Aqueous Methanol Fractions Research Articles

Unraveling the Antidiabetic Effect of Alternantera brasiliana (L.) Kuntze: A Combined in Vitro and in Vivo Approach

Background of the study This study established the antidiabetic efficacy of Alternantera brasiliana in vitro and in vivo, identified the most active fraction and profiled the chemical constituents of the most active fraction. Methodology The leaf of A. brasiliana was air-dried, pulverized and extracted with methanol and evaluated for its α-amylase activity at different concentrations using in vitro method. The in vivo antidiabetic activity of the extract and glibenclamide was evaluated in glucose loaded and streptozotocin-induced diabetic rats using various doses, while the most active partitioned fraction was identified using glucose loaded method followed by identification of its chemical constituents through GC-MS analysis. Results The extract elicited good α-amylase inhibitory potential with IC50 = 0.45 mg/mL. Also, the 50 mg/kg dose demonstrated the highest percentage blood glucose level reduction and significantly ( P > 0.05) comparable to glibenclamide (5 mg/kg) from 0.5 to 4 h. The streptozotocin-induced antidiabetic assay showed that the 50 mg/kg demonstrated better activity than glibenclamide (5 mg/kg) and was significantly comparable on days 10 and 14. The aqueous methanol fraction was the most active fraction with 53% blood glucose level reduction at 4 h. The secondary metabolite profiling identified 30 chemical compounds whereby 1H-Indole-2-carboxylic acid, 6-(4-ethoxyphenyl)-3-methyl-4-oxo-4,5,6,7-tetrahydro-, isopropyl ester, Benzo[h]quinoline, 2,4-dimethyl-, thymol and 13,5-trioxane as the major constituents. Conclusion The antidiabetic activity demonstrated by the A. brasiliana extract established its antidiabetic efficacy

Phytochemical investigation, in-vitro antiplasmodial assessment and cytotoxic effect of ethanol extract of whole plant of Crotalaria arenaria (Benth)

Crotataria arenaria (Benth) is a native plant from Northern part of Nigeria which is employed as antimalarial herb in traditional medicine in the communities where it grows. The phytochemical composition, In-vitro antiplasmodial activity and in-vitro cytotoxic effect of the extract and fractions of the whole plant of Crotalaria arenaria were investigated. The mature and fresh whole plant of C. arenaria were collected, air dried and pulverized. The pulverized form of the plant were soaked in ethanol for two weeks and later decanted, filtered and concentrated using rotatory evaporator at 40oC and evaporated to dryness and labeled CRA-1. The dried ethanol solid extract (CRA-1) was patitioned/fractionated using water, chloroform, ethyl acetate, 18% aqueous methanol, n-hexane which afforded chloroform fraction (CRA-1-01), water fraction (CRA-1-02), ethyl acetate fraction (CRA-1-03) aqueous methanol fraction (CRA-1-04) and n-hexane (CRA - 1- 05) and they were dried and tested for their photochemicals and In-vitro antiplasmdial activity against Plasmodium falciparum strain (K1). The ethanol extract and its fractions were found to significantly inhibited/suppressed multi-drug resistant strain of P. falciparium (K1) in the range of 86.73% - 65.31% at varied concentrations of 5000 µg/ml, 2000 µg/ml, 1000 µg/ml and 500 µg/ml. The ethanol extract and its fractions showed the presence of tannins, saponins and alkaloids which could be responsible for the In-vitro antiplasmodial activity of the whole plant extract of C. arenaria and each of its fractions. Ethanol crude extracts of whole plant of Crotalaria arenaria and its fractions were investigated for cytotoxicity in Brine shrimp lethality Test (BSLT). Larvicidal activities were noticed with dosage concentration from 1000 µg/ml down to 10 µg/ml of the plant extract and all its fractions. The relative cytotoxic effects of extract and fractions obtained from whole plant of Crotalaria arenaria were found to be dose-dependent because higher dosage brought about an increase in mortality of Artemia salina Leach. Sea salty water of the crude ethanol extract and its fractions served as the negative control. The chloroform fraction was observed to be most cytotoxic killing 30% of brine shrimp larvae at lowest concentration of 10 µg/ml with average percentage lethality of 46.67%. Aqueous methanol and ethanol crude extract appears to show similar and closely related activities against brine shrimp larvae at highest concentration of 1000 µg/ml. The ethanol crude extract and aqueous methanol fractions are toxic at higher dosage as they were found to induce significant mortality effect (In-vitro) against Artemia salina Leach particularly at concentration of 1000 µg/ml and therefore not safe for oral consumption especially at higher uncontrolled doses but at relatively low/moderate doses. The findings in this present study demonstrated that the extract of C. arenaria (whole plant) and fractions have significant in vitro antiplasmodial activity and this has justified the traditional use of the whole plant extract of Crotaria arenaria in the folklore medicine to cure malaria related illness. The results obtained in this study may serve as key data for utilization of Crotalaria arenaria in the development of bioactive agents which could be used as antimalarial, anticancer, pesticidal, insecticidal and anti-proliferation agents. The study recommended in-vivo antiplasmodial assay of the extract of the whole plant of Crotalaria arenaria to further substantiate the findings of this present study.

Radical scavenging dihydroxycinnamic natural compounds from Trianthema pentandra

BackgroundTrianthema pentandra is a promising plant with numerous medical applications. Previous studies have confirmed that the plant is strongly cytotoxic in brine shrimp lethality tests and has antibacterial effects. However, the compounds responsible for these biological activities have not been identified. This study aimed to screen plants in an antiradical assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH). This assay was used to guide the isolation of active compounds, which were identified at the molecular structural level by spectroscopic methods. MethodsThe plant was extracted using ethanol, labelled F1 and fractionated by solvents of different polarities (F2 chloroform, F4 ethyl acetate, F5 aqueous methanol, and F6 n-hexane). The ethyl acetate and aqueous methanol (F4 and F5) fractions were selected for further purification based on their yields and activities. They were run on chloroform-methanol and n-hexane-ethyl acetate gradients, respectively. Fractions resulting from column chromatography were further screened for DPPH antioxidant activity, upon which fraction F5–1–077 had unusually high activity (IC50 = 3.57 µg/ml). Further purification of these fractions through recrystallization and high-performance liquid chromatography (HPLC) led to the isolation of three compounds. Results: Among these compounds, two were identified and characterized using FT-IR, LC-MS, and complete nuclear magnetic resonance (NMR) data, and 2,3-dihydroxycinnamic acid ethyl ester and its analog acid were isolated from the ethyl acetate fraction (F4). The former compound has been proven to have good activity in comparison with standards, ascorbic acid, and butylated hydroxytoluene (BHT), even at a low concentration of 5 µg/ml with an IC50 value of 0.13 µg/ml in the DPPH assay. The molecular docking data supported the potent activity of the compound with binding affinity, ∆G = -6.4 kcal/mol compared to the ascorbic acid (∆G = -5.0 kcal/mol) used as standard. ConclusionThis study serves as a groundbreaking foundation for the investigation of the natural dihydroxycinnamic compounds present in this plant.

Grapefruit (Citrus paradisi Mcfad.) and its phytochemical inhibits pancreatic lipase enzyme and modulates the saturated fat-induced obesity model

The prevalence of obesity has reached epidemic proportions and warrants numerous interventions, mostly using functional foods or medicinal plants to combating obesity. This review focuses on medicinal plants that elicit anti-obesity effect targeting pancreatic lipase enzyme (PLE). However, the putative processes of the plants targeting PLE and its consequential effects on triglyceride breakdown remains elusive. The effect of aqueous methanolic extracts, fractions and isolates of selected plants on PLE was tested in-vitro. The potent plant extract was examined for its effect on triglyceride levels in rats administered using saturated fat-rich coconut milk versus non-fat milk model in-vivo. Our observations illustrates that the Citrus paradisi aqueous methanolic extract (CPAME) inhibits PLE and modulate the saturated fat-induced weight gain and triglyceride levels. Whilst, the hesperidin isolated from CPAME has shown potential to inhibit PLE, the observations warrant further investigations on flavonoid and other compounds in grape fruit. Therefore, CPAME could be a promising target in combating obesity by inhibiting PLE.

In-Vivo Antivenom Effect of Annona senegalensis (Pers) Against Biological Activities of Naja nigricollis (Hallowell) Envenomation

Snake bites are a common, serious medical issue often neglected in developing countries. This study aims to investigate the effectiveness of methanolic extract from the root bark of Annona senegalensis in neutralizing the biological activities of Naja nigricollis envenomation in vivo. The methanolic extract was fractionated using a liquid-liquid fractionating method. The inhibition of venom-induced edematogenic and hemorrhagic effects was evaluated in albino rats using a pre-incubation protocol. The aqueous-methanol fraction (AM) of A. senegalensis AM root methanolic extract significantly inhibited the hemorrhagic and edema-inducing activities of the venom. The methanolic extract derived from the root bark of A. senegalensis has exhibited promising potential as an effective anti-snake venom agent.

Antidiabetic Activity of Apigenin (4, 5, 7 – Trihydroxy Flavone) from Leaves of Stachytarpheta jamaicensis (L) Vahl (Verbennaceae)

Background: Apigenin is a polyphenolic compound that belongs to the class of flavonoids and is considered highly therapeutic.
 Aim: To evaluate the antidiabetic activity of apigenin isolated from dichloromethane: methanol extract of leaves of Stachytarpheta jamiacensis (L) Vahl (Verbennaceae) in alloxan-induced diabetic rats.
 Methods: Cold maceration was used to extract the S. jamiacensis powdered leaves with dichloromethane: methanol (1:1). Hexane, dichloromethane, and aqueous methanol fractions of the extract were obtained through fractionation. To isolate the bioactive molecule, the dichloromethane fraction (DCMF) was then subjected to column chromatography and eluted with several solvent mixtures in ascending polarity order. With the aid of data from FTIR, UV, GC-MS, 1HNMR (400MHz), and 13CNMR (101MHz), the structure of the isolated compound was identified. The Phytochemical analysis of the isolate and acute toxicity study was done following standard procedures. The anti-diabetic potential of the isolate was assessed by determining fasting blood glucose levels on alloxan-induced rats at the dose of 25 and 50 mg/kg body weight.
 Results: The compound was identified as apigenin (4, 5, 7 – trihydroxy flavones) and showed significant (p<0.05) reduction of 79.56 and 81.74 % in fasting blood glucose levels at the dose of 25 and 50 mg/kg respectively when compared with the standard drug (glibenclamide 83.40 %). The isolate's phytochemical analysis revealed flavonoids and the LD50 test demonstrates that apigenin was not harmful.
 Conclusion: The findings show that the apigenin from Stachytarpheta jamaicensis (L) Vahl has potent anti-diabetic properties.

Endocrine disruptors in Adansonia digitata (Linn) extract induce alteration of female Wistar rats’ oestrous cycle, hormone and lipid profiles

ObjectiveHexane-acetyl acetate (HAAF) and acetyl acetate–methanol fractions (AAMF) but not aqueous methanol (AQMF) and aqueous fractions (AQF) of Adansonia digitata Linn root bark induce reproductive effects in female Wistar rats. The current study investigated the exclusive components of HAAF, AAMF, AQMF, and AQF of Adansonia digitata Linn root bark and the effect of AAMF on the female Wistar rat's oestrous cycle progression, and hormone and lipid profiles. MethodologyGas chromatography and mass spectrometry explored the components of HAAF, AAMF, AQMF, and AQF. Mature female Wistar rats with a proven 4–5-days oestrous cycle were synchronised and randomly assigned into three treatment groups of 30 rats each on the day of proestrus. For seven days, rats in the different groups received 0, 150, and 300 mg kg-1 body weights of AAMF, respectively. Six rats were euthanised from each group based on a standard oestrous stage-timed sequence. The oestrous stage, hormone profile (oestrogen, progesterone, progesterone/oestrogen ratio, and FSH) and lipid profile (Total cholesterol-TC, Triglycerols, High-HD and low density-LD lipid cholesterol) of the euthanised rats were determined. Resultstricosene, cyclopentadecanone 2-hydroxy-, oleic acid, and 9,17-octadecadienal, were exclusively found in HAAF and AAMF. The oestrous stage, serum hormone and lipids varied significantly (p < 0.05) between treatment groups. AAMF fraction induced sustained progesterone levels and depleted oestrogen levels, and TC and LDL were inversely related to serum oestrogen levels. DiscussionThe results suggest a depression of oestrogen and sustenance of progesterone-mediated effects, respectively, on GnRH surge. Oleic acid in AAMF may be responsible for its reproductive effects. ConclusionAAMF fraction of A. digitata (L) root bark disrupts the endocrine activity in female Wistar rats. The oleic acid component of the AAMF fraction may be responsible for modulating the activities of reproductive hormones. The authors recommend further studies to ascertain the significance of Adansonia digitata extract's oleic acid in regulating the female reproductive cycle.

Isolation and identification of novel selective antitumor constituents, sidrin and sidroside, from Zizyphus spina-christi

BackgroundThe leaves of Zizyphus spina-christi (L.) Willd contain several compounds exhibiting different pharmacologic activities. However, studies on the cytotoxic activity of these compounds are limited. ObjectivesWe aimed to investigate and isolate cytotoxic compounds with selective antitumor effects from the leaves of Z. spina-christi using bioassay-guided fractionation of methanol extract. MethodsPowdered, dried leaves were subjected to methanol extraction and fractionated using n-hexane, chloroform, ethyl acetate, and n-butanol. Fractions with positive cytotoxicity against HeLa and THP-1 cell lines were further fractionated and eluted using various concentrations of organic solvents. Active compounds were isolated using different chromatographic methods and their chemical structures were determined using extensive spectroscopic methods, such as 1D NMR (1H NMR, 13C NMR, and DEPT), 2D NMR (COSY, HMBC, and HMQC), HRFAB-MS, and IR. Furthermore, the cytotoxic effects of the isolated compounds were evaluated against 62 tumor cell lines (including HeLa and THP-1) in addition to normal bone marrow cells. ResultsThe chloroform and aqueous methanol fractions of the leaves showed cytotoxic activity. Two compounds were successfully isolated and named “sidrin” (13-β-hydroxy-lup-20(30)-ene-2,3-β-epoxy-28-carboxylate) and “sidroside” (3-O-β-D-glucopyranosyl-(1–3)-α-L-arabinopyranosyl-jujubogenin-20-O-α-L-rhamnopyranoside). Sidrin exhibited cytotoxic activity against the human leukemia (Hl-60, RPMI-8226), lung cancer (A549, EKVX), breast cancer (BT-549, MDA-MB-231/ATCC), colon cancer (KM12), melanoma (M14, SK-MEL-5), and central nervous system (CNS) cancer (SF-295) cell lines, and selectivity was observed against the Hl-60, EKVX, BT-549, KM12, and SF-295 cell lines. In addition, sidrin was more active than sidroside and doxorubicin against the Hl-60 and EKVX cell lines. In contrast, sidrin had a similar effect to doxorubicin against the BT-549 and renal cancer (UO-31) cell lines. Sidroside was more selective against the leukemia (CCRF-CEM, MOLT-4), lung cancer (HOP-92, NCI-H322M), breast cancer (MDA-MB-468), melanoma (LOX IMVI), CNS cancer (SNB-19), ovarian cancer (OVCAR-8), renal cancer (UO-31, RXF 393), and prostate cancer (PC-3) cell lines. Both compounds exhibited similar activity against the breast cancer (MDA-MB-231, T-47D), colon cancer (HCC-2998, HCT-116), ovarian cancer (OVCAR-3), renal cancer (UO-31, 786–0, and SN 12C) cell lines. Normal bone marrow cells were unaffected at the same concentrations of sidrin and sidroside applied to tumor cells. ConclusionsThese results suggest tumor-selective cytotoxicity of sidrin and sidroside.

Free radical scavenging and antiproliferative evaluation of the Olax viridis Oliv. (Olacaceae) whole root

Olax viridis Oliv (Olacaceae) has numerous ethnomedicinal uses including treatment of breast cancer. The study aimed at evaluating the free radical scavenging and antiproliferative activities of O. viridis whole root and the phytoconstituents responsible for this activity. The sample was defatted using n-hexane(NHE), further extracted by cold maceration using absolute methanol to obtain crude extract which was subjected to liquid-liquid partitioning using dichloromethane to afford the dichloromethane fraction (DCM) and aqueous methanol fraction (MEF). Further precipitation of some aqueous methanol fraction (MEF) using acetone yielded saponin-rich fraction (SRF). Furthermore, acid hydrolysis of the SRF gave the sapogenin-rich fraction (ASRF). These extract/fractions: NHE, DCM.,MEF, SRF and ASRF were used for further investigation. Phytochemical screening of fractions was carried out using standard phytochemical methods. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was used for antioxidant evaluation in vitro with ascorbic acid as the reference standard for comparison while antiproliferative (AP) activity was by cell viability using yeast (Saccharomyces cerevisae) as a model organism. O. viridis whole root contains carbohydrate, cardiac glycoside, steroids, triterpenes and saponins. The fractions showed dose-dependent activities for DPPH radical scavenging activity with the trend at 1 mg/ml thus: DCM (77.53%) &gt;ASRF(70.60%) &gt;SRF(46.82%) &gt;MEF(33.50%) &gt;NHE(22.83%) and the promising fractions showed median concentration; ASRF(IC50=0.54 mg/ml) &gt;DCM(IC50=0.55 mg/ml). All the fractions showed dose dependent antiproliferative activities ASRF(IC50=3.35 mg/ml) &gt;SRF(IC50=5.10 mg/ml) &gt;MEF(IC50=6.28 mg/ml) &gt;DCM(IC50=7.44 mg/ml). Sapogenin may be responsible for the AP and antioxidant activities as ASRF which contains triterpenidal/steroidal nucleus showed a promising activity compared to other fractions. This study validated the traditional use of Olax species in the treatment of cancer.

An Analysis of the Toxicity, Antioxidant, and Anti-Cancer Activity of Cinnamon Silver Nanoparticles in Comparison with Extracts and Fractions of Cinnamomum Cassia at Normal and Cancer Cell Levels

In this work, the extract of cinnamon bark was used for the green synthesis of cinnamon-Ag nanoparticles (CNPs) and other cinnamon samples, including ethanolic (EE) and aqueous (CE) extracts, chloroform (CF), ethyl acetate (EF), and methanol (MF) fractions. The polyphenol (PC) and flavonoid (FC) contents in all the cinnamon samples were determined. The synthesized CNPs were tested for the antioxidant activity (as DPPH radical scavenging percentage) in Bj-1 normal cells and HepG-2 cancer cells. Several antioxidant enzymes, including biomarkers, superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione-S-transferase (GST), and reduced glutathione (GSH), were verified for their effects on the viability and cytotoxicity of normal and cancer cells. The anti-cancer activity depended on apoptosis marker protein levels (Caspase3, P53, Bax, and Pcl2) in normal and cancerous cells. The obtained data showed higher PC and FC contents in CE samples, while CF showed the lowest levels. The IC50 values of all investigated samples were higher, while their antioxidant activities were lower than those of vitamin C (5.4 g/mL). The CNPs showed lower IC50 value (55.6 µg/mL), whereas the antioxidant activity inside or outside the Bj-1 or HepG-2 was found to be higher compared with other samples. All samples execrated a dose-dependent cytotoxicity by decreasing the cells' viability percent of Bj-1 and HepG-2. Similarly, the anti-proliferative potency of CNPs on Bj-1 or HepG-2 at different concentrations was more effective than that of other samples. Higher concentrations of the CNPs (16 g/mL) showed greater cell death in Bj-1 (25.68%) and HepG-2 (29.49%), indicating powerful anti-cancer properties of the nanomaterials. After 48 h of CNPs treatment, both Bj-1 and HepG-2 showed significant increases in biomarker enzyme activities and reduced glutathione compared with other treated samples or untreated controls (p < 0.05). The anti-cancer biomarker activities of Caspas-3, P53, Bax, and Bcl-2 levels were significantly changed in Bj-1 or HepG-2 cells. The cinnamon samples were significantly increased in Caspase-3, Bax, and P53, while there were decreased Bcl-2 levels compared with control.

Evaluation of the Antioxidant and Wound Healing Properties of 80% Methanol Extract and Solvent Fractions of the Leaves of Vernonia auriculifera Hiern. (Asteraceae).

The leaves of Vernonia auriculifera (Asteraceae) have traditionally been used to treat wounds in several regions of Ethiopia. The purpose of this study was to assess the wound healing properties of the leaf extract and solvent fractions of V. auriculifera in mice. The leaf extract and solvent fractions of V. auriculifera have also been evaluated for their anti-oxidant properties because of their impact on the wound healing process. Air-dried leaves were extracted using 80% methanol. They were also successively fractionated with n-hexane, ethyl acetate, and methanol. The residue was then macerated in water for 72 hr. Simple ointment bases were formulated according to British Pharmacopoeia. Thereafter, two types of ointment formulations, 2.5% w/w and 5% w/w, were formulated. Wound healing and acute dermal toxicity studies were performed on mice. To assess free radical scavenging activity, a 2,2-diphenyl-2-picrylhydrazyl free radical (DPPH) assay was performed. In both models, wounds treated with 2.5% and 5% (w/w) of the ME, the aqueous fraction (AQF), methanol fraction (MEF), and ethyl acetate fraction (EAF) ointments demonstrated significant wound healing activity, as shown by enhanced wound contraction, a shortened epithelialization time, increased hydroxyproline content, and enhanced tissue breaking strength. The extract and solvent fractions displayed free radical scavenging activity with IC50 values of 1.2 mg/mL, 1.46 mg/mL, 1.5 mg/mL, and 2.83 mg/mL for ME, AQF, MEF, and EAF, respectively, as compared to 1.42 mg/mL for ascorbic acid. The result of this study indicates that 80% of methanol extract and solvent fractions are endowed with wound healing activity. Additionally, this study has also revealed that ME, AQF, MEF, and EAF have the capacity to scavenge free radicals. The study indicated that the wound healing effect could be attributed to the anti-inflammatory and antioxidant activities.

Nelsonia canescens (Acanthaceae) aqueous extract and partitioned fractions ameliorates type-2 diabetes in alloxan-induced diabetic rats

BackgroundDiabetes mellitus is a metabolic disorder that affects the body’s ability to produce or use insulin. There is a continuous rise of this disease particularly in developing countries due to changes in life style and poverty among the people. In this study, antidiabetic activities of aqueous extract of Nelsonia canescens and its partitioned fractions in alloxan-induced diabetic rats were evaluated. Male albino rats were divided into 9 groups (diabetic and non-diabetic) of 5 rats each. Diabetes was induced by single intraperitoneal administration of alloxan (90 mg/kgbwt). The experimental design consists of a diabetic control group (untreated), a normal control group (1 mL saline), a standard diabetic drug (Glibenclamide; 5 mg/kgbwt), two doses (50 and 300 mg/kgbwt) of aqueous extract, ethyl acetate and methanol fractions of Nelsonia canescens were orally administered for a period 21 days. Blood glucose of the rats was monitored at 3-days intervals while biochemical and in vivo antioxidant assays of serum and liver were determined after 21 days.ResultsThe hypoglycemic effect of the extract observed was in a dose dependent manner with a significant reduction (p < 0.05) of blood glucose in ethylaceate fraction > aqueous extract > methanol fraction compared with the diabetic control group. A significant difference (p < 0.05) in lipid profiles and serum enzyme activity of rats in the diabetic control group was observed compared with the extract and fraction treated groups.ConclusionThe results suggest that the aqueous extract and fractions of N. canescens showed hypoglycemic and hypolipidemic potentials and significantly (p < 0.05) reduced the progression of oxidative stress.

In vitro investigation of antimicrobial, enzyme inhibitory and free radical scavenging activities of Inula salicina L.

In this study, in vitro biological activities and total phenol/flavonoid contents of methanol extract (ISM) and its hexane (ISH), chloroform (ISC), ethyl acetate (ISEA) and aqueous methanol (ISAM) fractions obtained from aerial parts of Inula salicina were investigated. ISEA showed the highest antioxidant activity against DPPH and ABTS radicals with an IC50 value of 0.014 mg ml-1for both assays. ISEA exhibited a good anti-inflammatory activity with an IC50 value of 0.060 mg ml-1. ISEA was found to exhibit a moderate level of antidiabetic activity against α amylase enzyme with an IC50 value of 0.290 mg ml-1. ISEA and ISM presented low and moderate inhibitory activity against acetylcholinesterase and butyrylcholinesterase enzymes with IC50 values of 0.577 and 0.279 mg ml-1, respectively. ISC with MIC values of 78 and 156 µg ml-1 displayed a significant antimicrobial activity against Staphylococcus aureus and S. epidermidis, respectively. Almost all extracts had moderate effect against Candida species. The highest total phenolic and flavonoid contents were determined in ISEA with 574.8 mg GAE (gallic acid equivalent) g-1 extract and 30.48 mg QE (quercetin equivalent) g-1 extract, respectively. These results showed that ISEA had a good antioxidant and anti-inflammatory activity with moderate α-amylase and butyrylcholinesterase inhibitory activity. Also, ISC exhibited a significant antimicrobial activity against Staphylococcus species.

Phytocheical and antidiabetic evaluation of the solvent fractions of &lt;em&gt;Coccinia barteri&lt;/em&gt; Hook F (Cucurbitaceae) on alloxan induced diabetic rats

The use of natural anti-diabetic medications in treating diabetes is receiving more attention daily. This study evaluated the phytochemical constituents and anti-diabetic properties of the leaves of Coccinia barteri on alloxan induced diabetic rats. The powdered leaf was macerated in methanol for 72hrs and then fractionated with ethyl acetate, chloroform and aqueous methanol solvents. Phytochemical and analytical evaluations were done using standard methods. The toxicity study was carried out on mice using Lorke’s method. The Albino rats were divided into 8 groups of 4 rats each, 6 groups for the fractions and 2 for negative control and positive controls. Alloxan monohydrate (120 mg/kg) was used to induce diabetes. Treatment were with oral doses of the fractions (100 and 300mg/kg body weight) and Glibenclamide 5mg for 7days and their glucose levels were checked daily. The macroscopic and microscopic analysis showed dark green leaf, reticulate veination, smooth texture, fresh leafy odour, glandular trichome, wavy epidermal cell and anisocytic stomata. Analytical evaluation produced total ash (7.00), acid insoluble ash (0.93), water soluble ash (2.96), moisture content (8.40), alcohol extractive value (29.67), water extractive value (40.17) and ethyl acetate extractive value (21.00). The phytochemical analysis revealed flavonoids, alkaloids, steroids, glycosides and saponins are present. The anti-diabetic test revealed a significant decrease in the rat's fasting blood glucose especially in the aqueous methanol fraction (300 mg/kg). The least reduction was seen in chloroform fraction (100 mg/kg).The phytochemical constituents C.barteri has good anti-diabetic effects and can be used for further studies.

In vitro antioxidant, anti‐inflammatory and antihypertensive activities of methanol leaf extract of Peasea americana

Hypertension (HBP) is a cardiovascular disease of man and animal worldwide. It is a risk factor for many other cardiovascular diseases and target organ dysfunction. HBP management with orthodox medicine is expensive and unaffordable to patients from low income countries in Africa and they are associated with side effects. P. americana leaf extract (PALE) is commonly used in the management of hypertension in Nigeria trado‐medicine. In this study, we investigated the antioxidant, anti‐inflammatory and anti‐hypertensive activities of the crude methanol extract, fractions and phytochemicals of P. americana leaf. The in vitro‐antioxidant assays were carried out to evaluate the free radicals scavenging activities of PALE on 1, 1‐diphenyl‐2‐picrylhydroxyl (DPPH), 2, 2‐azenobis‐3‐ethyl benzothiozoline‐6‐sulfonic acid (ABTS), hydroxyl and nitric oxide radicals. In addition, metal chelating and ferric reducing power assay were done. Anti‐inflammatory activities were evaluated using 15‐1ypoxygenase enzyme inhibition assay. Absorption were read spectophotometrically and 1C50 was calculated using a standard calibration curve. Phytocompound isolation was by extract fractionation, column, thin layer and preparatory thin layer chromatography. Crude methanol extracts, N‐hexane, ethyl acetate, chloroform, N‐butanol and aqueous methanol fractions had significantly higher anti‐oxidant activities when compared with gallic acid. Their anti‐inflammatory activities were comparable to that of Indomethacin and antihypertensive activity for PALE (with IC50 of 135.99±10.06) was significantly lower when compared with captopril (with IC50 41.86±2.10). Four pure phytochemicals were isolated and named LEACA, LEACB, LEACC, and LEACD. The isolated compounds had significantly higher antioxidant activities on DPPH, ABTS, and hydroxyl and nitric oxide radicals when compared with gallic acid. The anti‐hypertensive activities of the isolated phytocompounds from the ethyl acetate fraction of the leaf were significantly higher (with IC50 of 24.83±0.63, 9.48±1.45, 2.79±1.35 and 1.59±0.48 respectively) than that of captopril (with 1C50 of 41.89±2.10). The findings from this study suggest that P. americana leaf has free radical scavenging and antioxidant activities, anti‐inflammatory and anti‐hypertensive activities and can ameliorate oxidative stress and inflammation associated with hypertension.

Peel of pineapple (Ananas comosus) as a potential source of antioxidants and photo-protective agents for sun protection cosmetics

The present study was aimed to evaluate the antioxidant activity and photo-protective property of methanolic extract of pineapple peel to study its potential as a natural source in sun protection cosmeceutical products. The chemical constituents of dried and powdered pineapple peels extracted into methanol by soxhlet extraction were sequentially partitioned into hexane, dichloromethane (DCM) and aqueous methanol (50%). The 50% methanol fraction was found to be rich in phytochemicals with antioxidant activity with IC50 value of 85.70 ± 0.09 μg/mL and the total phenolic content of 208.899 ± 9.388 mg gallic acid equivalent (GAE)/kg dry weight of plant material. DCM fraction was rich in flavonoids with total flavonoid content of 79.913 ± 2.491 mg catechin (CAT) equivalent/kg dry weight of pineapple peel. All the fractions of the pineapple peel were exhibited UV – B protection ability and DCM fraction was consisted with an impressive photoprotective property with the Sun Protection Factor (SPF) of 29.74 ± 0.03 at 1 mg/mL. The aqueous methanol fraction was found to be the most photo-stable after irradiation with direct solar radiation for 21 days. Pearson's correlation revealed that there is a very strong positive correlation between SPF and TFC (r = 0.9497) and a strong positive correlation between SPF and TPC (r = 0.6366). Since the DCM fraction was rich in compounds with photo-protective properties it was further separated by silica gel column chromatography and analyzed by GC-MS for volatile compounds. The results revealed that the DCM fraction was rich in bioactive compounds with known antioxidant activities indicating the possibility of using pineapple peel to develop natural sunscreen formulations with antioxidant properties.

Alpha-Amylase Inhibitory and Antioxidant Activities in Aqueous Acetone Extract and its Fractions from Ampelocissus martini Root

This study aimed to evaluate and correlate phytochemical content, antioxidant activity and alpha-amylase inhibitory activity in aqueous acetone extract and fractions derived from it (ethyl acetate fraction, watersoluble fraction, aqueous methanol fraction and aqueous acetone fraction) which are obtained from Ampelocissus martini Planch. root. Ethyl acetate fraction and aqueous acetone fraction had the highest total phenolic content and total proanthocyanidin content, respectively. 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid), cupric reducing antioxidant capacity and ferric reducing antioxidant power assays showed that aqueous acetone fraction had higher antioxidant activity compared to other samples and standards. Acarbose and all samples except aqueous methanol fraction inhibited alpha-amylase, a key enzyme linked to type 2 diabetes, in a dose-dependent manner and aqueous acetone fraction showed the strongest inhibition (half-maximal inhibitory concentration=8.77±0.28 μg/ml). Aqueous acetone fraction was a mixed noncompetitive inhibitor of the enzyme. Correlation analysis showed strong positive correlations among proanthocyanidin content, antioxidant activity and alphaamylase inhibitory activity. These results suggest that aqueous acetone fraction, proanthocyanidins-rich fraction from Ampelocissus martini root, may be used for effective diabetes management because of its high potential antioxidant activity and alpha-amylase inhibitory activity.

Clitorienolactones and Isoflavonoids of Clitorea ternatea Roots Alleviate Stress-Like Symptoms in a Reserpine-Induced Zebrafish Model.

Clitorea ternatea has been used in Ayurvedic medicine as a brain stimulant to treat mental illnesses and mental functional disorders. In this study, the metabolite profiles of crude C. ternatea root extract (CTRE), ethyl acetate (EA), and 50% aqueous methanol (50% MeOH) fractions were investigated using ultrahigh-performance liquid chromatography–diode array detector–tandem mass spectrometry (UHPLC–DAD–MS/MS), while their effect on the stress-like behavior of zebrafish, pharmacologically induced with reserpine, was investigated. A total of 32 compounds were putatively identified, among which, a series of norneolignans, clitorienolactones, and various flavonoids (flavone, flavonol, isoflavone, and isoflavanone) was found to comprise the major constituents, particularly in the EA and 50% MeOH fractions. The clitorienolactones, presently unique to the species, were present in both the free and glycosylated forms in the roots. Both the EA and 50% MeOH fractions displayed moderate effects on the stress-induced zebrafish model, significantly decreasing freezing duration and elevating the total distance travelled and average velocity, 72 h post-treatment. The results of the present study provide further evidence that the basis for the use of C. ternatea roots in traditional medicine to alleviate brain-related conditions, such as stress and depression, is attributable to the presence of clitorienolactones and the isoflavonoidal constituents.

Phytochemical profiling and GC-MS analysis of aqueous methanol fraction of Hibiscus asper leaves

BackgroundMedicinal plants are of great importance to researchers in the field of pharmacology as most pharmaceutical industries depend on medicinal plant for their raw materials. Hibiscus asper belongs to the family Malvaceae and is well known for its medicinal properties. The present study was carried out to evaluate the antioxidant effect and possible bioactive components present in the aqueous methanol fraction of Hibiscus asper leaves.ResultsThe phytochemical of aqueous methanol fraction of Hibiscus asper leaves (AMFHAL) revealed the presence of flavonoids, tannin, phenols, saponins, alkaloids, glycosides, terpenoids, and steroids. The GC-MS analysis revealed the presence of twenty-three bioactive compounds which include 9,12,15-octadecatrien-1-ol, n-Hexadecanoic acid, octadecatrienol acid, methyl palmitate, and phytol.ConclusionThe phytochemical and GC-MS profiling of aqueous methanol fraction of Hibiscus asper leaves revealed the presence of bioactive compounds with important medicinal properties. Hence, the presence of these phytochemicals could be responsible for the therapeutic effects of the plant.

Biological activity of phenolics enriched extracts from industrial apple pomace

Apple processing industries around the globe generate huge quantity of pomace as waste material, whose sustainable and cost-effective utilization continually being attempted. In general, industrial apple pomace is a conglomeration of different varieties, however, rich in array of inherited nutritional and phytochemical constituents. In present study, aqueous-ethanol, -methanol and -acetone mediated extractions of phenolics from industrial apple pomace was performed. The obtained extracts from respective solvents were further partitioned with ethyl acetate. The phytochemical evaluation of ethyl acetate fractionated aqueous acetone fraction (APA1), aqueous ethanol fraction (APE1) and aqueous methanol fraction (APM1) by high pressure liquid chromatography and electrospray-ionization quadrupole time-of-flight tandem mass spectrometry showed the presence of phloridzin, phloretin, quercitrin and quercetin as major constituents. The cytotoxic effects of APA1, APM1, and APE1 fractions were evaluated against human cancer cell lines i.e. cervical squamous cell carcinoma (SiHa), oral carcinoma (KB) and colorectal adenocarcinoma (HT-29) cell lines. Significant differences were obtained for oral cancer cells in time and dose dependent manner. Cytotoxicity data validated by clonogenic cell survival assay showed significant inhibition of KB cancer cells by APA1 and APE1 after 24 and 36 h. Caspase 3/7 activity of fractions was also found to be increased in time dependent manner. Furthermore, the flow cytometer analysis revealed that KB cells follow apoptotic and necrotic mechanism for cell death after treatment with APA1 and APE1 fractions for 24 and 30 h. Results also showed significant nitric oxide inhibition in lipopolysaccharide– interferon gamma stimulated mice peritoneal macrophages at different concentrations. Present study established that industrial apple pomace indeed has substantial amount of bioactive phenolics that can be bioprocessed to develop variety of health supplements.