Studies on wound healing activity of some Euphorbia species on experimental rats

Background: Plants of Euphorbiaceae are used in folkloric medicines in variety of ailments and well known for chemical diversity of their isoprenoid constituents. This study was carried out to explore the preliminary wound healing potential of four Euphorbia species (E. consorbina 1, E. consorbina 2, E. inarticulata, E. balsamifera and E. schimperi).Materials and Methods: Excision wound surface of the animals were topically treated with ethyl acetate and methanol extracts of plants at a dose of 400 mg/kg body weight for twenty days. Povidone-iodine ointment was used as a reference drug. Wound contraction measurement and period of epithelialization were used to assess the effect of plants extracts on wound repairing.Results: The groups treated with methanol extracts of E. balsamifera and E. schimperi showed profound effects, high rate of wound contraction (100%) and decrease in epithelization period 19.00±0.40 and 18.50±0.64 respectively, followed by methanol extracts of E. consorbina 2, ethyl acetate extract of E. inarticulata and ethyl acetate extracts of E. consorbina 2 which showed significant (P <0.001) wound contraction and decrease in epithelization period. Conversely ethyl acetate extract of E. consorbina 1, E. balsamifera and E. schimperi and methanol extract of E. Consorbina 1 and E. Inarticulata treated groups was not showing significant wound healing. Methanol extracts of E. balsamifera and E. schimperi were also tested for their safety margin and found safe up to dose of 2000mg/kg body weight.Conclusion: Topical application of methanol extracts of E. balsamifera and E. schimperi have potential wound healing activity which is identical with standard drug Povidone-iodine.Keywords: Wound healing, excision wounds, Euphorbia, extract

EVALUATION OF ACUTE TOXICITY AND ANTI-INFLAMMATORY EFFECTS OF BACCHAROIDES SCHIMPERI (DC.) IN EXPERIMENTAL ANIMALS

Background: Steroidal and non-steroidal anti-inflammatory drugs are most commonly used to treat inflammation, and shown to have severe side effects. In this study, we aimed at evaluating the anti-inflammatory and acute toxicity effects of Baccharoides schimperi (DC.) in order to get new anti-inflammatory agents of natural origin. Materials and methods: The aerial part of the plant was dried under shade, ground and extracted with 96% alcohol (BSE). It was further fractionated in sequence to n-hexane (BSH), chloroform (BSC) and methanol (BSM) soluble fractions. Acute toxicity was evaluated by oral administration of plant and hind paw induced-edema method in rats was used for the anti-inflammatory evaluation. Results: The BSE was found safe up to the dose level of 3 g/kg b.w. and showed LD50 value 7.250 g/kg body weight (b.w.) in mice. BSE showed significant anti-inflammatory effect (62.91%) at 500 mg/kg b.w. Further the n-hexane, chloroform and methanol fractions of BSE were tested for anti-inflammatory activity. The n-hexane fraction (BSH) exhibits significant activity (64.87%) at 400 mg/kg b.w. The methanol fraction (BSM) showed dose dependent activity, highest activity (60.42%) was observed at higher dose 400 of mg/kg b.w. In chloroform fraction (BSC) no significant activity was observed. Conclusion: The results of the study revealed that the plant is safe to the experimental model and recommended as a potential source of anti-inflammatory agent

STUDIES ON WOUND HEALING ACTIVITY OF SOME EUPHORBIA SPECIES ON EXPERIMENTAL RATS

Background: Plants of Euphorbiaceae are used in folkloric medicines in variety of ailments and well known for chemical diversity of their isoprenoid constituents. This study was carried out to explore the preliminary wound healing potential of four Euphorbia species (E. consorbina 1, E. consorbina 2, E. inarticulata, E. balsamifera and E. schimperi). Materials and Methods: Excision wound surface of the animals were topically treated with ethyl acetate and methanol extracts of plants at a dose of 400 mg/kg body weight for twenty days. Povidone-iodine ointment was used as a reference drug. Wound contraction measurement and period of epithelialization were used to assess the effect of plants extracts on wound repairing. Results: The groups treated with methanol extracts of E. balsamifera and E. schimperi showed profound effects, high rate of wound contraction (100%) and decrease in epithelization period 19.00±0.40 and 18.50±0.64 respectively, followed by methanol extracts of E. consorbina 2, ethyl acetate extract of E. inarticulata and ethyl acetate extracts of E. consorbina 2 which showed significant (

Comparative profiling of biomarker psoralen in antioxidant active extracts of different species of genus Ficus by validated HPTLC method

Background: A simple but sensitive HPTLC method was developed for the comparative evaluation of psoralen in antioxidant active extracts of leaves of five different species of genus Ficus (Ficus carica, Ficus nitida, Ficus ingens, Ficus palmata and Ficus vasta).Materials and Methods: HPTLC studies were carried out using CAMAG HPTLC system on Glass-backed silica gel 60F254 HPTLC pre-coated plates using selected mobile phase toluene: methanol (9:1). The antioxidant activity was carried out, using DPPH free radical method.Results: Among all the five species of genus Ficus, F. palmata and F. carica exhibited comparatively good antioxidant activity in DPPH assay. The developed HPTLC method was found to give a compact spot for psoralen (Rf = 0.55±0.001) at 305 nm. The regression equation and r2 for psoralen was found to be Y= 4.516X+35.894 and 0.998. The quantification result revealed the presence of psoralen in only two species, F. carica (0.24%, w/w) and F. palmata (1.88%, w/w) which supported their supremacy for anti-oxidant potential over other species. The statistical analysis proved that the developed method was reproducible and selective.Conclusion: The developed method can be used as an important tool to assure the therapeutic dose of active ingredients in herbal formulations as well as for standardization and quality control of bulk drugs and in-process formulations. This method can also be employed for the further study of degradation kinetics and determination of psoralen in plasma and other biological fluids.Key words: Ficus species, psoralen, antioxidant, HPTLC, Validation

Lapatinib-based therapy for women with advanced/metastatic HER2 positive breast cancer

Background: Lapatinib alone or in combination with other agents, mostly capecitabine is used for patients with advanced/metastatic HER2 positive breast cancer (HER2+BC) after progression on trastuzumab based therapy. Here we report our experience with lapatinib based therapy in this setting. Material and Methods: 67 consecutive patients received lapatinib based therapy. 58 (86.6%) received lapatinib + capecitabine (LC), 7 (10.4%) with other agents and 2 (3.0%) as single agent lapatinib. Data was collected from patients’ records retrospectively. Results: Objective response to lapatinib based therapy in 64 evaluable patients was 64.0% in all patients and 64.0% in patients who received LC. Median progression free survival and overall survival were 10 and 27 months in all patients and 10 and 17 months in patients who received LC, respectively. 16 (24.0%) patients had dose delay > 1 week and/or dose reduction. Conclusion: Lapatinib based therapy is an effective treatment for women with advanced/metastatic HER2+BC after prior exposure to trastuzumab. It yields meaningful response rates, progression free and overall survival. Some patients require dose adjustments. Key Words: lapatinib-based therapy, metastatic breast cancer, HER2 positive breast cancer, trastuzumab

Neoclerodane Diterpenoids from Reehal Fatima, <i>Teucrium yemense</i>

<i>Teucrium yemense</i> (Defl), locally known as Reehal Fatima, is a medicinal plant commonly grown in Saudi Arabia and Yemen. Phytochemical investigation of the aerial parts of <i>T. yemense</i> yielded six new neoclerodane diterpenoids, namely fatimanol A–E (<b>1</b>, <b>2</b>, <b>3</b>, <b>5</b>, and <b>6</b>) and fatimanone (<b>4</b>), and the known teulepicephin (<b>7</b>). As both the <i>Teucrium</i> genus and the related <i>Lamiaceae</i> family have previously been widely reported to possess anthelmintic and antimicrobial activities, the structural and biological characterization of the seven diterpenoids was pursued. The structures of the new compounds were elucidated from their 2D NMR and MS profiles and by comparison to related compounds. The structure of fatimanol D (<b>5</b>) was confirmed by X-ray crystallographic analysis. The new structures contribute to the breadth of knowledge of secondary metabolites in this genus

COMPARATIVE PROFILING OF BIOMARKER PSORALEN IN ANTIOXIDANT ACTIVE EXTRACTS OF DIFFERENT SPECIES OF GENUS FICUS BY VALIDATED HPTLC METHOD

Background: A simple but sensitive HPTLC method was developed for the comparative evaluation of psoralen in antioxidant active extracts of leaves of five different species of genus Ficus (Ficus carica, Ficus nitida, Ficus ingens, Ficus palmata and Ficus vasta). Materials and Methods: HPTLC studies were carried out using CAMAG HPTLC system on Glass-backed silica gel 60F254 HPTLC pre-coated plates using selected mobile phase toluene: methanol (9:1). The antioxidant activity was carried out, using DPPH free radical method. Results: Among all the five species of genus Ficus, F. palmata and F. carica exhibited comparatively good antioxidant activity in DPPH assay. The developed HPTLC method was found to give a compact spot for psoralen (Rf = 0.55±0.001) at 305 nm. The regression equation and r2 for psoralen was found to be Y= 4.516X+35.894 and 0.998. The quantification result revealed the presence of psoralen in only two species, F. carica (0.24%, w/w) and F. palmata (1.88%, w/w) which supported their supremacy for anti-oxidant potential over other species. The statistical analysis proved that the developed method was reproducible and selective. Conclusion: The developed method can be used as an important tool to assure the therapeutic dose of active ingredients in herbal formulations as well as for standardization and quality control of bulk drugs and in-process formulations. This method can also be employed for the further study of degradation kinetics and determination of psoralen in plasma and other biological fluids

Three new diterpenes and the biological activity of different extracts of Jasonia montana.

Three new diterpenes, namely jasonin-a (1), jasonin-b (2), and jasonin-c (3) were isolated from the aerial parts of Jasonia montana (Asteraceae). Their structures were elucidated on the basis of spectral data as [(1E)-2-((2S)-1,2,5-trimethylbicyclo[3.2.l]octan-8-yl)vinyl] benzene-3-carboxylic acid (1), [3-((2S, 5S)-1,2, 5-trimethylcycloheptanyl)propyl]benzene-3-carboxylic acid (2), and [(1E)-3-((7R)-1,7-dimethy-4-methylenecycloheptanyl)prop-1-enyl] benzene-3-carboxylic acid (3). In addition, the previously reported 5,7,3'-trihydroxy-3,6,4'-trimethoxy flavone designated as centaureidin (4), was also isolated and characterized from this source. The different extracts of the plant were also screened for hypoglycemic, antidiabetic, and antimicrobial activities, wherein the petroleum ether and ethanolic extracts exhibited hypoglycemic and antidiabetic activity, and the petroleum ether and chloroform extracts showed antimicrobial activity