International Journal of Phytomedicine
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Cinnamic acid Supplementation Regulates the Production of Licochalcone A, Liquirtigenin and Licoisoflavone B in Glycyrrhiza glabra Callus Cultures.
Glycyrrhiza glabra is an ancient herbal medicine rich in large number of secondary metabolites which attribute to its therapeutic properties. These metabolites are usually obtained from field grown plants and their yields vary greatly on the basis of environmental conditions. Plant tissue culture can thus be a preferred method for consistent production of such metabolites. This study dealt with the enhancement of flavonoids through precursor feeding in callus cultures of G. glabra and investigated the influence of cinnamic acid on phenylalanine ammonia lyase (PAL) activity and production of licochalcone A, liquirtigenin and licoisoflavone B. Unorganized callus cultures were established from young leaf explants on Murashige and Skoog’s (MS) medium supplemented with NAA (1mg/l), BAP (0.5 mg/l) and various concentrations of cinnamic acid. Flavonoids were obtained from calli through solvent extraction and were identified and quantified through Gas-Chromatography Mass spectrometry. Cinnamic acid supplementation at appropriate concentrations (50mg/100ml for licochalcone A and liquirtigenin, and 125mg/100ml for licoisoflavone B) significantly increased their production to 1.28, 1.2 and 9.76 folds respectively. However, prolonged treatment of cinnamic acid at concentration beyond 50mg/100ml led to decrease in the production of liquirtigenin and licochalcone A , but caused fair increase in licoisoflavone B. Also cinnamic acid concentrations higher than 50mg/100ml reduced the activity of PAL enzyme due to its feedback inhibition, but at the same time might have modulated other intermediate enzymes of the pathway like chalcone isomerase favoring the formation of licoisoflavone B. Therefore, this study provides clear evidences of enzymatic regulation of phenylpropanoid pathway by cinnamic acid in G. glabra callus cultures
Possibilities of developing novel potent antitumor agents from the leaves of Cryptomaria japonica
During past few decades cancer has remained as the largest cause of mortality worldwide and number of patients suffering from cancer has been increasing at a fast rate. Hence medical research during the last few decades has been concentrating on identification and characterization of new synthetic pharmacological compounds to overcome this enormous problem. Leaf extracts of coniferous plant Cryptomeria japonica being known for their strong antibacterial and antifungal functions were selected to determine their antitumor/anticancer potentialities. Methanolic extract of leaves were tested to determine its antitumor action in standard murine model of Ehrlich Ascites Carcinoma (EAC). Graded doses of the extract were given intraperitoneally to batches of mice, who received EAC challenge after 3hr. Treatment with same amounts of extract was continued for 9 consecutive days. Protective capacity of the leaf extract was evaluated in animals. Statistically significant protection was observed with respect to different parameters including tumor volume , tumor cell count , viable tumor cell count, non- viable tumor cell count , mean survival time and increase in life span. Simultaneously hematological parameters were restored in treated mice vis-à-vis untreated control animals. Furthermore, the extract revealed distinct cytotoxic property, which may be the relevant reason of its anticancer/antitumor function. This study shows efficacy of methanolic extract of leaves of Cryptomeria japonica as a probable antitumor/anticancer agent. Phytochemical analysis of the extract showed presence of flavonoids, which are known to possess significant anticancer activity. Thus there is a definite possibility of developing novel anticancer drugs from such plant product
Evaluation of essential oils from Boswellia sacra and Teucrium mascatense against acetyl cholinesterase enzyme and urease enzyme
Enzyme inhibition is one of the most important areas of pharmaceutical research which resulted in the discoveries of several useful drugs. The prime aim of this study is to identify effective natural inhibitors against pharmacologically important enzymes such as acetylcholinesterase enzyme and urease enzyme. In present study, we evaluated the essential oils extracted from medicinally important plants including Boswellia sacra Flückiger (frankincense) and Teucrium mascatense Boiss. Two major constituents of frankincense essential oil including (+)-α-pinene and (R)-+-limonene were also investigated against these enzymes. The essential oils were extracted from Boswellia sacra and Teucrium mascatense which are native plants to the southern and northern areas of Oman, respectively. In this study, the essential oil of frankincense exhibited significant inhibition with IC50 value of 0.043±0.02 mg/mL, against acetylcholinesterase enzyme while against urease enzyme it has shown good inhibition with IC50 value of 0.17 ± 0.05 mg/mL. The essential oil obtained from the Teucrium mascatense was found to be in active against both the enzymes. On acetylcholinesterase enzyme inhibition assay, the (+)-α- pinene exhibited significant inhibition (IC50 = 0.094±0.01 mg/mL) while (R)-+- limonene was found to be inactive on this assay. Against urease enzyme (+)-α- pinene and (R)-+- limonene showed moderate activity 40.06±1.03 % and 19.5±1.00 %, respectively. Interestingly, the mixture of equal concentration of (+)-α- pinene and (R)-+- limonene exhibited 70% inhibition with IC50 value of (0.195 ± 0.10 mg/mL) which shows the synergistic relationship between them. Promising inhibitory potential of frankincense essential oil and (+)-α-pinene, against acetylcholinesterase enzyme and urease enzyme indicated their potential therapeutic role to manage Alzheimer’s disease and stomach ulcers, respectively
Antiulcer And Antioxidant Potential Of Zizyphus jujuba Mill Root Extract In Aspirin And Ethanol Induced Gastric Ulcers.
The root of Zizyphus jujuba Mill. (Rhamnaceae) (ZJ) has been used to treat mouth ulcers as indigenous medicine. However there is no scientific report of its use for protection and treatment of gastric ulcers. The aqueous root extract of ZJ (AREZJ) was evaluated for antiulcerogenic potential in aspirin and ethanol induced ulcer models in Wistar rats along with in vitro antioxidants potential. Single dose toxicity studies were carried out to determine LD50. Two doses i.e. 150 and 250 mg/kg b.wt were evaluated for antiulcer activity by measuring ulcer index and percentage of ulcer healing in two of the ulcer models. Antioxidants activity was estimated in vitro by DPPH, H2O2 free radical scavenging and reducing power assay. Phytocostituents were determined by standard method. Based on ulcer index, percentage protection of 76.92% in aspirin model and 70% in ethanol model were noted with a dose of 250 mg/kg b.wt of AREZJ, whereas standard drug omeprazol (50 mg/kg b.wt) showed 80.77 % and 80 % protection in aspirin and ethanol models respectively. AREZJ showed 89.2% DPPH and 88.5% H2O2 free radical scavenging activity at concentration of 200 μg/ml and 80 μg/ml respectively. AREZJ also exhibited 87.5% reducing power at 50 μg/ml. Phytochemical screening of AREZJ showed presence of alkaloids, carbohydrates, flavanoids, glycosides, proteins and tannins. No mortality was noted till 2500 mg/kg b.wt of AREZJ, indicating higher LD50 value. AREZJ was found to have antiulcerogenic effect, which could be related to its antioxidant potential
Evaluation of total phenolics, antioxidant and antiproliferative activities of rhizome extracts from select Zingiberaceae species in South India
Zingiberaceae family members are well known for their ethnobotanical diversity and medicinal importance. This study aimed to evaluate total phenolic content, antioxidant and antiproliferative capacity of five different organic solvent extracts prepared from the rhizomes of Curcuma mutabilis (CM), Curcuma haritha (CH), Curcuma neilgherrensis (CN) and Zingiber anamalayanum (ZA), four hitherto unexplored Zingiberaceae species. Folin-Ciocalteu method and DPPH radical scavenging assay were used to determine respectively the total phenolic content and antioxidant capacity. The antiproliferative activity of the extracts were tested against four human cancer cell lines – K562, REH, Nalm6 and MCF7 to ascertain the IC50 values. Based on total phenolic content, extracts were classified into high-H (> 150 mg GAE/g), medium-M (50-150 mg GAE/g) and low-L (< 50 mg GAE/g) categories. Likewise, percentages of DPPH scavenging activity of extracts were also grouped into high-H (> 50%), medium-M (25 – 50%) and low-L (< 25%) categories. Ten of the twenty extracts exhibited strong cytotoxicity with an IC50 value less than 30 μg/mL. To our knowledge, this is the first report on quantitative assessment of total phenolics, antioxidant and antiproliferative potential of organic solvent extracts of rhizomes from the above mentioned plants
Isolation, evaluation and characterization of isolated compounds from aqueous extract of Cestrum nocturnum
The aim of present study was to isolate, characeterise and evaluation anticoagulant properties of the isolated compound from aqueous extract of Cestrum nocturnum using aPTT-Activated Partial Thromboplastin Time, PT- Prothrombin Time & TT-Thrombin Time as standard procedures. From all the result it can be concluded that water extract of Cestrum nocturnumplant was found to be best among all the extract under study and from the isolates of water extract of Cestrum nocturnum plant AE5 was found to be best activity (anti-platelet, Fibrinolytic and anti-coagulant). Further fractionation of water extract generated two isolates AE5a & AE6a and after their pharmacological activity they were found to be potent phytochemical constituents. From the structural elucidation study of AE5a & AE6a were identified as Rutin and quercetin respectively. From this study it was concluded that the flavoinoidal compound i.e. Rutin and Quercetin were present in the Cestrum nocturnum plant and they both responsible for the anti-platelet, Fibrinolytic and anticoagulamt activity of plant
Preclinical safety assessment and mutagenicity of the hydroethanolic extract of Syzygium campanulatum leaves.
Syzygium campanulatum (Myrtaceae) is a species indigenous to Southeast Asia, a widely consumed medicinal herb and rich in phytochemical content and notable antiangiogenic and anti-colon cancer. Safety reports of administration of S. campanulatum are however lacking. In this study, we investigated the quality of dried leaves, chemical composition analyzed by FTIR and HPLC, phytochemicals content and repeated doses toxicity and mutagenicity effect of the hydroethanolic extract of S. campanulatum leaves (HESCL). The rats were divided into experimental and control groups and fed with 500, 1000, 2000 mg/kg/day of the hydroethanolic extract of S. campanulatum leaves for 28 and 90 days and with a single dose of 5000 mg/kg in acute study. The obtained results showed the dry leaves of S. campanulatum were devoid of any heavy metal and microbial contamination. The major components of HESCL were, respectively betulinic acid (60.43 mg/g.), total glycol saponins, total phenolics, total proteins, total tannins, and total flavonoids. No mutagenicity was detected in S. typhimurium auxotroph and no signs of clinical toxicity and mortality were observed in the experimental groups after 28 and 90-day experiment. However, significant (p < 0.05) statistical deviations were observed in hematological, and biochemical parameters but they were within the normal clinical range for rat, therefore not considered treatment-related. Based on these findings the fifty percent lethal dose was > 5000 mg/kg and the NOAEL was up to 2000 mg/kg for 90 days, as such HESCL is a relatively safe herb
Identification of natural products and their derivatives as promising inhibitors of protein glycation with non-toxic nature against mouse fibroblast 3T3 cells
This study was performed to identify new inhibitors of protein glycation in vitro. Protein glycation is one of the major causes of late diabetic complications. In this study, terpenoids and alkaloids, isolated from different medicinal plants, along with their derivatives, were evaluated for their antiglycation activity in vitro, while MTT assay on mouse fibroblast 3T3 cells was used to assess their potential cytotoxicity. Among the tested compounds, gossypol (2,2′-bis-(formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene) (1), isolated from Gossypium herbaceum, and its derivatives, gossypol acetic acid (2), gossypolidene- 4-aminoantipyrine (4), and gazolidone (6), showed a potent antiglycation activity (IC50 < 16 µM), while gossypolidene-4-aminoantipyrine (5) showed a significant antiglycation activity with IC50 value 82.934±2.924 µM, in BSA-fluorescence assay. Alkaloid, noscapine (3S)-6,7-Dimethoxy-3-[(5R)-4-methoxy-6-methyl-5,6,7,8-tetrahy-dro-1,3-dioxolo[4,5-g]isoquinolin-5-yl] isobenzofuran-1(3H)-one (7), isolated from Papaver somniferum, N-nitrosoaphyllinic acid (9), a derivative of alkaloid aphylline, and 2H-quinolizine, octahydro salt (11), a salt of alkaloid lupinine, exhibited significant inhibition activity with IC50 values 152.662±5.432, 393.758 ±4.001 µM and 110.203±4.816µM, respectively. Similarly, compounds gossypolidene thiocarbamide (3), deoxypeganine hydrochloride (8), lupinine (10) and cytisine (12) showed moderate inhibition with IC50 values of 401.865 ±18.450, 863.322 ±6.415, 712.176±7.745, and 728.462±2.331 µM, respectively. The results were compared with the standard antiglycation agent, rutin (13) (IC50 =98.012±2.030 µM). Cellular cytotoxicity assay showed only gossypol acetic acid (2) and gossypolidene thiocarbamide (3) as somewhat toxic to 3T3 (mouse fibroblast) cells with IC50 values 2.07 ±0.61 and 5.00 ±1.89 µM, respectively. Cycloheximide was used as a standard in this assay with IC50 value 0.3 ± 0.089 μ
Larvicidal and Anti-inflammatory Activities of Funtumia Africana (Benth) Stapf Leaf and Stem
Larvicidal and Anti-inflammatory Activities of Funtumia Africana (Benth) Stapf Leaf and Ste
In vitro antioxidant activities of n-butanol extract of Helianthemum confertum
Antioxidants play an important role to protect damage caused by oxidative stress. Plants having phenolic contents are reported to possess antioxidant properties. The basic aim of this research was to investigate the antioxidant properties of n-butanol extract of Helianthemum confertum, Cistaceae family. The antioxidant activities and phenolic contents of n-butanol extract were evaluated in vitro using spectrophotometer methods. There antioxidant activities were determined by DPPH (1,1-diphenyl-2-picrylhydrazine) radical scavenging assay and lipid peroxidation inhibition by TBARS method. Antioxidant activities were compared to ascorbic acid. Measurement of total phenolic compounds and total flavonoids content of the n-butanol extract of Helianthemum confertum were achieved using Folin-Ciocalteau reagent and AlCl3 respectively. The results showed that this extract containing 263.33±19.85µg of gallic acid equivalents/mg extract of total phenolic and 25.35±3.15µg of quercetin equivalents/mg extract total flavonoids