Antioxidant, Phytotoxic and Antiurease Activities, and Total Phenolic and Flavonoid Contents of Conocarpus lancifolius (Combretaceae)

Purpose: To evaluate the antioxidant, phytotoxic and anti-urease properties of dichloromethane and methanol extracts of Conocarpus lancifolius in correlation with total phenolic and flavonoid contents.Methods: The whole plant (dried aerial parts and root) of Conocarpus lancifolius was extracted successively with dichloromethane, methanol and water at room temperature. Antioxidant activity was determined by DPPH, Nitric oxide scavenging and FRAP methods. Phytotoxicity was performed by Lemna minor assay and analyzed relative to control with effective dose (ED50) to determine FI50 values (concentration necessary to inhibit 50 % frond proliferation) and 65 % confidence intervals. Urease inhibitory activity was assessed at a concentration of 125 μg/mL by Berthelot reaction with slight modification. Total phenolic contents were calculated with reference to gallic acid equivalent and confirmed by Folin and Ciocalteau’s phenol method. Total flavonoid was determined with reference to quercetin.Results: The DPPH and hydroxyl radical scavenging activities of the methanol extract were 93.35 %. The phytotoxicity of the methanol extract was 90 % growth regulation while the anti-urease inhibitory activity was 91.1 % with half-maximal inhibitory concentration (IC50) of 49.1 ± 1.3 μg/mL. Total flavonoid contents of dichloromethane extract was 629.4 ± 1.57 μg/mL. The phenolic content of the extract calculated with reference to quercetin, gallic acid, chlorogenic acid, ferulic acid and 4-hydroxy 3-methoxy benzoic acid equivalent was 45.772, 9.779, 70.304, 74.93 and 57.80 ppm, respectively.Conclusion: The results confirm that Conocarpus lancifolius extracts possess some antioxidant, phytotoxicity and anti-urease potentials due to its phenolic and flavonoid contents.Keywords: Antioxidant, Phenolics, Falvonoids, Phytotoxicity, Anti- urease, Conocarpus lancifoliu

Total phenolic and flavonoid contents, cytotoxic, immunomodulatory and anti-inflammatory potential of whole plant of Astragalus creticus (Fabaceae)

Purpose: To determine total phenolic and flavonoid contents, as well as the cytotoxic, immunemodulatoryand anti-inflammatory potentials of the whole plant of Astragalus creticus (Fabaceae).Methods: Folin-Ciocalteu (FCR) method was used for determination of total phenolic and flavonoid contents of the methanol and dichloromethane extracts of Astragalus creticus. The cytotoxic potential of the extracts on 3T3 and HeLa cell lines were evaluated using MTT assay. Brine shrimp larvae mortality was determined by lethality bioassay, while inhibitory effects were determined on mouse fibroblast (3T3)and cervical cancer (HeLa) cell lines. In vitro immunomodulatory and in vivo anti-inflammatory effectswere assessed using reactive oxygen species (ROS) chemiluminescence and formalin-induced rat paw edema assays, respectively.Results: Dichloromethane extract had higher contents of phenolics (TPC = 324.75 ± 2.47 mg GAE/g) and flavonoids (TFC = 95.51 ± 0.82 QE/g) than the methanol extract (TPC = 79.82 ± 1.53 mg GAE/g, TFC = 56.11 ± 0.93 QE/g). The dichloromethane extract exhibited high cytotoxic andimmunomodulatory potentials, with 76.66 % mortality in brine shrimp lethality bioassay and 83.9 % inhibition (IC50 = 18.0 ± 1.1 μg/mL) in chemiluminescence assay. The extract also resulted in 22 and 13 % inhibition of viability of HeLa and 3T3 cells, respectively, while the methanol extract produced 13 % inhibition of both cell lines. The methanol extract produced very significant anti-inflammatory activity,with a maximum of 49 % inhibition of paw edema at a dose of 160 mg/kg (p < 0.01).Conclusion: These results suggest that the dichloromethane and methanol extracts of Astragalus creticus (Fabaceae) exert cytotoxic, immunomodulatory and anti-inflammatory effects. These findings provide scientific validation for the traditional medicinal use of the Astragalus genus

Isolation of squarrosal and squarrosol compounds from methanol root extract of Ruellia squarrosa (Acanthaceae)

Purpose: To identify, characterize and structurally elucidate bioactive compounds from root of Ruellia squarrosa.Methods: One kilogram of crude Ruellia squarrosa root was shade dried for 14 days, ground to a fine powder and subjected to a methanol extraction. The resultant extract underwent column chromatography for further purification. The isolated compounds were subjected to ultraviolet spectroscopy (UV), infra-red (IR), proton nuclear magnetic resonance (1H-NMR), 13C–NMR and high resolution electron ionization mass spectrometry (HR-EI-MS) for the identification, characterization and structural elucidation of bioactive compounds. The most active compounds were tested for anticancer activities against human prostate cancer cell.Results: Two active compounds, squarrosol and squarrosal, were obtained with half-maximal inhibitory concentration (IC50) of 15.6 and 26.6 μg/mL, respectively, against human prostate cancer cell lines. Squarrasol showed a significantly (p < 0.05) greater inhibition of cell proliferation than the same dose of squarrasal.Conclusion: These findings suggest that extracts of Ruellia squarrosa containing the bioactive compounds, squarrosol and squarrosal, can potentially be developed for the treatment of human prostate cancer.Keywords: Ruellia squarrosa, Prostate cancer, Squarrosol, Squarrosal, Anit-proliferativ

New α-Glucosidase inhibitors from Croton bonplandianum Croton bonplandianum Baill (Euphorbiaceae)

Purpose: To isolate and evaluate α-glucosidase inhibitors from dichloromethane extract of Croton bonplandianum Baill as probable remedy for management of diabetes.Methods: Activity-guided isolation of constituents from dichloromethane extract was carried out. Fractionation of dichloromethane extract by column chromatography on silica gel and Sephadex LH 20 using different mobile phase systems led to the isolation of compounds (A-I). The structures of these isolated compounds were established by ultraviolet (UV) and infrared (IR) spectroscopy. Proton nuclear magnetic resonance (1H NMR), 13C NMR and mass spectrophotometry, electron impact mass spectroscopy (EIMS) and high resolution mass spectroscopy (HRMS) were used for structural elucidation. All the isolated compounds were screened for their α-glucosidase inhibitory activity using standard in vitro α-glucosidase inhibition assay. Acarbose was used as positive control.Results: On the basis of their physical and spectral data from literature, the isolated compounds were identified as n-pentacosanyl-n-nonadeca-7′-en-9′-α-ol 1′-oate (A), n-tridecanyl n-octadec-9,12-dienoate (B), nonacosyl hexadecanoate (C), heptacosanoic acid (D), 1,3,5-trihydroxy-2-hexadecanoylamino- (6e,9e) heptacosdiene (E),cumarin (F), betulin (G), stigmasterol (H), and 3,5-dimethoxy 4-hydroxy cinnamic acid (I).Compounds F, GandI possessed significant α glucosidase inhibitory activity in a concentration-dependent manner with 50 % inhibitory concentration (IC50) values ranging from 23.0 to 26.7 μg/mL, relative to that of the positive control, acarbose (IC50, 38.2 μg/mL).Conclusion: The plant contains bioactive compounds with α-glucosidase inhibitory activity. This lendssome support for the traditional use of this herb in the management of diabetes. Compound F, GandI possessed significant α glucosidase inhibitory activity in a concentration-dependent manner and may be developed as a new α-glucosidase inhibitor.Keywords: α-Glucosidase, Inhibition, Diabetes, Acarbose, Cumarin, Betulin, 3,5 Dimethoxy 4-hydroxy cinnamic acid, Croton bonplandianu

Assessment of anti-diabetic activity of Cassia sophera (Caesalpiniaceae)

Purpose: To examine the ethnomedicinal claims regarding the antidiabetic uses of Cassia sophera L. (Caesalpiniaceae) using an alloxan-induced diabetes model.Methods: The methanol extracts of leaves (CSLM) and roots (CSRM) of C. sophera were evaluated for hypoglycemic and anti-diabetic activities in normal and alloxan-induced diabetic rats. Alloxan (120 mg/kg, i.p.) was administered to induce diabetes in rats. A dose regime of 50, 100 and 200 mg/kg of CSLM and CSRM was given orally to the respective groups (n = 6). Blank group consisted of normal animals maintained on saline. The diabetic untreated group served as negative control while the group that received glibenclamide (5 mg/kg) was positive control.Results: A significant (p < 0.05) lowering of fasting blood glucose level FBG in oral glucose tolerance test (OGTT) in normal rats was observed after daily  administration of the extract for 7 days. Both extracts demonstrated decreased (p < 0.05) BGL with significantly (p < 0.05) improved glucose tolerance and body weight at the end of 4th, 7th and 14th day in extract-treated diabetic rats when compared with negative control and normal untreated group, respectively. In normoglycemic rats, CSLM and CSRM showed dose-dependent decrease in BGL.Conclusion: These results suggest that both extracts possess significant blood glucose lowering activity in normal as well as in diabetic rats.Keywords: Cassia sophera, Hypoglycemic activity, Anti-diabetic activity, Alloxan, Weight los

FAMILY ACANTHACEAE AND GENUS APHELANDRA: ETHNOPHARMACOLOGICAL AND PHYTOCHEMICAL REVIEW

Aphelandra belong to family Acanthaceae. We have reviewed traditional uses, pharmacological potential and phytochemical study of family Acanthaceae and genus Aphelandra. Traditionally the most important part use in Acanthaceae is the leaves and they are used externally for wounds. We have found that Acanthaceae possess antifungal, cytotoxic, anti-inflammatory, anti-pyretic, anti-oxidant, insecticidal, hepatoprotective, immunomodulatory, Anti- platelet aggregation and anti-viral potential. Phytochemical reports on family Acanthaceae are glycosides, flavonoids, benzonoids, phenolic compounds, naphthoquinone and triterpenoids. We have also document genus Aphelandra, its phytochemical and pharmacological potential

CYTOTOXIC, α-CHYMOTRYPSIN AND UREASE INHIBITION ACTIVITIES OF THE PLANT Heliotropium dasycarpum L.

Background: The aim of this study was to investigate Cytotoxic, α-Chymotrypsin and Urease inhibition activities of the plant Heliotropium dasycarpum. Materials & Methods: Dichloromethane and methanol extracts of the plant were evaluated for cytotoxic, α-Chymotrypsin and Urease inhibition by using in vivo Brine Shrimp lethality bioassay and in vitro enzymatic inhibition assays respectively. Results: The methanol extract of the plant exhibited significant cytotoxic activity. Out of 30 brine shrimp larvae, 2 (6%), 26 (86%) and 28 (93%) larvae were survived at concentration of 1000μg/ml, 100μg/ml and 10μg/ml respectively with LD50; 215.837. Similarly 21 (70%), 25 (83%), 29 (96%) larvae were survived of dichloromethane plant extract with LD50; 6170.64. The methanol and dichloromethane extract exhibited 10.50±0.18% and 41.51±0.15% α-chymotrypsin enzyme inhibition respectively with IC50 values of greater than 500 μmol. The methanol extract showed 24.39±0.21% Urease enzyme inhibition with IC50 values of greater than 400 μmol. While dichloromethane extract has 11.46±0.09% enzyme inhibition with IC50 values of greater than 500 μmol. Conclusion: The results clearly indicated that Heliotropium dasycarpum has cytotoxic potential and enzyme inhibition properties. Further study is needed to screen out antitumor and anti-ulcerative agents

Immunomodulatory, antiglycation and anti-ulcerative properties of Ruellia squarrosa Fenzl Acanthaceae

Purpose: To evaluate the immunomodulatory, antiglycation and anti-ulcerative properties of Ruellia squarrosa Fenzl. Acanthaceae.Methods: Aerial parts and roots of Ruellia squarrosa were collected and extracted by maceration using dichloromethane and methanol as solvents. Luminol-enhanced chemiluminescence assay was used to evaluate immunomodulatory activity while antiglycation assay was performed by fluorescence method with rutin as standard. Anti-ulcerative activity was evaluated by enzymatic methods, namely, urease inhibition and carbonic anhydrase inhibition assays.Results: Dichloromethane extract showed immunomodulatory activity with half-maximal inhibitory concentration (IC50) of 39.48 ± 8.06 % using ibuprofen as standard and antiglycation effect (IC50 = 382.21 ± 3.43) using rutin as standard. The methanol extract of the aerial parts of the plant showed urease inhibition activity (IC50 = 130.2 ± 0.57) using thiourea as standard. The methanol extract of the aerial parts of the plant also showed carbonic anhydrase inhibition activity (IC50 = 1656.7 ± 0.08) using acetazolamide as standard.Conclusion: It was concluded from the present study that aerial and root extracts of the Ruellia squarrosa have significant immunomodulatory, antiglycation and anti-ulcerative properties.Keywords: Ruellia squarrosa, Immunomodulatory, Antiglycation, Anti-ulcerative activity, Carbonic anhydrase inhibition, Ureas

BIOLOGICAL SCREENING OF ARAUCARIA COLUMNARIS

Objective: The present research is biological screening of aerial part of Araucaria columnaris (Araucariaceae). There were investigation for their antibacterial, antifungal, phytotoxic and cytotoxic activities of Dichloromethane and methanol extract.Methods: Anti-bacterial, Anti-fungal, cytotoxicity and phytotoxicity activity was performed by Disc diffusion method, Agar tube dilution assay, Brine Shrimp Lethality bioassay and Lemna bioassay respectively.Results: Dichloromethane and methanolic extract exhibited significant phytotoxicity against Lemna minor having Paraquat as standard drug and incubation condition (28±1 °C). None of extracts presented any significant antibacterial and cytotoxic activity having Imipenum and Etoposide as standard drug respectively. Both extract had non-significant antifungal activity but it has been noted that MeOH and DCM extract of Araucaria columnaris showed 10% and 20% inhibition with linear growth at 90 mm and 80 mm respectively, when compared with control; against Fusarium solani and Aspergillus flavus respectively.Conclusion: Araucaria columnaris exhibited significant phytotoxicity bioassay. The phytotoxicty assay is a useful primary screen for weedicide research. Synthetic weedicides are expensive, toxic and non-specific. This study will help to discover the phytotoxic constituents of the plant by isolation, purification and structure elucidation to find out as effective herbicidal.Â

Antipyretic, analgesic and anti-inflammatory activities of methanol extract of root bark of Acacia jacquemontii Benth (Fabaceae) in experimental animals

Purpose: To investigate the ethnomedicinal claims regarding the use of Acacia jacquemontii Benth. (Fabaceae) in fever, pain and inflammation.Methods: The methanol root bark extract (AJRBM) of the plant was used in the studies. Preliminary phytochemical screening of the extract was carried out according to established methods. Analgesic, anti-inflammatory and antipyretic activities were evaluated using acetic acid-induced writhing, carrageennan-induced rat paw edema and Brewer’s yeast-induced pyrexia models, respectively. The extract was administered at doses of 50 and 100 mg/kg. Aspirin (300 mg/kg, p.o.) was used as a reference drug in all models. Normal saline (10 mL/kg p.o.) was used as negative control.Results: Phytochemical screening results indicate the presence of cardioactive glycosides, tannins, flavonoids and saponins. In the acetic acid-induced writhing model, the methanol extract exhibited significant (p < 0.05) analgesic effect with 58.98 % reduction in writhing response at a dose of 100 mg/kg, compared with untreated control group. The extract significantly (p < 0.05) reduced carrageenan-induced edema at doses of 50 and 100 mg/kg to 36.84 and 47.36 %, respectively, after 1h of extract administration. The extract exhibited predominantly dose-dependent antipyretic effect in Brewer’s yeast-induced pyrexia model. Maximum reduction in body temperature to 37.07 and 38.29 ºC at doses of 50 and 100 mg/kg, respectively, was observed, compared with untreated group (38.90 ºC) after 1 h, but this was not significant (p < 0.05).Conclusion: The plant extract exerts inhibitory effect on peripheral pain stimuli, edema and dosedependent anti-pyrexia, and thus justifies the ethnomedicinal use of Acacia jacquemontii Benth. in the management of pain, fever and inflammation.Keywords: Acacia jacquemontii, Antipyretic, Analgesic, Anti-inflammator