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   2011| July-September  | Volume 3 | Issue 3  
    Online since September 16, 2011

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Antioxidant, cytotoxic, antitumor, and protective DNA damage metabolites from the red sea brown alga Sargassum sp
Seif-Eldin N Ayyad, Saleh T Ezmirly, Salim A Basaif, Walied M Alarif, Adel F Badria, Farid A Badria
July-September 2011, 3(3):160-165
DOI:10.4103/0974-8490.85000  PMID:22022163
Background: Macroalgae can be viewed as a potential antioxidant and anti-inflammatory sources owing to their capability of producing compounds for its protection from environmental factors such as heat, pollution, stress, oxygen concentration, and UV radiations. Objective: To isolate major compounds which are mainly responsible for the pharmacological activity of brown alga under investigation, Sargassum sp. Materials and Methods: Algal material was air dried, extracted with a mixture of organic solvents, and fractionated with different adsorbents. The structures of obtained pure compounds were elucidated with different spectroscopic techniques, and two pure materials were tested for protection of DNA from damage, antioxidant, antitumor, and cytotoxicity. Results: Four pure compounds were obtained, of which fucosterol (1) and fucoxanthin (4) were tested; it was found that fucoxanthin has strong antioxidant and cytotoxicity against breast cancer (MCF-7) with IC 50 = 11.5 ΅g/ml. Conclusion: The naturally highly conjugated safe compound fucoxanthin could be used as antioxidant and as an antitumor compound.
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Anthocyanins from bilberry (Vaccinium myrtillus L.) alleviate pruritus in a mouse model of chronic allergic contact dermatitis
Katsunori Yamaura, Maki Shimada, Koichi Ueno
July-September 2011, 3(3):173-177
DOI:10.4103/0974-8490.85002  PMID:22022165
Background: Bilberry (Vaccinium myrtillus L.) is one of the richest sources of anthocyanins which are known to have anticancer, wound healing and anti-allergic effects. Here, we examined whether bilberry extract (Bilberon-25) alleviates pruritus in a mouse model of chronic allergic contact dermatitis. Materials and Methods: BALB/c mice with chronic allergic contact dermatitis induced by 3 weeks of repeated application of 2,4,6-trinitro-1-chlorobenzene (TNCB) were administered Bilberon-25 orally for 3 weeks after sensitization with TNCB. The effects of Bilberon-25 on pruritus and inflammation were evaluated by measurement of scratching behaviour and ear swelling, respectively. Results: Treatment with Bilberon-25 significantly attenuated the TNCB-induced increase in scratching behaviour, but dexamethasone did not. In contrast, ear swelling was ameliorated by dexamethasone treatment, and significantly decreased by Bilberon-25. Repeated application of TNCB induced a shift in the cutaneous cytokine milieu from a T helper cell type (Th)1 to a Th2 profile; Bilberon-25 and dexamethasone alleviated this Th2 predominance of the lesional skin. Conclusion: Anthocyanins from bilberry might be beneficial for the treatment of chronic pruritus which can occur in patients with inflammatory skin diseases such as atopic dermatitis.
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Combined effects of p-coumaric acid and naringenin against doxorubicin-induced cardiotoxicity in rats
Shruti S Shiromwar, Vijay R Chidrawar
July-September 2011, 3(3):214-219
DOI:10.4103/0974-8490.85012  PMID:22022172
Background: Doxorubicin (DOX) is the most active cytotoxic agents having efficacy in malignancies either alone or combined with other cytocidal agents. The clinical usefulness of the anthracycline drug has been precluded by cardiac toxicity. Many therapeutic interventions have been attempted to improve the therapeutic benefits of the drug. This study is based on the possible protective effects of combination of p-coumaric acid (PC) and naringenin (NR) on DOX induced cardiac toxicity in male Swiss albino rats. Methods: Total nine groups of Swiss albino rats were used, Group I (vehicle control) receive saline solution daily and Group II (disease control) receive saline solution daily up to 29 th day and at 30 th day a single dose of DOX (15 mg/kg i.p.) is given. PC alone (100 mg/kg/day p.o.) and (200 mg/kg/day p.o.) also NR alone (15 mg/kg/day) orally administer for 30 days. Similarly a standard drug Vit. E (100 mg/kg/day) administers alone for 30 days. Group PC/DOX and PC and NR/DOX receive PC (200 mg/kg/day) and combine PC (200 mg/kg/day).Results: Doxorubicin induced marked biochemical alterations characteristic of cardiac toxicity including increase in MDA level and decrease SOD, CAT & GSH level but prior administration of combination of PC & NR ahead of doxorubicin challenge ameliorated all these biochemical markers. Conclusion: The study proves the beneficial effects of combination of PC and NR in protecting animal against DOX induced cardiotoxicity.
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Antihistaminic activity of aqueous extract of stem bark of Ailanthus excelsa Roxb.
Dinesh Kumar, ZA Bhat, P Singh, SS Bhujbal, RS Deoda
July-September 2011, 3(3):220-224
DOI:10.4103/0974-8490.85014  PMID:22022173
Background: Biologically active compounds from natural sources are of interest as possible new drugs for different diseases. Over many centuries humans have been mining the bounties of nature for discovering natural products that have been used for the treatment of all human diseases. Ailanthus excelsa Roxb. (Simaroubaceae) is widely used in the Indian system of medicine as an antiasthmatic, antispasmodic, bronchodilator, anticolic pain, anticancer, antidiabetic etc. The plant was also reported for its antiasthmatic, bronchodilatory, antiallegic and many more such activities. Objective: To evaluate the antihistaminic activity of aqueous extract of stem bark of Ailanthus excelsa Roxb. Materials and Methods: We have studied the effect of aqueous extract of stem barks of A. excelsa Roxb. at a doses 100 μg/mL in the isolated goat tracheal chain preparation in vitro and 100, 200, 400 mg/kg doses orally in passive paw anaphylaxis in rat, clonidine-induced catalepsy in mice models in vivo for its antihistaminic activity. Results: Aqueous extract of stem barks of A. excelsa Roxb. significantly (***P<0.001) inhibits the percentage contraction at concentration of 100 μg/mL in goat tracheal chain preparation. A. excelsa Roxb. extract (100, 200, and 400 mg/kg oral) and dexamethasone (0.5 mg/kg, i.p.) also significantly reduced (**P<0.01) the paw volume at fourth hour and the percentage inhibition was found to be 13.98%, 28.49%, 42.47% and 46.77% respectively. The aqueous extract of stem barks of A. excelsa Roxb. (100, 200, 400 mg/kg, p.o.) and chlorpheniramine maleate (10 mg/kg, i.p.) significantly inhibited (*P<0.05, **P< 0.01) clonidine-induced catalepsy in mice at 150 min after the administration of clonidine. Conclusion: The aqueous extract of stem bark of A. excelsa Roxb. possess significant antihistaminic activity (H1-antagonist) and can be attributed to bronchodilating, anti-inflammatory, adaptogenic activity etc. Hence detailed study needs to be conducted to evaluate the phytoconstituent responsible for the above mentioned results and their clinical efficacy in the treatment of related diseases.
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Neuropharmacological activity of Lippia nodiflora Linn.
Kumaresan P Thirupathy, Asish Tulshkar, C Vijaya
July-September 2011, 3(3):194-200
DOI:10.4103/0974-8490.85007  PMID:22022169
Introduction: In the recent years, plants containing flavonoids have gained much more interest in research area, as they are found to be specific ligands for benzodiazepine receptors. Material and Methods: In our investigation, we evaluated the neuropharmacological profile of petroleum, chloroform and ethanolic extracts of aerial part of Lippia nodiflora Linn. With experimental models using test such as potentiation of diazepam-induced sleeping time, locomotor activity, motor coordination, exploratory behavior pattern, elevated plus maze and maximal electroshock convulsions. Diazepam at doses of 5, 4, and 1 mg/kg served as standard. Results: Results showed that the ethanolic extract of L. nodifl ora at both doses (250 and 500 mg/kg p.o.) and its chloroform extract at a higher dose of 500 mg/kg produced central inhibitory (sedative) effects, anticonvulsant effect and anxiolytic effect in mice. Values were statistically significant (P < 0.05 and P < 0.01) when compared to the control group. The petroleum ether extract of plant at both dose levels (250 and 500 mg/kg p.o.) did not produce any central effects. Conclusion: In conclusion, we can say that the ethanolic and chloroform extracts showed the central inhibitory activity due to the presence of fl avonoids and this fact was also supported by the finding that the petroleum ether extract did not show any central effect and flavonoids were not found in it.
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Antianaphylactic and mast cell stabilization activity of Strychnos potatorum Linn. seed
Umesh Jayantarao Patil, Anil Sidram Savali, Manjunath C Jirankali
July-September 2011, 3(3):208-213
DOI:10.4103/0974-8490.85011  PMID:22022171
Aim: The antianaphylactic activity of Strychnos potatorum Linn seed extract was evaluated by using compound 48/80 induced anaphylaxis and mast cell stabilization was studied by using peritoneal mast cells of rats. The possible antianaphylactic and mast cell stabilization mechanism was evaluated by using compound 48/80 induced mast cell activation and level of nitric oxide in rat peritoneal mast cells. Materials and Methods: Anaphylactic shock in mice was induced by the intraperitoneal administration of 8 mg/kg compound 48/80, prior to induction of anaphylaxis the animals were treated with S. potatorum Linn. seed extract administered orally 1 h before administration of compound 48/80, the rate mortality was observed in each group of animals. Mast cell stabilization was seen by preincubation of mast cells with the compound 48/80 and the extracts. Results: This study indicates that the chloroform, petroleum ether, and methanolic extracts were shown potent and has significant (P < 0.01 and P < 0.001) inhibitory effects on compound 48/80 induced anaphylactic reaction and mast cell activation. This compound also inhibited significantly compound 48/80 induced increased level of nitric oxide in rat peritoneal mast cells. Conclusion: We conclude from this study that the different extracts of S. potatorum seed have potent antianaphylactic activity through mast cell stabilization and inhibition of nitric oxide synthesis. The inhibitory effect of S. potatorum Linn. on release of histamine and nitric oxide protects from compound 48/80 induced anaphylactic reaction may be through blocking vasodilatation, decrease vascular resistance, hypotension and tachycardia induced by immunogenic agent used in this study.
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Antibacterial, anti-inflammatory, and antioxidant effects of the leaves and stem bark of Glyphaea brevis (Spreng) Monachino (Tiliaceae): A comparative study
RA Dickson, E Ekuadzi, K Annan, G Komlaga
July-September 2011, 3(3):166-172
DOI:10.4103/0974-8490.85001  PMID:22022164
Background: Glyphaea brevis (Spreng) Monachino (Tiliaceae) have traditional uses in the management of conditions characterized by infections, inflammatory disorders and oxidative stress. The paper aims to report the comparative data on the leaves and stem bark of Glyphaea brevis with respect to their antibacterial, anti-inflammatory and antioxidant effects. Materials and Methods: The antibacterial effects of the 70% ethanol extracts of the leaves and stem bark were determined using the agar well diffusion and micro dilution assays. The anti-inflammatory activity was assessed using the carrageenan-induced oedema model in 7-day old cockerels. Using the DPPH free radical scavenging, total antioxidant and total phenol content assays, the antioxidant potential of the extract was assessed. Results: The bark extract had the higher antibacterial effect against 6 of the 8 microorganisms used. Noteworthy are its activity against Bacillus subtilis and Enterococcus faecalis with lowest MIC value of 500 ΅g/mL respectively. In doses of 30, 100 and 300 mg/kg, both extracts reduced the carrageenan-induced oedema in 7-day old cockerels. Based on the ED 50 values, both extracts demonstrated similar potencies (ED 50 =21.00 mg/kg). The stem bark extract exhibited higher free radical scavenging activity (IC 50 = 1.392 mg/mL) compared to the leaf extract (IC 50 = 9.509 mg/mL). In the total phenol content, the bark extract showed higher content (15.91 mg/g of dry mass) compared to the leaf extract (2.68 mg/g dry mass). Both extracts demonstrated equal potencies in the total antioxidant capacity determinations (0.60 mg/g dry weight of extract). Conclusions: The results of this work provide scientific evidence for the traditional uses of Glyphaea brevis.
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Isolation and identification of a new flavonoid glycoside from Carrichtera annua L. seeds
Abdelaaty A Shahat, Khaled A Abdelshafeek, Husseiny A Husseiny
July-September 2011, 3(3):151-154
DOI:10.4103/0974-8490.84998  PMID:22022161
Background: Flavonoids are a major group of constituents and are assumed to be among the beneficial components. Recently, they have also received considerable interest as components of foodstuffs and nutraceuticals because of their antioxidant and anticancer properties. Materials and Methods: About 500 g of air-dried powdered seeds of C. annua were defatted seeds and extracted with 70% methanol. The combined methanol extract was partitioned with chloroform and n-butanol. The butanol extract was concentrated and subjected to column chromatography on polyamide. Results: The fraction eluted with aqueous methanol (40% and 50%) was found to contain three main flavonoids (1, 2, and 3). Repeated column chromatography on polyamide and Sephadex LH-20 gave compound 1. Compounds 2 and 3 were further purified using preparative paper chromatography with 20% HOAc and Sephadex LH-20 column. Conclusions: Reinvestigation of the flavonoidal constituents of the butanol fraction of the aqueous methanolic extract of Carrichteraannua seeds led to isolation and identification of a new flavonoidal glycosidenamed as quercetin 3-O-[(6-sinapoyl-b-glucopyranosyl)-(1;2)-b-arabinopyranosyl]-7-O-b-glucopyranoside 1, in addition to, quarecetin-3-O-glucoside 2, isorhamnetin-3-O-b-runtinoside3, and isorhamnetin4.Structures of the isolated compounds were established by UV, MS, and 1 H and 13 C NMR.
  2 3,538 60
Extract from peel of Citrus natsudaidai alleviates experimental chronic allergic dermatitis in mice
Noriyuki Nakayama, Katsunori Yamaura, Maki Shimada, Koichi Ueno
July-September 2011, 3(3):155-159
DOI:10.4103/0974-8490.84999  PMID:22022162
Background: Citrus natsudaidai (natsumikan) is a typical citrus fruit containing several antioxidative nutrients which are found in higher concentration in the peel than in the pulp of the fruit. In this study, we examined whether extract from immature natsumikan peel prevents development of chronic allergic dermatitis in mice. Materials and Methods: Chronic allergic dermatitis was induced by repeated application of 2, 4, 6-trinitro-1-chlorobenzene in BALB/c mice and natsumikan was administrated orally for 30 days. Ear swelling and dermatitis score were measured after each challenge. The level of derivative-reactive oxygen metabolites (d-ROM) in serum was measured on day 30. Results: Treatment of natsumikan significantly attenuated the increase in ear swelling and improved dermatitis scores. In addition, increases in serum d-ROM were attenuated by a treatment of natsumikan. Although the routine treatment with dexamethasone resulted in a clear and significant reduction in body weight, natsumikan treatment did not have such effects. Conclusion: Immature natsumikan peel is beneficial for the treatment of chronic allergic dermatitis.
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Standardised herbal extract of chlorogenic acid from leaves of Etlingera elatior (Zingiberaceae)
Eric W.C Chan, Yau Yan Lim, Shiau Pin Tan
July-September 2011, 3(3):178-184
DOI:10.4103/0974-8490.85003  PMID:22022166
Background: Chlorogenic acid (CGA) or 5-caffeoylquinic acid, was found to be the dominant phenolic compound in leaves of Etlingera elatior (Zingiberaceae). The CGA content of E. elatior leaves was significantly higher than flowers of Lonicera japonica (honeysuckle), the commercial source. In this study, a protocol to produce a standardised herbal CGA extract from leaves of E. elatior using column chromatography was developed. Materials and Methods: Freeze-dried leaves of E. elatior were extracted with 30% ethanol, and sequentially fractionated using Diaion HP-20 and Sephadex LH-20. Results: The CGA fractions, which yielded extracts of 10% and 40% w/w purity, possessed antioxidant, tyrosinase inhibition, and antibacterial properties. The entire fractionation process took only 6.5 hours, using gravity flow. From 50 g of leaves, the final yield of CGA extract was 0.2 g (0.4%). The CGA content of the standardised herbal extract from leaves of E. elatior (40%) is 1.6 times that of commercial extracts from honeysuckle flowers (25%). Conclusion: With high CGA content, the standardised herbal extract has a great potential to be developed into functional food and other health products. Leaves of E. elatior, which currently have no economic value, could serve as an alternative source of CGA. Leaves are large, available in abundance, and harvesting is non-destructive to the plants.
  2 4,145 42
Acaricidal effect of an isolate from Hoslundia opposita vahl against Amblyomma variegatum (Acari: Ixodidae)
Kofi Annan, Nora Jackson, Rita A Dickson, George H Sam, Gustav Komlaga
July-September 2011, 3(3):185-188
DOI:10.4103/0974-8490.85004  PMID:22022167
Background: Hoslundia opposita Vahl. (Lamiaceae), a common local shrub in Ghana, is traditionally known not only for its pharmacological benefits but also for its insecticidal properties. Its acaricidal property, however, has not been investigated. Objective: To test the acaricidal effects of the crude extract and fractions of H. opposita leaves as well as to isolate and characterize the acaricidal principles. Materials and Methods: The crude methanolic extract, pet. ether, ethyl acetate and aqueous fractions of the leaves of H. opposita were tested against the larvae of the cattle tick, Amblyomma variegatum, using the Larval Packet Test. A bioassay-guided isolation was carried out to identify the acaricidal principle obtained from the ethyl acetate fraction. Results: The active principle was characterised as ursolic acid, a triterpene previously isolated from the leaves of the same plant. The extract and fractions were less potent than the control, malathion (LC 50 1.14 Χ 10 -4 mg/ml). Among the plant samples however the crude methanolic extract exhibited the highest effect against the larvae (LC 50 5.74 Χ 10 -2 mg/ml), followed by the ethyl acetate fraction (LC 50 8.10 Χ 10 -2 mg/ml). Ursolic acid, pet. ether and aqueous fractions however showed weak acaricidal effects with LC 50 values of 1.13 mg/ml, 8.96 Χ 10 -1 mg/ml and 1.44 mg/ml, respectively. Conclusion: Ursolic acid was not as potent as the crude methanolic extract and the ethyl acetate fraction from which it was isolated. The overall acaricidal effect of H. opposita may have been due to synergy with other principles having acaricidal properties.
  2 2,728 32
Cucurbitacins-type triterpene with potent activity on mouse embryonic fibroblast from Cucumis prophetarum, cucurbitaceae
Seif-Eldin N Ayyad, Ahmed Abdel-Lateff, Salim A Basaif, Thomas Shier
July-September 2011, 3(3):189-193
DOI:10.4103/0974-8490.85006  PMID:22022168
Background: Higher plants are considered as a well-known source of the potent anticancer metabolites with diversity of chemical structures. For instance, taxol is an amazing diterpene alkaloid had been lunched since 1990. Objective: To isolate the major compounds from the fruit extract of Cucumis prophetarum, Cucurbitaceae, which are mainly responsible for the bioactivities as anticancer. Materials and Methods: Plant material was shady air dried, extracted with equal volume of chloroform/methanol, and fractionated with different adsorbents. The structures of obtained pure compounds were elucidated with different spectroscopic techniques employing 1D ( 1 H and 13 C) and 2D (COSY, HMQC and HMBC) NMR (Nuclear Magnetic Resonance Spectrometry) and ESI-MS (Eelectrospray Ionization Mass Spectrometry) spectroscopy. The pure isolates were tested towards human cancer cell lines, mouse embryonic fibroblast (NIH3T3) and virally transformed form (KA3IT). Results: Two cucurbitacins derivatives, dihydocucurbitacin B (1) and cucurbitacin B (2), had been obtained. Compounds 1 and 2 showed potent inhibitory activities toward NIH3T3 and KA31T with IC 50 0.2, 0.15, 2.5 and 2.0 μg/ml, respectively. Conclusion: The naturally cucurbitacin derivatives (dihydocucurbitacin B and cucurbitacin B) showed potent activities towards NIH3T3 and KA31T, could be considered as a lead of discovering a new anticancer natural drug.
  2 2,885 35
Pharmacognosy Research - Indexed on PubMed Central
Ambrose Furey
July-September 2011, 3(3):149-150
DOI:10.4103/0974-8490.84997  PMID:22022160
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Amelioration of nitrobenzene-induced nephrotoxicity by the ethanol extract of the herb Euphorbia hirta
Subramanian Suganya, Dominic Sophia, Chinthamony Arul Raj, Muthaiyan Ahalliya Rathi, Lakshmanan Thirumoorthi, Periyasamy Meenakshi, Dugganaboyana Guru Kumar, Velliyur Kanniyapan Gopalakrishnan
July-September 2011, 3(3):201-207
DOI:10.4103/0974-8490.85009  PMID:22022170
Background: Euphorbia hirta (L.) (Euphorbiaceae) is a very popular herb amongst practitioners of traditional medicine and used in the treatment of female disorders, respiratory ailments, tumors, jaundice, digestive problems, wounds, etc. We aimed to evaluate the protective effect of E. hirta against nitrobenzene-induced nephrotoxicity in albino rats. Materials and Methods: The nephroprotective activity of the ethanol extract of E. hirta (400 mg/kg body weight) was studied in nitrobenzene-induced albino rats (1000 mg/kg body weight). The activities of antioxidant enzymes superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione-S-transferase (GST), and the levels of reduced glutathione (GSH), total thiols and vitamin C in the kidney tissues were determined. Histopathologic investigation was performed in the kidney tissue samples. Results: Nitrobenzene administration significantly (P < 0.01) enhanced the lipid peroxidation and significantly (P < 0.05) depleted the levels of SOD, CAT, GPx, GST, GSH, total thiols and vitamin C. Treatment with the ethanol extract of E. hirta significantly normalized the antioxidant levels. The nephroprotective activity was also supported by histopathologic studies of kidney tissue. Conclusion: The results indicate that the ethanol extract of E. hirta ameliorates renal dysfunction and could be used as an effective protector against nitrobenzene-induced nephrotoxicity, primarily through its antioxidant capacity.
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