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Background: Oleamide is an essential substance for human health. So, the plants with high oleamide content are great sources for health care products. Objective: This study is conducted to investigate the quality of oleamide in plants and test the bioactivity in the selected two studied species. Methods: The three Ipomoea and five Dillenia species including Ipomoea alba, Ipomoea aquatica and Ipomoea pes-caprae, and Dillenia indica, Dillenia obovata, Dillenia ovata, Dillenia parviflora and Dillenia pentagyna were investigated for the quantity of oleamide by high-performance liquid chromatography. The biological activity test was conducted on the powder formulation of the chosen plants, Dillenia ovata and Dillenia parviflora at a ratio of 30:70, for anti-inflammatory activity ex vivo on a panel of molecular targets through ion channel inhibition including voltage-gated sodium channel, voltage-gated potassium channel, and the cardiac ion as human ether-a-go-go related gene. Results: The results showed that the leaf extracts of I. aquatica and D. ovata gave the highest and subsequent oleamide quantity i.e. 7.52 and 5.17 mg/g, respectively. Out of the Dillenia formulation which contained various compounds, oleamide showed the highest percentages of inhibition at 8.0-20.0%, and 6.2-14.2% in voltage-gated sodium channel, and voltage-gated potassium channel which had slightly lower values than the oleamide standard, and no effect as 0.0% value inhibition in the cardiac ion channel. Conclusion: The Dillenia formulation exhibits anti-inflammatory activity without affecting the heart. Accordingly, the three studied Ipomoea and three studied Dillenia species may be used for the same activity as a single component or formulation with effective solvent for disease treatments.

Davilla elliptica (Dilleniaceae) is a shrub that occurs naturally in the Brazilian Savannah (Cerrado). This shrub has been widely used in Brazilian folk medicine in tea preparing; infusions; and decoctions from leaves and roots for gastritis, ulcers, and diarrhea treatment. Given the therapeutic potential of this species, the present study provides a comprehensive review on its ethnopharmacological uses, botanical aspects, phytochemistry characterization, and in vivo and in vitro pharmacological studies. The relevant studies on D. elliptica were retrieved from the following scientific databases: Web of Science, Google Scholar, Scopus, SciFinder, PubMed, Scielo, and ScienceDirect. Additional information derived from other literature sources, such as books and Ph.D. and MSc theses, was also considered after a critical review. Ethnopharmacological reports of D. elliptica revealed the use of infusions from roots with tonic and purgative effects, whereas leaves have been used as anti-inflammatory and anti-ulcerative treatments, as well as to treat diarrhea and gastric disorders. Furthermore, fresh leaves have been used in baths to treat swelling. Phytochemical studies have led to the isolation of several compounds, including flavonoids derived from quercetin and myricetin, and tannins, which are known to exhibit relevant pharmacological activities. In vitro assays using crude extracts and/or isolated fractions and chemical constituents from D. elliptica have evidenced antibacterial, cytotoxic activities, while in vivo studies have proven gastroprotective, anti-inflammatory, antihemorrhagic, and antibacterial activities, corroborating ethnomedicinal reports. No relevant side effects has been reported previously, and some studies found a low toxicity and genotoxicity. However, further studies are still needed to ensure the safety of its therapeutic use. Future studies should focused on molecular mechanisms involved in bioactive components’ effects based on both fractions and isolated compounds, creating great opportunities for new investigations.

BACKGROUND Ibuprofen is used both for acute and chronic disorders, such as ankylosing spondylitis, osteoarthritis and rheumatoid arthritis; however, ibuprofen causes gastrointestinal disturbances. Therefore, it would be desirable to design it as a sustained-release preparation. OBJECTIVES To design ibuprofen microbeads using polymers obtained from Xanthosoma sagittifolium starch and Dillenia indica mucilage to provide sustained-release delivery of ibuprofen. MATERIAL AND METHODS The polymers were extracted using standard methods and characterized by their material, physicochemical, elemental, and rheological profiles. Microbeads loaded with ibuprofen were prepared using the ionotropic gelation method utilizing blends of the polymers and sodium alginate. The microbeads were evaluated using particle shape, particle size, swelling index, entrapment efficiency, and release assays. RESULTS The results showed that the polymers have distinct material and physicochemical properties unique to their botanical sources. The microbeads were spherical and free-flowing, and they rolled without friction. The swelling properties ranged from 47.62 ±2.74% to 79.49 ±3.66%. The particle size of the microbeads ranged from 88.14 ±68.57 μm to 214.90 ±66.95 μm, while the encapsulation efficiencies ranged from 20.67 ±4.66% to 83.61 ±6.35%. The dissolution times suggested that the concentration of the natural polymers in the bead formulation could be used to modulate the dissolution properties. Generally, formulations containing the mucilage yielded higher dissolution times than those containing the starch. The kinetics of drug release from the microbeads containing the polymer blends generally fitted the Korsmeyer-Peppas model. The highest similarity was found between formulations C6 and D4 with f2 of 81.07. CONCLUSIONS The microbeads prepared with polymers obtained from Xanthosoma and Dillenia showed acceptable physicochemical properties, dependent upon polymer type, blend and concentration.

Made available in DSpace on 2022-05-01T09:47:19Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-01-01 Doliocarpus dentatus (Dilleniaceae) has been used in folk medicine to treat inflammation and pain; however, studies evaluating its toxicity potential, as well as its effects on anxiety and depression, are scarce. This study investigated the toxicological profile of an ethanolic extract from leaves of D. dentatus (EEDd), and its effects on anxiety and depression models in mice. Male and female mice received either a single dose (500, 1000 or 2000 mg/kg) or repeated doses (75, 150 or 300 mg/kg) of EEDd by oral gavage. During the subacute toxicity assay, behavioral tests were performed on days 4, 14, 21 and 28. No evidence of toxicity was observed in the animals in both acute and subacute tests. However, males treated with the highest dose presented a reduction in the absolute weight of the kidney, an elevation in the AST levels, in addition to an alteration in the urea levels. The treatment did not affect other biochemical parameters, and did not induce any depressive-like behavior. EEDd exhibited low toxicity after single and repeated exposures. Since some analyzed parameters were compromised, further toxicity studies should be carried out. Faculty of Health Sciences Federal University of Grande Dourados Postgraduate Program in Chemistry Faculty of Exact Sciences and Technology Federal University of Grande Dourados Faculty of Health Sciences University Center of Grande Dourados Faculty of Exact and Agrarian Sciences University Center of Grande Dourados Center of Studies in Natural Resources State University of Mato Grosso Do Sul Department of Structural and Functional Biology Institute of Biosciences of Botucatu UNESP–Paulista State University Pharmaceutical Sciences Food and Nutrition College Federal University of Mato Grosso do Sul Department of Structural and Functional Biology Institute of Biosciences of Botucatu UNESP–Paulista State University

Tetracera scandens is a medicinal shrub that belongs to Dilleniaceae. The leaves of the plant have been traditionally used in the treatment of diabetes mellitus in Malaysia. The conventional quality control analysis of medicinal plants that relies on the quantification of few major metabolites is considered time-consuming since it requires extensive sample preparation and neglects the possible impacts that the minor metabolites could have on the activity. This study was aimed to investigate the α-glucosidase inhibitory (AGI) potential of different hydromethanolic extracts of T. scandens leaves and to establish a predictive multivariate model that could be used for the quality evaluation of T. scandens leaf based on the Fourier transform infrared (FT-IR) spectra of its extracts. Different solvent ratios (0%, 20%, 40%, 60%, 80% and 100% methanol in water) were used to prepare a total of 36 extracts. The AGI potential and the FT-IR fingerprint spectrum were acquired for each extract. A four components orthogonal partial least squares (OPLS) model (1 + 3 + 0) with R2Y of 0.951 and Q2Y of 0.916 was established to describe the correlation between the fingerprint FT-IR spectra of different T. scandens extracts and their corresponding AGI activities. The carbon-halide, carbon–oxygen single bonds, as well as the hydroxyl and carbonyl groups were identified to be positively correlated with the AGI activity. To sum up, an OPLS model was successfully developed as a rapid quality evaluation method to predict the AGI activity of T. scandens.

The aim of this study was to assess the efficiency of mucilage extracted from the fruit of Dillenia indica for enhancing coagulation in the treatment of textile effluent. The mucilage extraction was carried out in water at room temperature. The pH, concentration of coagulant FeCl3.6H2O, and concentration of mucilage solution were optimized with star-type central composite design (CCD). We were able to analyze the synergistic effects between the FeCl3.6H2O and mucilage concentrations: the process of coagulation/flocculation (CF) for chemical oxygen demand (COD) removal was more efficient at a low chemical coagulant concentration (8.00 mg L−1) and a higher natural coagulant (NC) concentration (15.00 mg L−1). This demonstrated the potential of this mucilage to treat textile effluents, with 67.66%% COD removal, 96.86% turbidity removal and 91.12% apparent color reduction. The characterization of the mucilage of Dillenia indica was done using Fourier transform infrared spectroscopy (FTIR) and solid-state cross-polarization magic angle spinning carbon-13 nuclear magnetic resonance (CP/MAS 13C NMR), and the signals obtained indicated the presence of polysaccharides, which are responsible for enhancing the CF process.

Dillenia indica Linn. (syn. P. lanigerum; chalta in Bangla; Family Dilleniaceae) is an evergreen large shrub or small to medium-sized tree that grows all over the NE states, especially Tripura and Bangladesh. Named after Johann Jacob Dillenius, a German botanist, Dillenia is a genus of about 100 species of flowering plants in tropical and subtropical trees of southern Asia, Australasia, and the Indian Ocean Islands. However, up to now, only eight Dillenia species have been reported to be used traditionally for different medical purposes including treatment of cancerous growth. Medicinal properties of the fruit juices of D. indica are manifold, as a cooling beverage to treat fever and to relieve fatigue. Although mainly a source of food for elephants and monkeys, the ripped fruits are taken orally to increase appetite and overcome weakness, as laxative and medication for abdominal pain. Native communities in Mizoram, India, have used the fruits of the plant as a remedy for jaundice. All the plant parts viz., leaves, bark, fruit, fruit peel, etc. all have proven medicinal properties against most of the common ailments including anti-cancer and anti-microbial properties. Some of the major compounds with medicinal and nutritive value are lupeol, betulinaldehyde, betulinic acid and stigmasterol.

Here, we report an ultrasonic-assisted extraction (UAE) of phytochemicals from bark, leaves, sepals, fruits, and seeds of Dillenia pentagyna (Roxb) using different organic solvents such as chloroform, ethanol, and n-hexane. The preliminary phytochemical screening results showed that the ethanolic extract is enriched with phenolics, flavonoids, tannin, saponin, alkaloid, and terpenoids. The profiling of phytochemicals is carried out employing UV–Vis and Fourier-transform infrared (FTIR) spectroscopy analyses. The higher amount of phenolic compounds obtained in the ethanolic extract of bark and leaves as compared to other parts of the plant. Consequently, a higher amount of total flavonoid compounds unveiled in the bark of targeted species. The ethanolic extract of bark and leaves showed good free radical scavenging activity using DPPH with inhibition percentage of 90.58 ± 1.89% and 76.46 ± 1.58%, respectively, in comparison to standard ascorbic acid at 10 μg/mL. Moreover, the half-maximal inhibitory concentration (IC50) value of bark and leaves are 5.64 and 6.54 μg/mL, respectively, in comparison to standard ascorbic acid. With the best of our knowledge, it is the first report pertaining to characterization and quantification of phenols and flavonoids as well as the investigation of the medicinal property in D. pentagyna.

Ethnopharmacological relevance In the State of Mato Grosso do Sul, the watery sap of Doliocarpus dentatus is used to alleviate thirst, and the leaves of this species are used to relieve pain and swelling associated with inflammatory processes. Aim of the study This study aimed to analyze the compounds of the leaves from the aqueous extract of D. dentatus (EADd) and evaluate its toxicogenetic and pain relief effects in animal models. Materials and methods Compounds were identified in EADd by UHPLC-HRMS (Ultra high-performance liquid chromatography coupled to high resolution mass spectrometry). The oral dose of 17 mg/kg EADd, calculated according to ethnopharmacological uses, and doses between 30 and 300 mg/kg were used to test Swiss mice in formalin- and acetic acid-induced models of pain and behavior. EADd (100–2000 mg/kg) was assayed in mice by comet, micronucleus, and phagocytosis tests and by peripheral leukocyte counts. Results Phenolic compounds and flavonoids as well as trigonelline and isoquercetin were identified in EADd. All oral doses of EADd exhibited antinociceptive activity, as indicated by a decrease in pain in both phases, a decrease in cold hypersensitivity induced by formalin, and a decrease in abdominal contortions induced by acetic acid. EADd did not alter the exploratory, motor or motivational activities of the animals. The comet and micronucleus tests indicated that EADd was not genotoxic and did not change the phagocytic activity or peripheral leukocyte count. Conclusions These results demonstrate that EADd could act as an antinociceptive agent that does not present genotoxicity. This study should contribute to justifying, in part, the popular use of D. dentatus in pain management, ensuring its safe use.

Background Tetracera alnifolia Willd. (Dilleniaceae) is used in traditional African Medicine for the treatment of headache, abdominal pain, and rheumatism. Hence, this study sought to investigate the antinociceptive and anti-inflammatory effects of the hydroethanolic leaf extract of T. alnifolia (HeTA) in rodents. Methods Antinociceptive activity was evaluated using the acetic acid-induced writhing, formalin-/capsaicin-induced paw licking and hot plate tests in mice. The contribution of opioidergic, l-arginine-nitric oxide, and ATP-sensitive potassium channel pathways in HeTA-induced antinociception was also evaluated. The anti-inflammatory effect was assessed using the carrageenan-induced paw edema, xylene ear edema, cotton pellet granuloma, and complete Freund’s adjuvant (CFA)-induced arthritis in rats. Results HeTA (100, 200, and 400 mg/kg, p.o.) produced significant (pl-arginine (nitric oxide precursor), or glibenclamide (ATP-sensitive potassium channel blocker). HeTA (100 mg/kg, p.o.) produced a significant anti-inflammatory effect against carrageenan-induced rat paw edema (1–5 h), xylene-induced ear edema, cotton pellet-induced granuloma formation, and CFA-induced arthritis in rats. The effects of HeTA in various models were similar to the effect of the standard reference drugs. Conclusions Findings from this study showed that HeTA possesses antinociceptive effect possibly mediated through peripheral opioid receptors with activation of l-arginine-nitric oxide and ATP-sensitive potassium channel pathway as well as anti-inflammatory activity.

The bioactivity guided fractionation of Tetracera indica leaves crude ethanolic extract has afforded the isolation and characterization of six compounds including a new natural product viz., 5,7-dihydroxyflavone-O-8-sulphate (1) and five known flavonoids (2–6). The structures of the compounds were elucidated using 1D and 2D NMR and HRESIMS spectroscopic analyses. All the isolated compounds were evaluated for their in vitro inhibitory activity against alpha-glucosidase. Compound 1, 5 and 6 showed strong alpha-glucosidase inhibitory activity, 3 and 4 displayed weak activity while compound 2 was inactive. The interactions of the active compounds with alpha-glucosidase were further investigated using molecular docking to confirm their antidiabetic potential.

Background:The plant under investigation (Tetracera sarmentosa) is a dicotyledonous flowering plant and belongs to the family Dilleniaceae. The goal of our investigation was to determine whether the leaf extracts of this plant held any significant medicinal properties.Methods:Leaves ofT. sarmentosawere extracted with pure ethanol (EETS) and methanol (METS), and then methanol extract fractioned withn-hexane (NHFMETS) and chloroform (CHFMETS). The extracts and fractions were tested for antioxidant activity, which was measured by using qualitative and quantitative procedures. Thrombolytic activity was evaluated by the clot lysis test. Analgesic activity was evaluated employing the acidic acid-induced writhing test, the formalin-induced paw licking test and tail immersion on Swiss albino mice. The anti-inflammatory activity test was studied using the paw edema test. Forced swimming, tail suspension, elevated plus maze and hole board model tests were used to evaluate neuropharmacological activity.Results:All the extracts and fractions possessed antioxidant effects. All the extracts, fractions and streptokinase exhibited significant (pConclusions:The overall results suggested that this plant deserves further investigation to isolate the active compounds which are responsible for these activities and to establish the mechanism of action.

Tetrascera scandens , a member of Dilleniaceae, is used for traditional medicine; the stem is utilized by the Anak Dalam tribe of Jambi Province, Sumatera island, Indonesia, to treat diarrhea symptoms. The aims of this study were to identify the secretory structures, histochemical aspects, and the antibacterial potency of T. scandens stem. Histological study of the secretory structures of T. scandens stem was carried out. The species has idioblast cells and trichomes as its secretory structures. Histochemical analysis indicated the substance secreted by T. scandens idioblast cells mainly contains alkaloids, terpenoids, and phenols. Trichomes of T. scandens only contain flavonoids. The antibacterial activity of methanol extracts was tested against Staphyllococcus aureus and Escherichia coli . Different concentration of extracts was tested using the well diffusion method. According to the results, 100 mg/mL T. scandens extract showed the best inhibitory activity with a maximum inhibition zone of 17.7 mm against S. aureus and of 12.5 mm against E. coli . This study provides scientific evidence that the stem of T. scandens has antibacterial activity and justifies its use by the local community.

The fruit of Dillenia indica L. is extensively used as a food additive. Betulinic acid (BA) is the most prominent secondary metabolite present in D. indica. This study screened the bioassay guided isolation of BA from D. indica and explored its tyrosinase inhibitory mechanism. Half maximal inhibitory concentration (IC50) of BA were calculated as 13.93µM and 25.66µM for diphenolase and monophenolase. Enzyme kinetic analysis revealed that BA inhibited tyrosinase activity non-competitively. Further, conformational analysis of tyrosinase with BA was measured by fluorescence and circular dichroism spectroscopy. These results implied that diminish rigidity of enzyme might disturb the catalytic conformation of tyrosinase. Moreover, In-silico analysis confirmed probable binding polar and non-polar region on the active site of tyrosinase. Based on these findings, we suggest that BA from D. indica may be useful in preventing enzymatic browning reactions in food products.

Background Tetracera indica Merr. (Family: Dilleniaceae), known to the Malay as ‘Mempelas paya’, is one of the medicinal plants used in the treatment of diabetes in Malaysia. However, no proper scientific study has been carried out to verify the traditional claim of T. indica as an antidiabetic agent. Hence, the aims of the present study were to determine the in vitro antidiabetic potential of the T. indica stems ethanol extract, subfractions and isolated compounds. Methods The ethanol extract and its subfractions, and isolated compounds from T. indica stems were subjected to cytotoxicity test using MTT viability assay on 3T3-L1 pre-adipocytes. Then, the test groups were subjected to the in vitro antidiabetic investigation using 3T3-L1 pre-adipocytes and differentiated adipocytes to determine the insulin-like and insulin sensitizing activities. Rosiglitazone was used as a standard antidiabetic agent. All compounds were also subjected to fluorescence glucose (2-NBDG) uptake test on differentiated adipocytes. Test solutions were introduced to the cells in different safe concentrations as well as in different adipogenic cocktails, which were modified by the addition of compounds to be investigated and in the presence or absence of insulin. Isolation of bioactive compounds from the most effective subfraction (ethyl acetate) was performed through repeated silica gel and sephadex LH-20 column chromatographies and their structures were elucidated through 1H–and 13C–NMR spectroscopy. Results Four monoflavonoids, namely, wogonin, norwogonin, quercetin and techtochrysin were isolated from the T. indica stems ethanol extract. Wogonin, norwogonin and techtochrysin induced significant (P

A green approach was envisaged for the rapid synthesis of stable silver nanoparticles in an aqueous medium using phenolic rich ethanolic bark extract from D. indica with marked free radical scavenging and reducing ability. Biosynthesis of silver nanoparticles (AgNPs) was confirmed and characterized by using UV–visible spectroscopy, particle size analyzer, X-ray diffractometry (XRD), Transmission Electron Microscopy (TEM) and Fourier Transform Infrared Spectroscopy (FT-IR). Bio-reduction of Ag+ was confirmed with the appearance of golden yellow coloration within 5–10 min at 45 °C with maximum absorbance at 421 nm. XRD analysis of AgNPs indicated the crystalline nature of metallic Ag. As analyzed by TEM, AgNPs were found to be spherical in shape, well dispersed and size varied from 15 to 35 nm and dynamic light scattering (DLS) studies showed the average particle size of 29 nm with polydispersity index (PDI) of 0.280. Synthesized AgNPs were showing surface functionalization as revealed through FTIR studies. These AgNPs were observed to be highly stable at room temperature (28 ± 2 °C) for more than 3 months, thereby indicating the ethanolic extract of D. indica was a reducing as well as a capping agent for stabilization of AgNPs. Moreover, these green synthesized AgNPs showed enhanced free radical scavenging and excellent catalytic activities when used in the reduction of 4-nitrophenol and methylene blue dye, at room temperature.

Based on ethnopharmacological studies, a lot of plants, as well as its compounds, have been investigated for the potential use as wound healing agents. In Brazil, Curatella americana is traditionally used by local people to treat wounds, ulcers and inflammations. However, to the best of our knowledge, its traditional use in the treatment of wounds has not been validated by a scientific study. Here, some compounds, many of them flavonoids, were identified in the hydroethanolic extract from the leaves of C. americana (HECA) by LC-HRMS and LC-MS/MS. Besides that, solutions containing different concentrations of HECA and a gel produced with this extract were evaluated for its antimicrobial, coagulant and wound healing activities on an excision mouse wound model as well as its acute dermal safety. A total of thirteen compounds were identified in HECA, mainly quercetin, kaempferol and glucoside derivatives of both, besides catechin and epicatechin known as wound healing agents. The group treated with 1% of HECA exhibited highest wound healing activity and best rate of wound contraction confirmed by histopathology results. The present study provides scientific evidence of, this extract (HECA) possess remarkable wound healing activity, thereby, supporting the traditional use.

Multi- drug resistant microbial pathogens are a serious global health problem and thus new antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. Hence, the objective of the present study was to investigate the antibacterial activity of 6β-hydroxy-3-oxolup-20(29)-en-28-oic acid (6β-hydroxy betunolic acid) isolated from the bark of Schumacheria castaneifolia and its effect when combined with oxacillin. Antibacterial potential of 6β-hydroxy betunolic acid alone was performed using broth micro dilution assay against sixteen bacterial strains which included eight standard strains [Staphylococcus aureus (ATCC 29213 and ATCC 25923), Enterococcus faecalis (ATCC 29212), Escherichia coli (ATCC 35218 and ATCC 25922), carbapenemase producing Kebsiella pneumonia (ATCC BAA 1705), carbapenemase non-producing K. pneumonia (ATCC BAA 1706) and Pseudomonas aeruginosa (ATCC 27853)] and four strains each of clinically isolated meropenem resistant Acinetobactor sp. and methicillin resistant S. aureus (MRSA) which were included in the urgent threat list and serious threat list, respectively in 2019 by the Centers for Disease Control and Prevention in the United States. Its effect when combined with oxacillin was tested against S. aureus (ATCC 29213) and MRSAs using a checkerboard dilution method. The results indicated that 6β-hydroxy betunolic acid had antibacterial activity against the tested Gram positive organisms with MICs ranging from 16 to 32 mg L−1 (MIC of oxacillin and meropenem ranged from 0.25–16 and 0.03–128 mg L−1 respectively). The high MIC values (>1024 mg L−1) of 6β-hydroxy betunolic acid against Gram negative strains indicated a likely lack of activity. Further, 6β-hydroxy betunolic acid exhibited synergistic effect with oxacillin against Staphylococcus aureus (0.49) and showed an additive effect against all the tested MRSAs. The present study suggested that the antibacterial activity of the 6β-hydroxy betunolic acid is restricted to Staphylococcus isolates and possibly Enterococcus faecalis. Further testing on different types of Gram positives and identification of the exact mechanism of action would be of importance.

Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis ( Fomogne-Fodjo et al., 2014 ). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs. Materials and methods T. potatoria medium polar extract [MeOH/DCM (1:1, v/v)] was fractionated sequentially with petroleum ether to which EtOAC and MeOH were gradually added to increase the polarity. The examination of T. potatoria extract and its fractions was guided by bioassays for anti-mycobacterial activity against M. smegmatis (ATCC 23246) and M. aurum (NCTC 10437) using the minimum inhibitory concentration (MIC) method. All the isolated compounds were structurally elucidated using spectroscopic techniques and evaluated for their anti-mycobacterial activity. Results Two novel secondary metabolites (1, 2) named tetraceranoate and N-hydroxy imidate-tetracerane, together with five known compounds [β-stigmasterol (3), stigmast-5-en-3β-yl acetate (4), betulinic acid (5), betulin (6) and lupeol (7)] were isolated and identified. Tetraceranoate exhibited the best activity against M. smegmatis with a minimum inhibitory concentration (MIC) of 7.8 µg/mL, while β-stigmasterol, betulinic acid and betulin showed appreciable anti-mycobacterial activity against both strains (MIC 15 µg/mL). Conclusion Seven compounds were isolated from the medium polar extract [MeOH/DCM (1:1, v/v)] of T. potatoria stem bark. Only tetraceranoate one of the isolated compounds showed antibacterial activity against M. smegmatis having efficacy as high as rifampicin (one of a three drug regimen recommended in the initial phase short-course anti-tuberculosis therapy). Thus, tetraceranoate might be an interesting target for systematic testing of anti-TB treatment and management. This research supports the use of T. potatoria in African traditional medicine for the treatment of tuberculosis related symptoms.

Context: Dillenia indica Linn. (Dilleniaceae) is traditionally used to treat skin inflammation. Objective: This study evaluated the healing effect of Dillenia indica fruit extracts on induced psoriasis-like wounds in Wistar rats. Materials and methods: Extracts were standardized to betulinic acid, including an aqueous ethanolic extract (AEE), ethyl acetate extract (EAE) and petroleum ether extract. Effects against lipid peroxidation were assessed in vitro. Wounds were created at rat tails (n = 12). Topical treatments were applied once daily for 7 days (1 mL of AEE or EAE at 5 or 50 mg/mL). Maximal dose was defined by the extract solubility. A 10-fold lower dose was also tested. Positive and negative controls were treated with clobetasol (0.5 mg/mL) or excipient. Half of each group was euthanized for histology. The remaining animals were observed for 20 days for wound measurements. Results: Yields of AEE and EAE were 4.3 and 0.7%, respectively. Betulinic acid concentrations in AEE and EAE were 4.6 and 107.6 mg/g. Extracts neutralized lipid peroxidation in vitro at 0.02 μg/mL, accelerating healing at 50 mg/mL. Complete healing in mice treated with AEE occurred 16 days after wound induction. This time was 14 and 12 days in mice treated with EAE and clobetasol. Compared to orthokeratosis, parakeratosis was reduced by AEE (25%), EAE (45%) and clobetasol (55%). EAE caused superior protection against biomolecules oxidation of skin compared to AEE. Discussion and conclusion: EAE exhibited activity closer to that of clobetasol. Betulinic acid may be an active constituent, which should be assessed in future studies.

This study aimed to evaluate the potential adverse effects of the dermal administration of Dillenia indica Linnaeus (D. indica) fruit extract in healthy rodents; the extract was standardized to betulinic acid. In the initial phase, the acute effects were evaluated on the skin application site of a single extract dose. A skin irritation test was performed in male Wistar rats (n = 8/group) receiving the extract (50-150 mg/mL) with betulinic acid (0.5-1.5%, respectively). A photosensitivity test was performed in male BALB/c mice (n = 6/group) receiving the extract (150 mg/mL). Afterwards, other BALB/c mice (n = 20, male:female, 1:1) were used to assess the systemic alterations caused by 14 daily repeated doses (150 mg/mL) by monitoring the effects on mortality, body morphology, behavior, nutrition status, neuromotor reactions, organ morphology and weight, and blood tests. At this time, 0.5 mg/mL clobetasol was used as the positive control. The skin irritation index suggested that negligible skin irritation had occurred, even when the extract was applied to the rat skin at 150 mg/mL. However, the extract acted as a photosensitizer on mouse skin, showing a photosensitizing activity close to that of 10 mg/mL 5-methoxypsoralen. Repeated doses caused no mouse mortality, aggressiveness, piloerection, diarrhea, convulsions, neuromotor alterations or nutrition status changes. The mouse organ weights did not change, and the mice did not have alterations in their blood compositions. Clobetasol caused a reduction in the mononuclear leukocyte numbers. In general, the data suggest that the extract was safe in healthy rodents but indicate that caution should be taken with the photosensitizing activity; in addition, this activity should be further explored as it may be useful for phototherapeutic drug development.

Dillenia indica Linn. (Dilleniaceae) is generally known as elephant apple and locally known as outenga. The vernacular names are chalta, chulta, bhavya, karambel, ouu, and ramphal. This evergreen deciduous tree is markedly disseminated in the seasonal tropics of many Asian countries, in India from Himalaya to south India. The different parts of this plant have been prevalently investigated for the plethora of biological activities including anticancer, antidiabetic, antihyperlipidemic, antileukemic, antioxidant, antimutagenic, antimicrobial, antinociceptive, antidiarrheal, and hairweaving activities. Differently prepared extracts of this plant have been reported mainly to contain a wide range of flavonoids, triterpenoids (lupene-type), phytosteroids, phenolics, alcohols, and ketones and an anthraquinone. Several phytochemical investigations revealed substantial presence of various types of active constituents including β-sitosterol, stigmasterol, betulin, betulinic acid, kaempferol, myricetin, quercetin, dillenetin and rhamnetin. Among these the major chemical constituents are betulin and betulinic acid (lupene-type triterpenoids) that show a wide spectrum of pharmacological activities like anti-HIV, anticancer, antimalarial, anti-inflammatory, etc. The present chapter thus approaches to highlight on phytochemistry, traditional and therapeutic uses, and biological activities of Dillenia indica.

RESUMO Davilla kunthii A. St. –Hil. (Dilleniaceae) tem ampla distribuição vegetal. Sua família agrega uma quantidade significativa de novas substâncias, bem como importantes atividades biológicas. O uso mais comum é na medicina alternativa para combater algumas doenças, mas estudos comprovam diferentes atividades biológicas de interesse farmacológico. A literatura sobre a bioatividade de D. kunthii é incipiente. Por esta razão, os objetivos deste trabalho se concentraram em verificar os efeitos biológicos do extrato das folhas de D. kunthii, através de bioensaios frente a microrganismos patógenos Escherichia coli, Salmonella tiphymurium (bactérias gram-negativa), Staphylococcus aureus e Streptococcus sanguinis (bactérias gram-positiva), ao fungo tipo levedura Candida albicans e aos fungos filamentosos Aspergillus flavus e Fusarium proliferatum. A pesquisa verificou ainda a atividade redutora da enzima de acetilcolinesterase, e, também, foi observada a atividade antioxidante via DPPH (2,2-difenil-1-picril-hidrazila) e de toxicidade frente ao microcrustáceo A. salina. Os resultados apontaram significativas atividades antioxidante, antimicrobiano, atingindo até 90% de inibição sobre a levedura C. albicans em todas as concentrações.

Ethnopharmacological relevance Dillenia suffruticosa (Family: Dilleniaceae) or commonly known as “ Simpoh air ” in Malaysia, is traditionally used for treatment of cancerous growth including breast cancer. Aim of the study D. suffruticosa root dichloromethane extract (DCM-DS) has been reported to induce G 0 /G 1 phase cell cycle arrest and apoptosis in caspase-3 deficient MCF-7 breast cancer cells. The present study was designed to investigate the involvement of p53/p21 and mitochondrial pathway in DCM-DS-treated MCF-7 cells as well as to identify the bioactive compounds responsible for the cytotoxicity of DCM-DS. Materials and methods Extraction of D. suffruticosa root was performed by the use of sequential solvent procedure. GeXP-based multiplex system was employed to investigate the expression of p53 , p21 , Bax and Bcl-2 genes in MCF-7 cells treated with DCM-DS. The protein expression was then determined using Western blot analysis. The bioactive compounds present in DCM-DS were isolated by using column chromatography. The structure of the compounds was elucidated by using nuclear magnetic resonance spectroscopy. The cytotoxicity of the isolated compounds towards MCF-7 cells was evaluated by using MTT assay. The percentage of betulinic acid (BA) in DCM-DS was determined by HPLC analysis. Results The expression of p53 was significantly up-regulated at protein level. The expression of p21 at both gene and protein levels was significantly up-regulated upon treatment with DCM-DS, suggesting that the induction of G 0 / G 1 phase cell cycle arrest in MCF-7 cells was via p53/p21 pathway. Bcl-2 protein was down-regulated with no change at the mRNA level, postulating that post-translational modification has occurred resulting in the degradation of Bcl-2 protein. Overall, treatment with DCM-DS increased the ratio of Bax/Bcl-2 that drove the cells to undergo apoptosis. A total of 3 triterpene compounds were isolated from DCM-DS. Betulinic acid appears to be the most major and most cytotoxic compound in DCM-DS. Conclusion DCM-DS induced cell cycle arrest and apoptosis in MCF-7 cells via p53/p21 pathway. In addition, DCM-DS induced apoptosis by increasing the ratio of Bax/Bcl-2. Betulinic acid, which is one of the major compounds, is responsible for the cytotoxicity of the DCM-DS. Therefore, BA can be used as a marker for standardisation of herbal product from D. suffruticosa . DCM-DS can also be employed as BA-rich extract from roots of D. suffruticosa for the management of breast cancer.

Dillenia suffruticosa L. (Dilleniaceae) is used in traditional medicine for protection against various diseases. The current study was designed to investigate the bioactive compounds and hepatoprotective potential of methanol leaves extract of D. suffruticosa against carbon tetrachloride (CCl4)-induced hepatic oxidative injury. Sprague Dawley rats were pretreated with methanol extract of D. suffruticosa leaves (200, 300, and 400 mg/kg body weight [bwt]) once daily for 14 days followed by two doses of CCl4 (1.0 mL/kg bwt). After 2 weeks the rats were sacrificed and hepatoprotective analysis was performed. The identified bioactive compounds include phenol (1.39%); benzyl alcohol (2.04%); 2H-pyran-2-one, 4,6-dimethyl (1.19%); phenol, 2,4-bis(1,1-dimethylethyl) (0.83%); dodecanoic acid (0.84%); hexadecanoic acid, methyl ester (2.66%); n-hexadecanoic acid (0.96%); and phytol (2.13%). The administration of D. suffruticosa significantly depleted the elevation of enzymatic levels of alanine transaminase and aspartate transaminase (4% to 59% recovery), reduced the extent of malondialdehyde production (13% to 79% recovery), elevated the level of reduced glutathione (5% to 21% recovery), and increased the activities of antioxidant enzymes (0.43% to 35% recovery). Histopathological analyses by light and electron microscopy revealed that the plant extract protects the liver from the toxic effects of CCl4 and cured lesions such as necrosis and fatty degeneration. It also decreased hepatocyte injuries such as irregular lamellar organization and dilations in endoplasmic reticulum. Immunohistochemical studies indicate the formation of 8-hydroxy-2'-deoxyguanosine (8-OHdG) and 4-hydroxyl-2-nonenal (HNE)-modified protein adducts. In addition, the overexpression of the inflammatory cytokines tumor necrosis factor alpha (TNF-α), interleukin 6 (IL-6), and prostaglandin E2 (PGE2) are reduced. Hence, we find D. suffruticosa to be a good source of bioactive compounds with hepatoprotective effects against CCl4-induced oxidative damage.

The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study

Ethnopharmacological relevance: Dillenia suffruticosa (Family: Dilleniaceae) locally known as Simpoh air has been reported to be used traditionally to treat cancerous growth. Therefore, the present study was attempted to investigate the antioxidant and cytotoxic properties of different parts (root, flower, fruit and leaf) of D. suffruticosa extracts. Methods and materials: In this study, direct solvent extraction (aqueous and methanol) from different parts of D. suffruticosa (root, flower, fruit and leaf) were carried out. Antioxidant activities of D. suffruticosa extract were determined by using DPPH, ABTS FRAP and β-carotene bleaching assays. Cytotoxicity and cell cycle arrest of the active extract were determined using MTT assay and flow cytometer, respectively. Sequential solvent extraction (hexane, DCM, EtOAc, and MeOH) were also carried out in root of D. suffruticosa to further evaluate the antioxidant and cytotoxic activity of the different solvent extracts. Results: Methanol (MeOH) root extract showed the highest TPC, antioxidant and cytotoxic activities (especially towards HeLa) compared to others (P

Introduction: Leaves of mempelas paya (Tetracera indica) (family: Dilleniaceae) is traditionally used in diabetes management in Malaysia. However, no attempt has ever been made to discover an active principle responsible for its blood glucose lowering effect. Hence, this research deals with the isolation, in vivo antidiabetic and toxicological evaluation of an active principle. Methods: Chemical investigation of methanol extract derived from the powdered leaves resulted in the isolation of a phenolic compound through repeated silica gel column chromatography. The structure was elucidated by spectroscopic (1H-NMR, 13C -NMR, MS, IR and UV) analysis. In vivo antidiabetic and toxicological studies were carried out using Sprague -Dawley rats (diabetic and normal) at three different concentrations (1, 5 and 25 mg/kg b.w.). Results: 5,7-dihydroxy-8-methoxyflavone was found to exhibit significant anti-hyperglycaemic activity (p

ObjectiveTo investigate antidiabetic, hypolipidemic histopathological analysis of Dillenia indica (D. indica) methanolic leaves (DIME) extract in alloxan induced diabetic rat by administering oral doses (250 and 500 mg/kg body weight).MethodsBlood glucose levels were measured using blood glucose test strips with elegance glucometer on weekly intervals till the end of study (i.e. 3 weeks). Other parameters e.g. liver profile, renal profile and total lipid levels were determined in normal and alloxan induced diabetic rats after oral administration of the extract for 21 days. Histopathological changes in diabetic rat organs (pancreas, liver and kidney) were also observed after extract treatment.ResultsDaily oral administration DIME (250 and 500 mg/kg body weight) and glibenclamide (10 mg/kg) showed beneficial effects on blood glucose level (P < 0.001) as well as improving kidney, liver functions and hyperlipidaemia due to diabetes. The extract treatment also showed to enhanced serum insulin level and body weight of diabetic rats as compared to diabetic control group. Furthermore, the extract has a favorable effect on the histopathological changes of the pancreas, liver and kidney in alloxan induced diabetes.ConclusionsD. indica possess antidiabetic property as well improve body weight, liver profile, renal profile and total lipid levels. DIME has also favorable effect to inhibit the histopathological changes of the pancreas and kidney in alloxan induced diabetes.

An EtOAc-soluble partition of the MeOH extract of a branch of Tetracera scandens (Dilleniaceae family) was subjected to a glucose-uptake assay, which led to the isolation and identification of five isoflavones of previously known structure namely, genistein (1), its derivatives 3',5'-diprenylgenistein (2), 6,8-diprenylgenistein (3), derrone (4) and alpinumisoflavone (5). Of these, compounds 2--5 exhibited significant glucose-uptake activity in basal and insulin-stimulated L6 myotubes. The findings from adenosine monophosphate-activated kinase (AMPK) activation and glucose transport protein4 (GLUT4) and GLUT1 over-expression revealed certain characteristics of compounds 2--5. These compounds inhibited protein tyrosine phosphatase 1B (PTP1B) activities with IC50 values ranging from 20.63 +/- 0.17 to 37.52 +/- 0.31 microM. No muscle cell toxicity was reported with compounds 3--5, while compounds 1 and 2 reduced muscle cell viability with IC50 values of 34.27 +/- 0.35 and 18.69 +/- 0.19 microM, respectively. It was concluded that T. scandens and its constituents exerted highly desirable activities on type 2 diabetes mellitus treatment since they significantly stimulated the uptake of glucose, AMPK phosphorylation, GLUT4 and GLUT1 mRNA expressions and PTP1B inhibition in L6 myotubes.

Dillenia indica f. elongata (Miq.) Miq. (Dilleniaceae) commonly known as Elephant apple. The vernacular names include Chalta, Chulta, Karambel, Bhavya and Ramphal.It is found in Bangladesh, Nepal, China, Indonesia and Assam, West Bengal, Orissa, Bihar, Myanmar regions of India. Dillenia indica f. elongata (Miq.) Miq. has been prevalently used in Indian traditional and ayurvedic medicine for curing plethora of ailments such as digestive, respiratory and central nervous systems. The information was put together, with the help of literature surveyed. Traditionally different parts of Dillenia indica f. elongata (Miq.) Miq. have been used for the relief of indigestion, asthma, influenza, dysentery,jaundice,promeho,weakness and rheumatic pain. Moreover, the extractives showed significant cytotoxic, CNS depressant and free radical scavenging activity. Wood obtained from the bark of the plant has been used for preparing rafters, tool-handles, cupboard and house pots. It is interesting to know that bark of Dillenia indica f. elongata (Miq.) Miq. is used for production of charcoal. Microspheres of metformin hydrochloride and novel mucoadhesive buccal tablets of oxytocin were also prepared from Dillenia indica f. elongata (Miq.) Miq. In vitro propagation is practised whereas micropropagation is considered at the time, when large scale plant multiplication is required. Phytochemical studies revealed substantial presence of polyphenols, tannins, alkaloids and flavanoids which are responsible for the various pharmacological activities. Major chemical constituents present in the plant are betulin (pentacyclic triterpenoid) and betulinic acid that show wide spectrum of pharmacological activities which include anti-HIV, anti-inflammatory, anti-cancer, anti-malarial etc. Furthermore, Dillenia indica f. elongata (Miq.) Miq. is found to possess analgesic, anti-diabetic, anti- microbial,anti-bacterial,anti-diabetic,anti-oxidant,anti-proliferation,anti-diarrhoeal, antiimplantation, cytotoxic, wound healing and hair waving activity. Keyword(s)- Dillenia indica f. elongata (Miq.) Miq . ; Phytochemical profile; Traditional uses; Pharmacological properties.

High levels of reactive oxygen species in the body and hyperlipidemia are key factors for the development of cardiovascular diseases such as atherosclerosis. The present study investigated the antioxidant and hypolipidemic activity of hydroethanolic extract ofCuratella americanaL. leaves (ExC). The antioxidant activity of ExC was assessed by 2,2-diphenyl-1-picrylhydrazyl free radical (DPPH) scavenging capacity and protection against hemolysis induced by 2,2′-azobis(2-amidinopropane) dihydrochloride (AAPH), followed by quantification of malondialdehyde (MDA). Wistar rats with hyperlipidemia induced by high-fructose diet (60%) were treated for 60 days with water, simvastatin (30 mg·Kg−1), ciprofibrate (2 mg·Kg−1), and ExC (200 mg·Kg−1). ExC revealed IC50of6.0±0.5 μg·mL−1, an intermediary value among positive controls used in the assay of DPPH scavenging capacity. At all concentrations (50 to 125 μg·mL−1) and times (60 to 240 min) evaluated, ExC protected erythrocytes against AAPH-induced hemolysis, which was confirmed by lower MDA levels.In vivotests showed a reduction of 34 and 45%, respectively, in serum concentration of cholesterol and triglycerides in hyperlipidemic rats treated with ExC, a similar effect compared to the reference drugs, simvastatin and ciprofibrate, respectively. Together, the results showed the antioxidant activity of ExC and its ability to improve the serum lipid profile in hyperlipidemic rats.

Ethnopharmacological relevance Dillenia suffruticosa is traditionally used for treatment of cancerous growth including breast cancer in Malaysia. Aim of the study Dillenia suffruticosa is a well-known medicinal plant in Malaysia for the treatment of cancer. Nevertheless, no study has been reported the cytotoxicity of this plant towards MDA-MB-231 triple-negative breast cancer cells. The present study was designed to investigate the mode of cell death and signalling pathways of MDA-MB-231 cells treated with dichloromethane Dillenia suffruticosa root extract (DCM-DS). Methods Extraction of Dillenia suffruticosa root was performed by the use of sequential solvent procedure. The cytotoxicity of DCM-DS was determined by using MTT assay. The mode of cell death was evaluated by using an inverted light microscope and flow cytometry analysis using Annexin-V/PI. Cell cycle analysis and measurement of reactive oxygen species level were performed by using flow cytometry. The cells were treated with DCM-DS and antioxidants α-tocopherol or ascorbic acid to evaluate the involvement of ROS in the cytotoxicity of DCM-DS. Effect of DCM-DS on the expression of antioxidant, apoptotic, growth, survival genes and proteins were analysed by using GeXP-based multiplex system and Western blot, respectively. The cytotoxicity of compounds isolated from DCM-DS was evaluated towards MDA-MB-231 cells using MTT assay. Results DCM-DS induced apoptosis, G 2 /M phase cell cycle arrest and oxidative stress in MDA-MB-231 cells. The induction of apoptosis in MDA-MB-231 cells by DCM-DS is possibly due to the activation of pro-apoptotic JNK1 and down-regulation of anti-apoptotic ERK1, which in turn down-regulates anti-apoptotic BCL-2 to increase the BAX/BCL-2 ratio to initiate the mitochondrial apoptotic pathway. The cell cycle arrest in DCM-DS-treated MDA-MB-231 cells is possibly via p53-independent but p21-dependent pathway. A total of 3 triterpene compounds were isolated from DCM-DS. Betulinic acid appears to be the most major and most cytotoxic compound in DCM-DS. Conclusion The data suggest the potential application of DCM-DS in the treatment of triple-negative breast cancer.

Inflammation and haemorrhage are the main characteristics of tissue injury in botropic envenomation. Although some studies have shown that anti-venom prevents systemic reactions, it is not efficient in preventing tissue injury at the site of the bite. Therefore, this work was undertaken to investigate the anti-inflammatory effects of the methanolic extract and fractions from D. elliptica and to evaluate the role of matrix metalloproteinases (MMPs) in this process. Effects of the extract and fractions from D. elliptica were evaluated using a carrageenan-induced paw oedema model in rats, and leukocyte rolling was visualized by intravital. The quantification of MMPs activities (MMP-2 and MMP-9) extracted from the dermis of mice treated with extract and fractions alone or incubated with venom was determined by zymographic analyses. Our results show that intraperitoneal (i.p.) injection of fractions significantly reduced paw oedema after the carrageenan challenge. Treatment with the tannins fraction also resulted in considerable inhibition of the rolling of leukocytes and this fraction was able to decrease the activation of MMP-9. These results confirmed the anti-inflammatory activity of the methanolic extract and tannins fraction of D. elliptica and showed that the dermonecrosis properties of B. jararaca venom might be mediated through the inhibition of MMP-9 activity.

A new lupane-triterpene acid ester, dillenic acid (I), is isolated along with four known compounds from the stem bark of Dillenia indica Linn (Dilleniaceae).

The ethnomedicinal plantCuratella americanaL. (Dilleniaceae) is a common shrub in the Brazilian cerrado, in which crude extract showed antifungal activity in a preliminary study. In this work, the antifungal and cytotoxic properties of the crude extract, fractions, and isolated compounds fromC. americanawere evaluated against the standard yeast strainsCandida albicans,C. tropicalis, andC. parapsilosis, clinical isolates, and fluconazole-resistant strains. The combinatory effects between subfractions and isolated compounds and effects on cell morphology, virulence factors, and exogenous ergosterol were also evaluated. The MIC obtained against theCandidaspecies including fluconazole-resistant strain ranged from 15.3 to 31.3 µg/mL for crude extract, 3.9 to 15.6 µg/mL for ethyl acetate fraction, and 7.8 to 31.3 µg/mL for subfractions. The isolated compounds identified as 4′-O-methyl-catechin, epicatechin-3-O-gallate, and 4′-O-methyl-catechin-3-O-gallate showed lower antifungal activity than the crude extract and fractions (MIC ranging from 31.3 to 125.0 µg/mL). The addition of exogenous ergosterol to yeast culture did not interfere in the antifungal activity of the extract and its fractions. Synergistic antifungal activity was observed between subfractions and isolated compounds. The effects on virulence factors and the different mechanisms of action compared to fluconazole and nystatin suggest that this ethnomedicinal plant may be an effective alternative treatment for candidiasis.

Davilla rugosa Poiret (“Cipo- Caboclo”) is commonly used in Brazilian folk medicine. The hydroalcoholic extract of the stems (HE) was fractionated with chloroform (CF), chloroform/ethyl acetate (CAF), ethyl acetate (AF), ethyl acetate/ethanol (AEF), ethanol (EF), and ethanol/water (EWF). The hydroalcoholic extract (HE) and fractions of the stems of D. rugosa Poiret were investigated for possible anti gastric ulcer properties. These extracts were shown to protect rats from developing gastric ulcers induced by two acute models: HCl/ethanol (400 mg/kg i.p.) and immersion-restraint stress (15 and 30 mg/kg of the HE and 15 mg/kg either of the ethanol or the ethanol/water fractions, p.o.). The daily oral dose of 800 mg/kg of HE for 30 consecutive days was tested for possible toxic effects. There were no modifications in body weight, water or food intake or in the external aspect of kidneys, spleen, lungs and liver. The only difference observed was a decrease of liver weight. These results suggest that the D. rugosa Poiret HE has an antiulcer activity in rats and the active components are in the two more polar fractions.

Tetracera scandens Linn. (Dilleniaceae), locally known as Mempelas Kasar, is traditionally used in folk remedies by various indigenous people in different countries including Malaysia for the treatment of rheumatism, inflammatory diseases, hepatitis, internal pains, urinary disorders, dysentery, sore throat, gout and diabetes infirmities; for lowering hypertension; and for child birth. In this study, phytochemical analysis of T. scandens leaf methanol (MeOH) extract was carried out for the first time and afforded three terpenoids (stigmasterol, betulinic acid and an isomeric mixture of sitosterol (∆5) glycoside and stigmasterol (∆5,22) glycoside) and six flavonoids (namely, kaempferol, quercetin, isoscutellarein, hypoletin, astragalin and kaempferol-3-O-(6″-O-p-trans-coumaroyl) glucoside, a rare compound which has been isolated for the first time from family Dilleniaceae). Structures of all compounds were elucidated through extensive UV–Vis, mass, IR and NMR spectral analysis. The occurrence of all these compounds is being reported for the first time from this plant. Due to the rare occurrence of hypoletin (3′,4′,5,7,8-pentahydroxyflavone) in plants, its in vitro antidiabetic effect was explored. Hence, the treatment of hypoletin in a dose-dependent manner was examined on the induction of lipid accumulation by using Oil Red O staining and glucose regulation in 3T3-L1 adipocytes in vitro with regard to its preventive role in the management of diabetes. After 8 days, morphological changes and high lipid accumulation activity were observed in cells treated with 10 μg/mL of hypoletin concentration (P < 0.01). In addition, the intracellular fat accumulation increased by up to 79.7 % relative to MDI-treated control cells at a dose of 10 μg/mL. Furthermore, insulin-induced 2-deoxy-d-[3H] glucose uptake was significantly increased (P < 0.001) in hypoletin-treated cells as compared to control (DMSO cells). Our results suggest that hypoletin could be useful for the management of type 2 diabetes due to its adipocyte stimulation and glucose uptake activity.

Aims. This study was designed to investigate the enzyme inhibitory and antidiabetic activity for the constituents isolated fromDillenia indica.Methods. The leaves ofD. indicawere extracted with methanol and subjected to fractionation and chromatographic separation, which led to the isolation of seven compounds: betulinic acid (1), n-heptacosan-7-one (2), n-nonatriacontan-18-one (3), quercetin (4),βsitosterol (5), stigmasterol (6), and stigmasteryl palmitate (7). Among these isolates, compounds1,4,5, and6were evaluated forin vitroenzyme inhibition and compounds4,5and6were evaluated for antidiabetic activity in streptozotocin-nicotinamide induced diabetic mice.Results. Compounds1,4,5, and6showed 47.4, 55.2, 48.8, and 44.3%α-amylase inhibition, respectively, and 52.2, 78.2, 52.5, and 34.2%α-glucosidase inhibition, respectively, at the dose of 50 µg/kg. Compounds4,5and6also showed significant (*P<0.05) antidiabetic activity in streptozotocin-nicotinamide induced diabetic mice at the dose of 10 mg/kg.Conclusion.These results provide evidence thatDillenia indicamight be a potential source of antidiabetic agents.

Ethnopharmacological relevance Davilla elliptica St.-Hil. (Dilleniaceae) is a medicinal plant traditionally used in Brazil to treat inflammatory processes, to relieve pain, as diuretic, gastro- and hepatoprotective agents. Aim of the study To undertake the fractionation of the ethanolic extract from Davilla elliptica leaves guided by an antinociceptive assay. Materials and methods The antinociceptive activity was evaluated through the formalin test in mice. Extract fractionation was performed by percolation through silica gel and partition between immiscible solvents, followed by successive column chromatography over Sephadex LH-20 and preparative RP-HPLC. Structure elucidation of the isolated compound was accomplished by spectroscopic data. Results The EtOAc and MeOH fractions derived from the crude extract reduced significantly the licking time in the late phase of the formalin test. The bioguided fractionation of the MeOH fraction resulted in the isolation of myricetin-3-O-β-galactopyranoside, which produced significant inhibition on nociception induced by formalin (ID50=0.26 mg/kg; p.o.). Conclusions These results point out that myricetin-3-O-β-galactopyranoside contributes for the antinociceptive effect of Davilla elliptica extract, a constituent considerably more potent than diclofenac, employed as reference drug.

The in vitro antileishmanial activity of triterpenes and lignans of an Amazonian medicinal plant, Doliocarpus dentatus (Aublet) Standley, is reported for the first time against amastigotes of Leishmania amazonensis. Terpenes, for example, betulinic acid, betulin and betulinaldehyde were isolated by bioassay-linked extraction. The lignans were characterized as (+) pinoresinol, (+) medioresinol and (-) lirioresinol B.

Knowing keratin is the main component and mechanical strength of hair a study was performed to evaluate whether Dillenia indica seed sap can affect molecular strength of hair or not. In the present study the human hair collected from barber shop waste were subjected to purified sap for 12 h and then analysed using Fourier transform infrared spectroscopy (FTIR) for documenting evidence for keratin degradation. Further the deterioration was confirmed by thermo gravimetric analysis (TGA) and scanning electron microscopy (SEM).

From the MeOH extract of the stem of Tetracera scandens L., a new nor-lupane triterpene, 28-O-β-D-glucopyranosyl ester of platanic acid (1), has been isolated together with six known compounds. Their structures were elucidated on the basis of spectroscopic data. Compounds 1-6 displayed significant xanthine oxidase inhibitory activity in a concentration-dependent manner, and compound 4 showed more potent inhibitory activity with an IC(50) value of 1.9 µM than that of a positive control allopurinol (IC(50) 2.5 µM).

OBJECTIVE The present study was carried out to investigate the antidiabetic and hypolipidemic activities of bioactive fraction (ethyl acetate fraction) of Dillenia indica methanolic extract in experimental diabetic Wistar rats. METHODS Type-1 diabetes was induced by single intraperitoneal injection of streptozotocin (60 mg/kg body weight), and type-2 diabetes was induced by single intraperitoneal injection of streptozotocin (60 mg/kg body weight), 15 min after the intraperitoneal injection of 120 mg/kg nicotinamide. The rats were treated by administering graded oral doses of isolated ethyl acetate fraction of methanolic extract of D. indica (DIEE), 200 and 400 mg/kg body weight, respectively, for 21 d. The blood glucose level was estimated at weekly intervals by glucometer. Serum cholesterol, triglycerides and high-density lipoprotein cholesterol (HDL-C) were also evaluated in normal and diabetic rats by an autoanalyzer. RESULTS In both experimental models, daily oral treatment with DIEE for 21 d resulted in a significant reduction in blood glucose (P

The leaves of the endemic Philippine plant, Dillenia philippinensis yielded 11 compounds including one new sulfated glucoside and a new seco-A-ring oleanane-type triterpenoid. The molecular structures of these compounds were elucidated by means of NMR, MS and other spectroscopic techniques, as well as by comparison with literature data. Anti-Leishmania activity and cytotoxic activity against A549 human lung adenocarcinoma cells were also examined.

Aim of the study The present study was aimed to investigate the anti-diabetic potential of the leaves of Tetracera scandens Linn. Merr. (Dilleniaceae) in vivo with regard to prove its efficacy by local herbalists in the treatment of diabetes frailties. Materials and methods Crude aqueous (AQ) and methanol (MEOH) extracts of the leaves of T. scandens L. were administered to both normal and alloxan induced diabetic male albino rats (Wistar strain). The blood glucose levels were measured at 0, 2, 4, 6 and 8 h after oral administration of AQ and MEOH extracts. Results Significant reduction in glucose was observed in fasting blood glucose levels in the treated diabetic rats without causing any hypoglycemic effect compared to normal rats. Both polar extracts of the leaves of T. scandens L. exhibited significant anti-hyperglycemic activity at different doses and intervals. The highest anti-hyperglycemic effect (62.5%) was observed by the AQ extract at 0.25 g/kg body weight (b.w.) and MEOH extract (36.5%) at 0.5 g/kg b.w. after 8 h. The significant anti-hyperglycemic activity was found to be comparable with a known oral synthetic hypoglycemic drug, glibenclamide 0.25 mg/kg b.w. Conclusion This study provides scientific evidence that the leaves of T. scandens L. have anti-diabetic efficacy and justifies its utility by local herbalists. However, more experiments at the clinical levels are required to confirm the utility of this plant by traditional practitioners in the management of diabetes mellitus.

Davilla nitida and Davilla elliptica (Dilleniaceae) are plants that occur predominantly in the cerrado region of South America. They are used in popular medicine to treat stomach diseases, diarrhea and swelling, particularly of the lymph nodes and testicles. Chemical investigation of these two plant species led to the identification of the compounds myricetin-3-O-α-l-rhamnoside (myricitrin), quercetin-3-O-α-l-rhamnoside (quercitrin), myricetin, quercetin and gallic acid derivatives in the leaves of D. nitida and D. elliptica. Therefore, it was concluded that the two species of Davilla possess qualitatively similar chemical profiles. In the present study, the mutagenic and genotoxic potential of these plants and of their isolated compounds was tested in the Salmonella typhimurium assay (Ames test) with strains TA100, TA98, TA102 and TA97a, in the micronucleus test with peripheral blood cells of mice treated in vivo, and in plasmid DNA to analyze DNA strand-breaks. In the assessment of mutagenic potential by the Ames test, extracts from both plant species and a D. nitida ethyl-acetate fraction induced positive responses. On the other hand, none of the extracts showed genotoxic activity in the mouse cells. In the presence of metal ion, D. nitida and D. elliptica aqueous and ethyl-acetate fractions, as well as their isolated compounds, induced single- and double-strand-breaks in plasmid DNA in a cell-free system.

The methanolic extract of Dillenia indica L. fruits showed significant anti-leukemic activity in human leukemic cell lines U937, HL60 and K562. This finding led to fractionation of the methanolic extract, on the basis of polarity, in which the ethyl acetate fraction showed the highest anti-leukemic activity. A major compound, betulinic acid, was isolated from the ethyl acetate fraction by silica gel column chromatography and was identified and characterized. Betulinic acid could explain the anti-leukemic activity of the methanolic extract and the ethyl acetate fraction. Hence the quantitative estimation of betulinic acid was approached in methanolic extract and fractions using HPLC.

Made available in DSpace on 2013-08-28T14:12:26Z (GMT). No. of bitstreams: 1 WOS000264565000014.pdf: 119866 bytes, checksum: 80217037ccfd8ca2d39ea1accf4c27bc (MD5) Made available in DSpace on 2013-09-30T19:10:41Z (GMT). No. of bitstreams: 2 WOS000264565000014.pdf: 119866 bytes, checksum: 80217037ccfd8ca2d39ea1accf4c27bc (MD5) WOS000264565000014.pdf.txt: 24181 bytes, checksum: 056565f08078e2cf0d624eb8c0faa588 (MD5) Previous issue date: 2009-03-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:49:52Z No. of bitstreams: 2 WOS000264565000014.pdf: 119866 bytes, checksum: 80217037ccfd8ca2d39ea1accf4c27bc (MD5) WOS000264565000014.pdf.txt: 24181 bytes, checksum: 056565f08078e2cf0d624eb8c0faa588 (MD5) Made available in DSpace on 2014-05-20T13:49:53Z (GMT). No. of bitstreams: 2 WOS000264565000014.pdf: 119866 bytes, checksum: 80217037ccfd8ca2d39ea1accf4c27bc (MD5) WOS000264565000014.pdf.txt: 24181 bytes, checksum: 056565f08078e2cf0d624eb8c0faa588 (MD5) Previous issue date: 2009-03-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Around 20,000 snakebites are reported annually in Brazil and 90% of them are inflicted by species of the genus Bothrops. Intravenous administration of antibothropic antivenom neutralizes the systemic actions, but it is of little effect on the reversal of local symptoms and often induces adverse reactions, a context that drives the search for complementary treatments for snakebite accidents. Vegetable extracts with a range of antiophidian activities constitute an excellent alternative. In this study, we investigated the anti-hemorrhagic effects of Mouriri pusa Gardn. (Melastomataceae), Byrsonima crassa Niedenzu (Malpighiaceae), Davilla elliptica St. Hill. (Dilleniaceae) and Strychnos pseudoquina St. Hil. (Loganiaceae) against Bothrops jararaca venom. The methanolic extracts from M. pusa (leaves), B. crassa (leaves) and D. elliptica (leaves) showed total neutralization capacity against local hemorrhages. The amenthoflavone and quercetin fractions from B. crassa and the flavonoids fractions (quercetin and myricetin) from M. pusa and D. elliptica also showed total neutralization capacity. We conclude that flavonoids derived from myricetin, quercetin and amenthoflavone play an important role in the anti-hemorrhagic potential of these Brazilian vegetables species against B. jararaca venom. São Paulo State Univ, UNESP, Dept Physiol, Botucatu, SP, Brazil São Paulo State Univ, UNESP, Dept Organ Chem, Araraquara, SP, Brazil Ctr Appl Toxinol, Instituto Butantan, São Paulo, Brazil São Paulo State Univ, UNESP, Dept Physiol, Botucatu, SP, Brazil São Paulo State Univ, UNESP, Dept Organ Chem, Araraquara, SP, Brazil

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:48:37Z No. of bitstreams: 1 S0100-40422006000500011.pdf: 172804 bytes, checksum: 37748f06447925b80cf74b36f09a67bc (MD5) Made available in DSpace on 2013-08-22T18:48:37Z (GMT). No. of bitstreams: 1 S0100-40422006000500011.pdf: 172804 bytes, checksum: 37748f06447925b80cf74b36f09a67bc (MD5) Previous issue date: 2006-10-01 Made available in DSpace on 2013-09-30T19:10:46Z (GMT). No. of bitstreams: 2 S0100-40422006000500011.pdf: 172804 bytes, checksum: 37748f06447925b80cf74b36f09a67bc (MD5) S0100-40422006000500011.pdf.txt: 16020 bytes, checksum: 6ef9c793c210961b4642bf0707f967be (MD5) Previous issue date: 2006-10-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T14:21:19Z No. of bitstreams: 2 S0100-40422006000500011.pdf: 172804 bytes, checksum: 37748f06447925b80cf74b36f09a67bc (MD5) S0100-40422006000500011.pdf.txt: 16020 bytes, checksum: 6ef9c793c210961b4642bf0707f967be (MD5) Made available in DSpace on 2014-05-20T14:21:19Z (GMT). No. of bitstreams: 2 S0100-40422006000500011.pdf: 172804 bytes, checksum: 37748f06447925b80cf74b36f09a67bc (MD5) S0100-40422006000500011.pdf.txt: 16020 bytes, checksum: 6ef9c793c210961b4642bf0707f967be (MD5) Previous issue date: 2006-10-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) High-speed counter-current chromatography (HSCCC) is a major tool for the fast separation of natural products from plants. It was used for the preparative isolation of the flavonoid monoglucosides present in the aerial parts of the Davilla elliptica St. Hill. (Dilleniaceae). This species is used in Brazilian folk medicine for the treatment of gastric disorders. The optimum solvent system used was composed of a mixture of ethyl acetate-n-propanol-water (140:8:80, v/v/v) and led to a successful separation of quercetin-3-O-alpha-L-rhamnopyranoside and myricetin-3-O-alpha-L-rhamnopyranoside in approximately 3.0 hours with purity higher than 95%. Identification was performed by ¹H NMR, 13C NMR and HPLC-UV-DAD analyses. Universidade Estadual Paulista Instituto de Química Departamento de Química Orgânica Universidade Estadual Paulista Instituto de Biociências Departamento de Fisiologia Universidade Estadual de Campinas Instituto de Biologia Departamento de Fisiologia e Biofísica Universidade Estadual Paulista Instituto de Química Departamento de Química Orgânica Universidade Estadual Paulista Instituto de Biociências Departamento de Fisiologia