl transferase). There was significant (P < 0.05) reduction in the level of antioxidant system in AFB1-induced hepatocarcinogenesis. Furthermore, lophirones B and C significantly (P < 0.05) attenuated AFB1-mediated decrease in the specific activities of antioxidant enzymes. Oxidative stress biomarkers, malondialdehyde, lipid hydroperoxides, conjugated dienes, protein carbonyl, and fragmented DNA were significantly (P < 0.05) elevated in AFB1-treated rats. Although lophirones B and C did not significantly (P < 0.05) alter these biomarkers, an AFB1-mediated increase in these biomarkers was significantly attenuated. Results obtained showed that lophirones B and C extenuate AFB1-mediated onslaught on cellular proteins, lipids, and DNA by enhancing nuclear erythroid-related factor-2 expression.

Selected spices and their combination modulate hypercholesterolemia-induced oxidative stress in experimental rats.

BACKGROUND: Effect of aqueous extracts of Allium sativum (garlic), Zingiber officinale (ginger), Capsicum fructensces (cayenne pepper) and their mixture on oxidative stress in rats fed high Cholesterol/high fat diet was investigated. Rats were randomly distributed into six groups (n=6) and given different dietary/spice treatments. Group 1 standard rat chow (control), group 2, hypercholesterolemic diet plus water, and groups 3, 4, 5, 6, hypercholesterolemic diet with 0.5 ml 200 mg · kg-1 aqueous extracts of garlic, ginger, cayenne pepper or their mixture respectively daily for 4 weeks. RESULTS: Pronounced oxidative stress in the hypercholesterolemic rats evidenced by significant (p<0.05) increase in MDA levels, and suppression of the antioxidant enzymes system in rat's liver, kidney, heart and brain tissues was observed. Extracts of spices singly or combined administered at 200 mg.kg-1 body weight significantly (p<0.05) reduced MDA levels and restored activities of antioxidant enzymes. CONCLUSIONS: It is concluded that consumption of garlic, ginger, pepper, or their mixture may help to modulate oxidative stress caused by hypercholesterolemia in rats.

Cytotoxic, antimutagenic, and antioxidant activities of methanolic extract and chalcone dimers (lophirones B and C) derived from Lophira alata (Van Tiegh. Ex Keay) stem bark.

The cytotoxic, antimutagenic, and antioxidant activities of methanolic extract and lophirones B and C derived from Lophira alata stem bark were evaluated. The extract and lophirones B and C significantly (P < .05) reduced the viability of Ehrlich ascites carcinoma cells. There were concentration-dependent reduction in 4-nitro-o-aminophenylenediamine and benzo[a]pyrene-induced frame shift mutation as well as aflatoxin B1-induced base pair substitution by the extract and lophirones B and C. The extract and lophirones B and C concentration dependently scavenged DPPH radical, superoxide anion radical, hydrogen peroxide, hydroxyl radicals, and reduced ferric ion in the potassium hexacyanoferrate III reducing system. The results obtained from this study revealed that methanolic extract and lophirones B and C derived from Lophira alata stem bark posses anticancer, antimutagenic, and antioxidant activities, with lophirone C producing the best anticancer, antimutagenic, and antioxidant activities. The acclaimed anticancer activity of Lophira alata may be attributed to lophirones B and C.

Electrophilic and reactive oxygen species detoxification potentials of chalcone dimers is mediated by redox transcription factor Nrf-2.

Nuclear erythroid related factor-2 (Nrf2), a redox-transcription factor, plays a critical role in the detoxification of electrophilic and reactive oxygen species that halt various biochemical and molecular processes. This makes it a candidate for regulation by polyphenols. This study investigates the capability of chalcone dimers (lophirones B and C) to induce expressions and activities of cytoprotective enzymes. Chalcone dimers administration to rats not only induced the Nrf2, but also suppressed cytoplasmic Kelch-like ECH-associated protein 1 (Keap1) expressions. In addition, the chalcone dimers significantly (p < 0.05) increased the expressions and activities of nicotinamide adenine dinucleotide and reduced quinone oxidoreductase-1, glutathione-S-transferase, epoxide hydrolase and uridyl glucuronosyl transferase in rat liver. Also, activities of superoxide dismutase, catalase, glutathione peroxidase, and glutathione reductase in rat liver increased significantly (p < 0.05). Overall, lophirones B and C increased the expressions and activities of cytoprotective proteins in rat liver possibly through the reduction of cytoplasmic Keap1 expression, leading to the nuclear translocation of Nrf2.

Selected spices and their combination modulate hypercholesterolemia-induced oxidative stress in experimental rats

BACKGROUND: Effect of aqueous extracts of Allium sativum (garlic), Zingiber officinale (ginger), Capsicum fructensces (cayenne pepper) and their mixture on oxidative stress in rats fed high Cholesterol/high fat diet was investigated. Rats were randomly distributed into six groups (n = 6) and given different dietary/spice treatments. Group 1 standard rat chow (control), group 2, hypercholesterolemic diet plus water, and groups 3, 4, 5, 6, hypercholesterolemic diet with 0.5 ml 200 mg · kg-1 aqueous extracts of garlic, ginger, cayenne pepper or their mixture respectively daily for 4 weeks. RESULTS: Pronounced oxidative stress in the hypercholesterolemic rats evidenced by significant (p < 0.05) increase in MDA levels, and suppression of the antioxidant enzymes system in rat's liver, kidney, heart and brain tissues was observed. Extracts of spices singly or combined administered at 200 mg.kg-1 body weight significantly (p < 0.05) reduced MDA levels and restored activities of antioxidant enzymes. CONCLUSIONS: It is concluded that consumption of garlic, ginger, pepper, or their mixture may help to modulate oxidative stress caused by hypercholesterolemia in rats.

Effect of Escherichia coli endotoxin on Archachatina marginata hemolymph coagulation system.

CONTEXT: Archachatina marginata Swainson (Achatinidae) is found in Nigeria, West Africa. Its hemolymph is applied as a disinfectant to blades and fresh cuts of circumcision in Yorubaland. The hemolymph is also used in traditional medicine practice. Investigation into its anti-endotoxin response is being studied for the first time. OBJECTIVE: This study determined whether endotoxin causes measurable and concentration-dependent protein coagulation in the separate hemolymph fractions and in hemocyte lysate (HL)/plasma mixtures. MATERIALS AND METHODS: Endotoxin was prepared by inoculating 5% w/v dextrose with locally isolated Escherichia coli cells and incubated for 48 h before sterilization. Pyrogenicity was determined by rabbit test method and use the of LAL kit. Hemolymph fractions were exposed to endotoxin while controls were exposed to endotoxin-free water (0.025 EU/ml). HL/plasma (1:1 v/v) was exposed to varied endotoxin concentrations. RESULTS: Data indicated significantly higher protein coagulates induced by endotoxin in all the hemolymph fractions (P < 0.05). Maximum protein coagulation in mixture of HL/plasma 1:1 was recorded. Exposure of HL/plasma at optimal ratio to varied endotoxin caused linear protein coagulation up to 1.0 EU/ml, beyond which it dropped significantly and unresponsive to further increase in endotoxin doses. DISCUSSION AND CONCLUSION: There was endotoxin-induced protein coagulation, which is endotoxin concentration-dependent. The optimal coagulation observed for 1:1 HL/plasma mixture suggests stronger interaction between the hemocytes and the plasma in response to endotoxin. There are LPS-binding proteins in the plasma and hemocytes of A. marginata. This finding may be employed in detection and quantification of endotoxin in future.

Antioxidant and drug detoxification potentials of Hibiscus sabdariffa anthocyanin extract.

The antioxidant and drug metabolizing potentials of Hibiscus anthocyanin extract in CCl(4)- induced oxidative damage of rat liver was investigated. Hibiscus anthocyanin extract effectively scavenge α-diphenyl-ß-picrylhydrazyl (DPPH) radical, superoxide ion, and hydrogen peroxide. It produced a 92% scavenging effect of DPPH radical at a concentration of 2.0 mg/mL. Hibiscus anthocyanin extract produced a 69 and 90% scavenging effect on superoxide ion and hydrogen peroxide, respectively, at 1.0 mg/mL, which compared favorably with the synthetic antioxidant (butylated hydroanisole and α-tocopherol). A reducing power of this anthocyanin was examined using K(3)Fe(CN)(6). Hibiscus anthocyanin extract has reducing power that is approximately 2-fold that of the synthetic antioxidant, butylated hydroanisole. Hibiscus anthocyanin extract produced a significantly increase and completely attenuated the CCl(4)-mediated decrease in antioxidant enzymes (e.g., catalase, superoxide dismutase, glutathione peroxidase, and glutathione reductase). However, the level of nonenzymic antioxidant molecules (i.e., vitamins C and E) were significant preserved by Hibiscus anthocyanin extract. There was an induction of phase II drug-detoxifying enzymes: glutathione S-transferase, NAD(H):quinone oxidoreductase, and uridyl diphosphoglucuronosyl transferase by 65, 45, and 57%, respectively. In view of these properties, Hibiscus sabdariffa anthocyanin extract can act as a prophylactic by intervening as a free radical scavenger both in vitro and in vivo as well as inducing the phase II drug detoxification enzymes.

Antioxidant and drug detoxification potential of aqueous extract of Annona senegalensis leaves in carbon tetrachloride-induced hepatocellular damage.

CONTEXT: Despite the myriad uses of Annona senegalensis Pers. (Annonaceae) leaves in folklore medicine of Nigeria, the basis is yet to be substantiated by scientific investigations. OBJECTIVES: To investigate the antioxidant (in vitro and in vivo) and drug detoxification potential of aqueous extract of A. senegalensis leaves in CCl4-induced hepatocellular damage. MATERIALS AND METHODS: In vitro antioxidant activity of the aqueous extract of A. senegalensis leaves was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH), H2O2, superoxide ion, 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulfonate) (ABTS) and ferric ion models while in vivo antioxidant and drug detoxification activities of the extract at 100, 200, and 400 mg/kg body weight were done by assaying the levels of enzymic and non-enzymic indices in CCl4-induced hepatocellular damage. RESULTS: The extract at 1 mg/mL scavenged DPPH, H2O2, superoxide ion, and ABTS radicals, whereas ferric ion was significantly (P <0.05) reduced. The levels of alkaline and acid phosphatases, alanine and aspartate aminotransferases, superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, glucose-6-phosphate dehydrogenase, reduced glutathione, vitamins C and E, glutathione S-transferase, nicotinamide adenine dinucleotide (reduced):Quinone oxidoreductase, uridyl diphosphoglucuronyl transferase, malondialdehyde, and lipid hydroperoxide that decreased in CCl4 treated animals were significantly attenuated by the extract in a manner similar to the animals treated with the reference drug. DISCUSSION AND CONCLUSION: The ability of the aqueous extract of A. senegalensis leaves to scavenge free radicals in vitro and reversal of CCl4-induced hepatocellular damage in rats suggest antioxidant and drug detoxification activities. Overall, this study has justified the rationale behind some of the medicinal uses of the plant in folklore medicine of Nigeria.

Biochemical evaluation of leachate-contaminated groundwater on the kidney of Albino rats.

The effect of leachate-contaminated groundwater on the cells of the kidney was evaluated. Serum Na(+) concentration of control rats was observed to be 120+/-1.0 nmol/l while that of rat placed on simulated leachate was 180+/-4.0 nmol/l. Serum K(+), urea and creatinine concentrations of rats placed on simulated leachate and leachate-contaminated groundwater were significantly higher(p<0.05) than those of control rats. The activity of Alkaline phosphatase (ALP) of the kidney and serum, respectively, observed for the control rats were (237+/-3.70 and 0.37+/-0.01)nmol/min/mg protein while (116+/-4.20 and 3.17+/-0.20)nmol/min/mg protein was the ALP activity of kidney and serum, respectively, observed for the rats placed on simulated leachate. Histological examination of the kidney of the control rats showed no visible lesion while that of rats placed on simulated leachate showed extensive necrosis of muscle fibres and cellular infiltration by macrophages. It is viewed that leachate-contaminated groundwater may damage kidney cells and impair renal function.

Acetaminophen perturbed redox homeostasis in Wistar rat liver: protective role of aqueous Pterocarpus osun leaf extract.

This study investigates the in vitro antioxidant potentials and attenuation of acetaminophen-induced redox imbalance by Pterocarpus osun Craib (Fabaceae) leaf in Wistar rat liver. The in vitro antioxidant activity of the extract (0.2-1.0 mg/mL) was evaluated using 2,2-diphenyl-1-picrylhydrazl (DPPH), hydrogen peroxide, superoxide ion, 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulfonate (ABTS), and ferric ion. The extract (150 and 300 mg/kg body weight) significantly (P<0.05) attenuated the altered liver and serum enzymes of acetaminophen treated animals. Superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, and glucose-6-phosphate dehydrogenase activities as well as vitamins C and E, and glutathione levels were significantly (P<0.05) elevated by the extract. The activities of uridyl diphosphoglucuronosyl transferase (59%), quinone oxidoreductase (53%), and glutathione S-transferase (73%) significantly increased. The extract of P. osun leaf extract at 1.0mg/mL scavenged the DPPH, hydrogen peroxide, superoxide ion, and ABTS at 94, 98, 92, and 86%, respectively, while ferric ion was significantly reduced. There was attenuation of malondialdehyde and lipid hydroperoxide. The results indicates that P. osun leaves attenuated acetaminophen-induced redox imbalance, possibly acting as free radical scavenger, inducer of antioxidant and drug-detoxifying enzymes, which prevented/reduced lipid peroxidation.