An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO 3 and poloxamer 188

Hong-mei Yan, Zhen-hai Zhang, Yan-rong Jiang, Dong-mei Ding, E. Sun, Xiao-bin Jia

Pharmacognosy Magazine 2014 10(38):311-317

Background: Tanshinone IIA (TSIIA) on solid dispersions (SDs) has thermodynamical instability of amorphous drug. Ternary solid dispersions (tSDs) can extend the stability of the amorphous form of drug. Poloxamer 188 was used as a SD carrier. Nano-CaCO 3 played an important role in adsorption of biomolecules and is being developed for a host of biotechnological applications. Objective: The aim of the present study was to investigate the dissolution behavior and accelerated stability of TSIIA on solid dispersions (SDs) by the use of ternary systems with nano-CaCO 3 and poloxamer 188. Materials and Methods: The TSIIA tSDs were prepared by a spray-drying method. First, the effect of combination of poloxamer 188 and nano-CaCO 3 on TSIIA dissolution was studied. Subsequently, a set of complementary techniques (DSC, XRPD, SEM and FTIR) was used to monitor the physical changes of TSIIA in the SDs. Finally, stability test was carried out under the conditions 40°C/75% RH for 6 months. Results: The characterization of tSDs by differential scanning calorimetry analysis (DSC) and X-ray powder diffraction (XRPD) showed that TSIIA was present in its amorphous form. Fourier transforms infrared spectroscopy (FTIR) suggested the presence of interactions between TSIIA and carriers in tSDs. Improvement in the dissolution rate was observed for all SDs. The stability study conducted on SDs with nano-CaCO 3 showed stable drug content and dissolution behavior, over the period of 6 months as compared with freshly prepared SDs. Conclusion: SDs preparation with nano-CaCO 3 and poloxamer 188 may be a promising approach to enhance the dissolution and stability of TSIIA.

Cytotoxicity of gypsogenic acid isolated from Gypsophila trichotoma

Ilina Krasteva, Maya Yotova, Deyan Yosifov, Niko Benbassat, Kristina Jenett-Siems, Spiro Konstantinov

Pharmacognosy Magazine 2014 10(38):430-433

Background: Gypsophila trichotoma Wend. (Caryophyllaceae) is a medicinal plant which is protected in Bulgaria by the Biodiversity Law. Previous studies have showed the presence of triterpene saponins, sterols, flavonoids, triterpens, etc. Objective: Gypsogenic acid, isolated from Gypsophila trichotoma roots, was evaluated for cytotoxic activity. Materials and Methods: The structure of the compound was elucidated by spectral methods. The cell survival fraction was determined by the MTT dye reduction assay, performed with some modifications. Results: Gypsogenic acid was tested in a panel of human tumor cell lines and was found to inhibit the proliferation of malignant cells. It was active against leukemic cells with lymphoid (SKW-3 and BV-173) or myeloid phenotype (HL-60, K-562, and LAMA-84), as well as against the EJ bladder carcinoma cell line. Bcr-Abl expressing myeloid cells (LAMA-84 and especially K-562) displayed lower sensitivity. HL-60/Dox cells were less sensitive to gypsogenic acid than the parent cell line, which shows that gypsogenic acid is probably a substrate of MRP-1.

Luteolin, a bioflavonoid inhibits azoxymethane-induced colon carcinogenesis: Involvement of iNOS and COX-2

Ashok Kumar Pandurangan, Suresh Kumar, Prakash Dharmalingam, Sudhandiran Ganapasam

Pharmacognosy Magazine 2014 10(38):306-310

Colon cancer (CRC) is a serious health problem through worldwide. Development of novel drug without side effect for this cancer was crucial. Luteolin (LUT), a bioflavonoid has many beneficial effects such as antioxidant, anti-inflammatory, anti-proliferative properties. Azoxymethane (AOM), a derivative of 1, 2-Dimethyl hydrazine (DMH) was used for the induction of CRC in Balb/C mice. CRC was induced by intraperitoneal injection of AOM to mice at the dose of 15 mg/body kg weight for 3 weeks. Mouse was treated with LUT at the dose of 1.2 mg/body kg weight orally until end of the experiment. The expression of inducible nitric oxide synthase (iNOS) and cyclooxygense (COX)-2 were analyzed by RT-PCR and immunohistochemistry. The expressions of iNOS and COX-2 were increased in the case of AOM induction. Administration of LUT effectively reduced the expressions of iNOS and COX-2. The present study revealed that, LUT suppresses both iNOS and COX-2 expressions and act as an anti-inflammatory role against CRC.

Anti-tumor activity of safranal against neuroblastoma cells

Saeed Samarghandian, Mohammad Ebrahim Shoshtari, Javad Sargolzaei, Hosna Hossinimoghadam, Jabbari Azad Farahzad

Pharmacognosy Magazine 2014 10(38):419-424

Objective: Safranal (2,6,6-trimethyl-1,3-cyclohexadiene-1-carboxaldehyde, C10H14O) is an active ingredient in the saffron, which is used in traditional medicine, and also, the biological activity of saffron in anti-cancer is in development. It has been reported to have anti-oxidant effects, but its anti-tumor effects remain uncertain. The aim of this study was to evaluate effects of safranal on anti-tumor on neuroblastoma cells. Materials and Methods: Neuroblastoma cells were cultured and exposed to safranal (0, 10, 15, 20, 50 μg/ml). Cell proliferation was examined using the 3-(4, 5-dimethyl thiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay. Apoptotic cells, cell cycle distribution, and sub-G1 fraction were analyzed using flow cytometric analysis after propidium iodide staining. Results: Safranal inhibited the growth of malignant cells in a dose-and time-dependent manner. The IC (50) values against the neuroblastoma cell line were determined as 11.1 and 23.3 μg/ml after 24 and 48 h, respectively. Safranal induced a sub-G1 peak in the flow cytometry histogram of treated cells compared to control cells indicating that apoptotic cell death is involved in safranal toxicity. Conclusions: Our pre-clinical study demonstrated a neuroblastoma cell line to be highly sensitive to safranal-mediated growth inhibition and apoptotic cell death. Although the molecular mechanisms of safranal action are not yet clearly understood, it appears to have potential as a therapeutic agent.

Efficacy of Acorus calamus on collagen maturation on full thickness cutaneous wounds in rats

Thangavel Ponrasu, Karuppanan Natarajan Madhukumar, Moorthy Ganeshkumar, Kuttalam Iyappan, Vilvanathan Sangeethapriya, Vinaya Subramani Gayathri, Lonchin Suguna

Pharmacognosy Magazine 2014 10(38):299-305

Background: The rhizomes of Acorus calamus and their essential oil are widely used in the flavoring industry and production of alcoholic beverages in Europe. Recent reports have confirmed the presence of several pharmacological components in the rhizomes of A. calamus. Objective: The objective of this study was to find out the efficacy of topical administration of ethanolic extract of A. calamus on dermal wound healing in rats. Wound healing is a natural process occurring in living organisms, which results in a complete or partial remodeling of injured tissue and ultimately progresses to the formation of a fibrous scar. Several natural products have been reported to augment the wound healing process. Materials and Methods: An ethanolic extract of A. calamus was prepared and its wound-healing efficacy was studied. An excision wound was made on the back of the rat and 200 μL (40 mg/kg body weight) of the A. calamus extract was applied topically once daily for the treated wounds. The control wounds were treated with 200 μL of phosphate buffered saline. Results: The granulation tissues formed were removed at 4, 8 and 12 days and biochemical parameters such as deoxyribonucleic acid, total protein, total collagen, hexosamine and uronic acids were measured. The amount of type I/III collagen formed in control and treated wound tissues was evaluated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The epithelialization time, tensile strength and histological examination of the wounds were also studied. Biochemical analyses of the granulation tissues revealed a significant increase in collagen, hexosamine and uronic acid when compared with the control. The tensile strength of extract treated wounds was found to increase by 112%. A significant reduction in lipid peroxide levels suggested that A. calamus possesses antioxidant components. Conclusions: The results strongly confirm the beneficial effects of A. calamus in augmenting the wound healing process.

In Vivo skin hydration and anti-erythema effects of Aloe vera, Aloe ferox and Aloe marlothii gel materials after single and multiple applications

Lizelle T Fox, Jeanetta du Plessis, Minja Gerber, Sterna van Zyl, Banie Boneschans, Josias H Hamman

Pharmacognosy Magazine 2014 10(38):392-403

Objective: To investigate the skin hydrating and anti-erythema activity of gel materials from Aloe marlothii A. Berger and A. ferox Mill. in comparison to that of Aloe barbadensis Miller (Aloe vera) in healthy human volunteers. Materials and Methods: Aqueous solutions of the polisaccharidic fractions of the selected aloe leaf gel materials were applied to the volar forearm skin of female subjects. The hydration effect of the aloe gel materials were measured with a Corneometer ® CM 825, Visioscan ® VC 98 and Cutometer ® dual MPA 580 after single and multiple applications. The Mexameter ® MX 18 was used to determine the anti-erythema effects of the aloe material solutions on irritated skin areas. Results: The A. vera and A. marlothii gel materials hydrated the skin after a single application, whereas the A. ferox gel material showed dehydration effects compared to the placebo. After multiple applications all the aloe materials exhibited dehydration effects on the skin. Mexameter ® readings showed that A. vera and A. ferox have anti-erythema activity similar to that of the positive control group (i.e. hydrocortisone gel) after 6 days of treatment. Conclusion: The polysaccharide component of the gel materials from selected aloe species has a dehydrating effect on the skin after multiple applications. Both A. vera and A. ferox gel materials showed potential to reduce erythema on the skin similar to that of hydrocortisone gel.

Screening of siddha medicinal plants for its in-vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity

Madhuri Kadiyala, Sivasankaran Ponnusankar, Kannan Elango

Pharmacognosy Magazine 2014 10(38):294-298

Background: The plants selected for the study were traditionally used in siddha system of medicine in neurological disorders. Aim: The aim of the following study isto screen the plant species for both acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) inhibition by in-vitro Ellman's method and a thin layer chromatography bioautographic assay for newer drug candidates for the treatment of Alzheimer's disease. Materials and Methods: Ellman's colorimetric method was performed in a 96 well micro plate for cholinesterases inhibition using galantamine as standard drug. Results: Present studies confirmed that out of all the tested extracts Hemidesmus indicus R.Br (HI) showed considerable IC 50 values for AchE (28.40 ± 0.92 μg/mL) and BuchE (43.47 ± 0.64 μg/mL) inhibition which indicates that HI extract has considerable specificity toward AchE and BuchE compared with all the tested extracts and the activity was followed by Vernonia anthelmintica (VA) Willd and Saussurea lappa Clarke (SL). The bioautograms also confirmed the activity potent extracts. Conclusion: Besides various bioactivities HI, VA and SL exhibited considerable cholinesterases inhibition making it to consider these species for further investigation of new compounds.

Anti-inflammatory effects of Cryptotympana atrataFabricius slough shed on contact dermatitis induced by dinitrofluorobenzene in mice

Miyoung Kim, Hanna Kim, Jeonghyun Ryu, Suzy Jo, Guemsan Lee, Mi Heon Ryu, Hyungwoo Kim, Su In Cho

Pharmacognosy Magazine 2014 10(38):377-382

Background: The slough shed of Cryptotympana atrata Fabricius is widely used to treat skin diseases in China, Japan, and Korea. Objective: To investigate the anti-inflammatory effects of C. atrata on contact dermatitis. Materials and Methods: We investigated the effects of C. atrata methanol extract (MECA) on ear swelling, histophathological changes and cytokine production in 1-fluoro-2,4-dinitrofluorobenzene (DNFB)-induced contact dermatitis (CD) mice. Results: Topical application of MECA effectively inhibited enlargement of ear swelling (30 and 100 &#956;/ear, P < 0.05; 300 &#956;g/ear, P < 0.01). MECA treatment also inhibited hyperplasia, spongiosis (100 and 300 &#956;g/ear, P < 0.001), and immune cell infiltration (30 &#956;g/ear, P < 0.05; 100 and 300 &#956;g/ear, P < 0.001) induced by DNFB. In addition, treatment with MECA suppressed the increase in the levels of TNF-&#945; (P < 0.05), IFN-g (3, 100 &#956;g/ear, P < 0.05; 300 &#956;g/ear, P < 0.01), and IL-6 (100 &#956;g/ear, P < 0.05; 300 &#956;g/ear, P < 0.01) production. Conclusion: These data suggest that MECA has the potential for use in the treatment of inflammatory skin diseases, including CD. Moreover, the results presented herein indicate that anti-inflammatory actions of MECA are mediated by decreasing production of TNF-&#945;, IFN-&#947;, and IL-6 in inflamed tissues.

Quantification of allicin by high performance liquid chromatography-ultraviolet analysis with effect of post-ultrasonic sound and microwave radiation on fresh garlic cloves

Sankhadip Bose, Bibek Laha, Subhasis Banerjee

Pharmacognosy Magazine 2014 10(38):288-293

Background: Garlic (Allium sativum L.) has been accepted universally to be applied in food, spice and traditional medicine. The medicinal and other beneficial properties of garlic are attributed to organosulfur compounds. Objective: As of today no simultaneous analysis has been performed; hence the transformation of allicin to its degraded products during cultivation and storage is open into doubt. Materials and Methods: In our present work, we have tried to develop a sensitive and reproducible analytical method to measure allicin by high performance liquid chromatography-ultraviolet analysis with effect of post-acoustic waves and microwave radiation on fresh garlic cloves. Results: The process revealed the effect of different radiation techniques on fresh garlic retains the principle component, allicin in its pure form and generated higher yield than the conventional way of extraction. Conclusion: Therefore, materializing these techniques in the pharmaceutical industry will definitely be proved beneficial in term of time as well as money. Most interestingly, the methods ruled out possibilities of degradation of organosulfur compounds as well.

Dietary supplementation of chloroquine with nigella sativa seed and oil extracts in the treatment of malaria induced in mice with plasmodium berghei

Promise Madu Emeka, Lorina Ineta Badger-Emeka, Chiamaka Maryann Eneh, Tahir Mahmood Khan

Pharmacognosy Magazine 2014 10(38):357-362

Background: The aim of the study was to investigate the effects of dietary combination of Nigella sativa seed and oil extracts with chloroquine (CQ), and how these combinations enhance CQ efficacy in mice infected with Plasmodium berghei and their survival rates. Materials and Methods: Chloroquine sensitive P. berghei, NK65 strain was used for the study. This was passaged intraperitoneally into albino mice with a 0.2ml standard inoculum consisting of 10 6 parasitized erythrocyte suspension in phosphate buffer solution (PBS). Parasitaemia was ascertained by microscopical examination of blood films under oil immersion at X100 magnification. Results: Nigella sativa seed in feed (NSSF), NSSF + CQ on day 4, produced 86.1% and 86.0% suppression respectively, while Nigella sativa oil extract in feed (NSOF) and in combination with CQ had 86.0% and 99.9% suppression respectively. The degree of suppression with the combination was significantly higher compared to CQ alone (P < 0.001) (36.1%). Complete parasitaemia clearance was obtained on the 20 th and 15 th day of treatment for NSSF, NSSF + CQ respectively, while that for NSOF and NSOF + CQ was on days 26 and 12 respectively. For CQ parasite clearance was 12 days with treatment. Also, the combinastion of 10 mg/kg Nigella sativa oil treatment injected intraperitoneally with oral CQ produced very significant parasite suppression (P < 0.0001) (93%). Survival rate in NSSF and NSOF and in combination with CQ groups was 100 and 60.0% for CQ alone. Conclusion : sThis study shows that the use of Nigella sativa seed and oil extract as dietary supplements in combination with CQ has a potential in enhancing the efficacy of CQ and could be of benefit in management of malaria.

Pharmacodynamic studies on the isolated active fraction of Acacia farnesiana (L.) willd

Bino Kingsley, Saminathan Kayarohanam, Pemaiah Brindha, Appian Subramoniam

Pharmacognosy Magazine 2014 10(38):283-287

Background: Acacia farnesiana is a medicinal plant that grows throughout tropical parts of Indian subcontinent, particularly in sandy soils of river beds in Northern India. The objective of the present study was to evaluate the anti-hyperglycemic activity of the extracts using glucose tolerance test. Isolation of an active fraction (AF) from the active extract (water extract) using alcohol precipitation and to get insight to the mechanism of action of the AF of A. farnesiana. Materials and Methods: Glucose uptake by isolated rat diaphragm of the AF was performed. Further the effect of release of Insulin from isolated and cultured pancreatic &#946;-cell was determined. Besides, effect of oral administration of the AF was compared with that of intraperitonial administration. The effect of AF on serum glucose levels in orally glucose loaded rats was compared with that of intraperitoneal glucose loaded rats. Results: The water extract significantly lowered the blood glucose level. When precipitated with alcohol, the activity was found in the soluble fraction. Glucose uptake in the isolated rat hemidiaphragm, was increased by the AF at 40 &#956;g/ml concentration, the AF did not significantly influence insulin release from cultured islets. The AF was found to be effective in orally glucose loaded in contrast to intraperitonial route. Conclusion: Our findings suggest that this plant is promising for further studies leading to the development of valuable medicine for diabetes.

Two novel antifungals, acornine 1 and acornine 2, from the bark of mangrove plant Aegiceras corniculatum (Linn.) Blanco from Sundarban Estuary

Vinod K. Gupta, Kalishankar Mukherjee, Amit Roy

Pharmacognosy Magazine 2014 10(38):342-349

Background: Microbes have been implicated in a wide variety of human diseases many of which are of life-threatening nature. New antimicrobials are urgently needed not only for combating these organisms but also to counter the menace of the harmful microbes developing resistance against drugs at alarming rates. Mangrove plants are rich sources of secondary metabolites having many beneficial biological activities including antimicrobial ones. True to this fact, this report describes identification, isolation and partial characterization of two novel antifungal compounds from Aegiceras corniculatum, a mangrove plant from Indian Sundarban estuary. Materials and Methods: Two compounds, named as Acornine 1 and Acornine 2, having antifungal activities were isolated from the bark of A. corniculatum, a mangrove plant, by using standard techniques. The compounds were characterized using routine microbiological and physicochemical methods. Results: Partial structural characterization of the two compounds indicated they are oleanane triterpenoids with linked sugar moieties. While both the compounds exhibited growth inhibition in tested Gram positive bacteria, Acornine 2 in particular demonstrated strong antifungal activities against several pathogenic fungi tested. Results also indicated that various environmental factors may govern the secondary metabolite profiles of the same mangrove plants growing in different geographical areas. Conclusion: Tissue extracts of Aegiceras corniculatum, a mangrove plant from Indian Sundarban estuary, exhibited the presence of remarkable antifungal activities. The isolated compounds responsible for such activities, named as Acornine 1 and Acornine 2, appear to have potential in food processing and health care industry. They need to be studied further.

Anti-cholinesterase activity of the standardized extract of Syzygium aromaticum L.

Manoj K. Dalai, Santanu Bhadra, Sushil K. Chaudhary, Arun Bandyopadhyay, Pulok K. Mukherjee

Pharmacognosy Magazine 2014 10(38):276-282

Background: Clove (Syzygium aromaticum) is a well-known culinary spice with strong aroma; contains a high amount of oil known as clove oil. The major phyto-constituent of the clove oil is eugenol. Clove and its oil possess various medicinal uses in indigenous medicine as an antiseptic, anti-oxidant, analgesic and neuroprotective properties. Thus, it draws much attention among researchers from pharmaceutical, food and cosmetic industries. Objective: The aim of the present study was to determine the anti-cholinesterase activity of the methanol extract of clove, its oil and eugenol. Materials and Methods: In vitro anti-cholinesterase activity of S. aromaticum was performed by a thin layer chromatography bio autography, 96 well micro titer plate and kinetic methods. Reverse phase high performance liquid chromatography (RP-HPLC) analysis was carried out to identify the biomarker compound eugenol in clove oil. Results: Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition study revealed that eugenol possess better inhibition of the enzymes than extract and oil. Clove extract, its oil and eugenol showed better inhibition of AChE than BChE. Polyphenolic compound eugenol was detected through RP-HPLC analysis. The content of eugenol in essential oil was found to be 0.5 &#956;g/ml. Kinetic analysis of the cholinesterase inhibition study of the extract; clove oil and eugenol have shown that they possess mixed type of inhibition for AChE and non-competitive type of inhibition for BChE. Conclusion: These results might be useful in explaining the effect of clove as anti-cholinesterase agent for the management of cognitive ailments like Alzheimer's disease.

Isolation and identification of cytotoxic compounds from the rhizomes of Paris quadrifolia L.

Jerzy Gajdus, Zbigniew Kaczynski, Anna Kawiak, Ewa Lojkowska, Justyna Stefanowicz-Hajduk, J. Renata Ochocka, Piotr Stepnowski

Pharmacognosy Magazine 2014 10(38):324-333

Background: Paris quadrifolia L. is a medicinal plant which contains steroidal saponins. The present study reports isolation and structural identification of six pennogenyl saponins obtained from P. quadrifolia rhizomes. The four spirostan saponins were obtained from P. quadrifolia for the first time. The cytotoxic effects of the sub-fractions and six compounds isolated from the plant extract were evaluated on tumour cells. Materials and Methods: Ethanol extract from the rhizomes of P. quadrifolia were partinioned using column chromatography. The saponins were isolated from the obtained sub-fractions by isocratic RP HPLC and their structures were determined by means of 1D and 2D NMR spectroscopy and MALDI TOF MS. The cytotoxic effects of the sub-fractions and the isolated compounds were tested against human promyelocytic leukaemia cells (HL-60), human cervical adenocarcinoma cells (HeLa) and human breast cancer cells (MCF-7) using the [(3-(4,5-dimethylthiazol-2-yl)]-2,5-diphenyltetrazolium bromide (MTT) assay. Results: Six pennogenyl saponins were isolated from P. quadrifolia rhizomes: pennogenin 3-O-&#946;-D-glucopyranoside (1), pennogenin 3-O-&#945;-L-rhamnopyranosyl-(1&#8594; 4)-&#946;-D-glucopyranoside (2), pennogenin 3-O-&#945;-L-rhamnopyranosyl-(1&#8594; 2)-&#946;-D-glucopyranoside (3), pennogenin 3-O-&#945;-L-rhamnopyranosyl-(1&#8594; 4)-&#945;-L-rhamnopyranosyl-(1&#8594; 4)-&#946;-D-glucopyranoside (4), pennogenin 3-O-&#945;-L-rhamnopyranosyl-(1&#8594; 4)-[&#945;-L-rhamnopyranosyl-(1&#8594; 2)]-&#946;-D-glucopyranoside (5), pennogenin 3-O-&#945;-L-rhamnopyranosyl-(1&#8594; 4)-&#945;-L-rhamnopyranosyl-(1&#8594; 4)-[&#945;-L-rhamnopyranosyl-(1&#8594; 2)]-&#946;-D-glucopyranoside (6). Pennogenyl saponins 5 and 6 exhibited cytotoxic activity against HL-60, HeLa and MCF-7 tumour cells with IC 50 values of 1.0 &#177; 0.04 &#956;g/ml, 1.8 &#177; 0.072 &#956;g/ml and 2.4 &#177; 0.096 &#956;g/ml respectively, and 2.0 &#177; 0.08 &#956;g/ml, 2.5 &#177; 0.125 &#956;g/ml and 3.2 &#177; 0.128 &#956;g/ml respectively. Conclusion: Compounds 1 -4 were isolated from this species for the first time.

Inhibitory effects of ginseng seed on melanin biosynthesis

Yeonmi Lee, Kyoung-Tack Kim, Sung Soo Kim, Jinyoung Hur, Sang Keun Ha, Chang-Won Cho, Sang Yoon Choi

Pharmacognosy Magazine 2014 10(38):272-275

Background: Ginseng root has been traditionally used for the treatment of many diseases in Korea. However, so far ginseng seed has been mostly unused and discarded. As part of our ongoing research on the ginseng seeds, the inhibitory effect of ginseng seeds on melanin production was verified to assess their potential as a skin depigmenting substance. Materials and Methods: The present study measured the inhibitory effect of ginseng seeds on melanin production through the tyrosinase inhibitory effect and analyzed their effects on melanin production in melan-a-cells. Results: Ethanol extract of ginseng seed was applied to melan-a-cells at a concentration of 100 ppm and melanin production was reduced by 35.1% without cytotoxicity. In addition, the ethanol extract of ginseng seed was shown to reduce tyrosinase activity. Conclusion: Because the results showed excellent melanin inhibitory activity compared with that obtained by arbutin, ethanol extracts of ginseng leaf and ginseng root at the same concentration, it can be concluded that ginseng seeds show great potential as a skin depigmenting substance.

Revisiting "Vegetables" to combat modern epidemic of imbalanced glucose homeostasis

Ashok Kumar Tiwari

Pharmacognosy Magazine 2014 10(38):207-213

Vegetables have been part of human food since prehistoric times and are considered nutritionally necessary and good for health. Vegetables are rich natural resource of biological antioxidants and possess capabilities of maintaining glucose homeostasis. When taken before starch-rich diet, juice also of vegetables such as ridge gourd, bottle gourd, ash gourd, chayote and juice of leaves of vegetables such as radish, Indian Dill, ajwain, tropical green amaranth, and bladder dock are reported to arrest significantly the rise in postprandial blood glucose level. Juice of vegetables such as ash gourd, squash gourd, and tropical green amaranth leaves are observed to tone-down sweet-beverages such as sucrose, fructose, and glucose-induced postprandial glycemic excursion. On the other hand, juice of egg-plant and juice of leaves of Ceylon spinach, Joyweed, and palak are reported to augment starch-induced postprandial glycemic excursion; and juice of leaves of Ceylon spinach, Joyweed, and radish supplement to the glucose-induced postprandial glycemia. Vegetables possess multifaceted antihyperglycemic activities such as inhibition of pancreatic &#945;-amylase and intestinal &#945;-glucosidase, inhibition of protein-tyrosine phosphatase 1&#946; in liver and skeletal muscles, and insulin mimetic and secretagogue activities. Furthermore, they are also reported to influence polyol pathway in favor of reducing development of oxidative stress, and consequently the development of diabetic complications. In the wake of emergence of modern maladaptive diet-induced hyperglycemic epidemic therefore, vegetables may offer cost-effective dietary regimen to control diet-induced glycemic over load and future development of diabetes mellitus. However, for vegetables have been reported to do both, mitigate as well as supplement to the diet-induced postprandial glycemic load, care is required in selection of vegetables when considered as medicament.

Molecular docking studies of flavonoids for their inhibition pattern against β-catenin and pharmacophore model generation from experimentally known flavonoids to fabricate more potent inhibitors for Wnt signaling pathway

Hira Iftikhar, Sajid Rashid

Pharmacognosy Magazine 2014 10(38):264-271

Background: Canonical Wnt signaling plays a key role in tumor cell proliferation, which correlates with the accumulation of &#946;-catenin in cell due to inactivation of glycogen synthetase kinase-3 &#946;. However, uncontrolled expression of &#946;-catenin leads to fibromatosis, sarcoma and mesenchymal tumor formation. Recently, a number of polyphenolic compounds of naturally occurring flavonoid family have been screened for the inhibition of Wnt signaling. Objective: Elucidation of the binding mode of inhibitors to &#946;-catenin, reporting more potent inhibitors for the disease-causing protein and designing a pharmacophore model based on naturally occurring compounds, flavonoids. Materials and Methods: In this study, a comparative molecular docking analysis was performed to elucidate the binding mode of experimentally reported and unknown inhibitors. Based on the knowledge of geometry, binding affinity and drug score, we described a subset of novel inhibitors. Results: The binding energy of known inhibitors (isorhamnetin, fisetin, genistein and silibinin) was observed in a range of &#8722;5.68 to &#8722;4.98 kcal/mol, while novel inhibitors (catechin, luteolin, coumestrol and &#946;-naphthoflavone) exhibited &#8722;6.50 to &#8722;5.22 kcal/mol. We observed good placement and strong interactions of selected compounds inside the binding pocket of &#946;-catenin. Moreover, flavonoid family members and T cell factors 4 (TCF4) compete for &#946;-catenin binding by sharing common binding residues. Conclusion: This study will largely help in understanding the molecular basis of &#946;-catenin/TCF4 inhibition through flavonoids by exploring their structural details. Finally, the novel inhibitors proposed in this study need further attention to uncover cancer treatment and with the generated pharmacophore model, more and potent &#946;-catenin inhibitors can be easily screened.

Effect of ultrasound on the isoflavonoid production in Genista tinctoria L. suspension cultures

Lenka Tumova, Jiri Tuma, Helena Hendrychova

Pharmacognosy Magazine 2014 10(38):425-429

Background: Application of ultrasound (US) to biotechnology is relatively new but several processes that take place in the presence of cells or enzymes are activated by ultrasonic waves. Genista tinctoria L. (Fabaceae) is rich on various kind of flavonoids, including isoflavones with valuable estrogenic activity. Objective: This study verified use of low-energy US elicitor to enhance secondary metabolite production in plant cell cultures. Materials and Methods: Suspension cultures of G. tinctoria cells was exposed to low-power US (with fixed frequency 35 kHz and power level 0.1 mW/cm 3 ) for period 1-5 min. Results: The US exposure significantly stimulated genistin content (0.8 mg/g DW) after 3 min of US treatment (sampled after 72 h). The highest daidzein level (1.4 mg/g DW) was reached after US irradiation for 5 min and 168 h sampling. Conclusion: The achieved results suggest that US can act as a potent abiotic elicitor to induce the defense responses of plant cells and to stimulate secondary metabolite production in plant cell cultures.

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