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Albizia lebbeck (L.) Benth. (Family: Mimosaceae) is commonly known as Sirisha in Sanskrit. The leaves and pods of A. lebbeck were claimed to be used against cancer in traditional medicine. Previous studies using bark, leaves, seeds and pods of A. lebbeck showed cytotoxic activity against hepatic, colon, larynx, cervical and breast cancer cell lines.To evaluate the anticancer activity of saponin rich fraction of Albizia lebbeck by using various in vitro models.Albiziasaponins (A-E) are oleanene triterpene presents in Albizia lebbeck were used for in silico studies. In silico testing of albiziasaponins for structure based pharmacological activity prediction using PASS Online software and docking with Autodock tool and Autodock Vina revels it's anticancer and apoptogenic potential. Antiproliferative activity of saponin rich fraction of A. lebbeck was performed using MCF-7 human breast cancer cells by MTT assay methods. Anti-angiogenic property of saponin rich fraction of A. lebbeck was evaluated in in vitro shell less chick embryo cultures with different concentrations (0.1 µg/ml, 0.5 µg/ml, and 1 µg/ml) by using ImageJ software. In vitro cultured lymphocytes chromosomal aberration assay was performed to determine the physical integrity of chromosomes in cells and effect of saponin rich fraction of A. lebbeck on cell cycle. Apoptogenic potential was evaluated using Caspases-3 and Caspase-8 ELISA assay in MCF-7 cells.Result of MTT assay showed IC50 of saponin rich fraction of A. lebbeck at 1 μg/ml in MCF-7 cells. Treatment with saponin rich fraction of A. lebbeck significantly (p 0.05) reduced angiogenic parameters. Significant chromosomal aberrations (hypodiploid, hyperdiploid, ring, premature separation, Dicentric fragments, Acentric fragment, chromatid break, and chromosomal gap) were observed in saponin rich fraction of A. lebbeck treated groups. Treatment with saponin rich fraction of A. lebbeck increased levels of Caspases-3 (optical density of 0.24 at 450 nm) and Caspase-8 (optical density of 0.31 at 450 nm) as compared to staurosporine (optical density of 2.47 and 2.65 for caspases-3 and -8 respectively at 450 nm).In our study, saponin rich fraction of A. lebbeck showed antiproliferative, antiangiogenic and apoptogenic potential using various in-vitro models. It also found to increase chromosomal aberration and thereby may affect cell cycle.

Ethnopharmacological relevance The use of plant extracts and their phytochemicals as candidates for targeting the microbial resistance inhibition is increasingly focused in last decades. In Mongolian traditional medicine, Irises were long used for the treatment of bacterial infections. Irises have been used since the Ancient Egyptians. Aim of the study Chemical composition and virulence inhibition potential of both polar (PF) and non-polar fractions (NPF) of three common Iris species (I. confusa, I. pseudacorus and I. germanica) were explored. Material and methods Secondary metabolites profiling was characterized by the UPLC-HRMS/MS technique. Multi-variate data analysis was performed using Metaboanalyst 3.0. Anti-virulence inhibitory activity was evaluated via anti-haemolytic assay and Quantitative biofilm inhibition assay. Results I. pseudacorus PF exhibited the most potent effect against S. aureus haemolytic activity. All the tested fractions from all species, except I. pseudacorus NPF, have no significant inhibition on the biofilm formation of methicillin resistant and sensitive (MRSA and MSSA) S. aureus. I. pseudacorus NPF showed potent biofilm inhibitory potential of 71.4 and 85.8% against biofilm formation of MRSA and MSSA, respectively. Metabolite profiling of the investigated species revealed ninety and forty-five metabolites detected in the PFs and NPFs, respectively. Nigricin-type, tectorigenin-type isoflavonids and xanthones allowed the discrimination of I. pseudacorus PF from the other species, highlighting the importance of those metabolites in exerting its promising activity. On the other hand, triterpene acids, iridals, triacylglycerols and ceramides represented the metabolites detected in highest abundance in I. pseudacorus NPF. Conclusions This is the sole map represents the secondary metabolites profiling of the PFs and NPFs of common Iris species correlating them with the potent explored Staphylococcus aureus anti-virulence activity.

Ethnopharmacological relevance Careya arborea Roxb. (Lecythidaceae) is a large tree found throughout India in deciduous forests and grasslands. C. arborea is traditionally used in tumors, inflammation, anthelmintic, bronchitis, epileptic fits, astringents, antidote to snake-venom, skin disease, diarrhea, dysentery with bloody stools, dyspepsia, ulcer, tooth ache, and ear pain. Aim of the study In our previous work, the methanolic extract of Careya arborea stem bark showed significant anti-inflammatory activity. As a continuity of that work, this study aimed at the isolation and evaluation of the anti-inflammatory effect of coumaroyl lupendioic acid, a new lupane-type triterpene from Careya arborea stem bark. Further, to give an insight into the underlying mechanism of action of the compound on the modulation of proinflammatory mediators. Materials and methods Methanolic extract of Careya arborea stem bark was suspended in water, and sequentially fractionated with n-hexane and ethyl acetate. Further ethyl acetate fraction was subjected to medium pressure liquid chromatography (MPLC) to isolate the active molecules. The isolated compounds were characterized by the various spectral techniques namely UV, IR, 1H NMR, 13C NMR, DEPT, 1H–1H COSY, HMBC and Mass spectral techniques. In vitro COX-1 and COX-2 enzyme inhibition assays using human whole blood was performed to investigate the inhibitory effect of the isolated compounds. The resulted potent COX-2 inhibitor of the isolated constituents compound 5, designated as coumaroyl lupendioic acid (CLA), was investigated in carrageenan induced inflammation and its effect was also compared with betulinic acid (BA) at the doses of 10 and 20 mg kg−1, p.o. using indomethacin and celecoxib (10 and 20 mg kg−1, p.o., respectively) as reference drugs. The effect of CLA on the production of NO, MPO, PGE2, TNF-α, IL-1β and IL-6 were assessed. In addition, the histopathology and immunohistochemistry (NF-ҡB, COX-2 and TNF-α protein expression) in paw tissues were also carried out. Results The chromatographic fractionation of the methanolic extract resulted in isolation of six new derivatives of lupane type triterpenes for the first time from the stem bark of C. arborea; 3β-hydroxy-lup-5,20 (29),21-trien-28-oic acid (Compound 1), 1, 3, 13, 16-tetrahydroxy-lup-9(11), 20(29)-diene-28-oic acid (Compound 2), 1, 7-di hydroxy betulinic acid (Compound 3), 3β-O-dihydrocinnamyl betulinic acid (Compound 4), 3β-O-trans-coumaryl-lup-6, 9(11), 20(29)-triene-27, 28-dioic acid (Compound 5), 16β-hydroxy-2, 3-seco-lup-5, 20(29)-dien-2, 3, 28-trioic acid (Compound 6). Among the all isolated compounds 3β-O-trans-coumaryl-lup-6, 9(11), 20(29)-triene-27, 28-olioic acid designated as coumaroyl lupendioic acid (CLA) showed higher COX-2 selectivity which is comparable to reference drug (celecoxib). CLA significantly reduced carrageenan induced inflammation whereas CLA revealed greater effect as compared to BA at the similar corresponding doses. Moreover, CLA significantly inhibited pro-inflammatory mediators elevated by carrageenan. CLA also preserved the tissue architecture as evidenced by the histopathology. Furthermore, immunohistochemical studies revealed that CLA significantly down regulated NF-ҡB, COX-2 and TNF-α protein expression. Conclusion The study gives an insight into the molecular mechanisms of coumaroyl lupendioic acid and suggests that the down-regulations of proinflammatory mediators provide credence to the ethno botanical use of the plant in the management of inflammation.

Ethnopharmacological relevance The dried rhizome of Cimicifuga heracleifolia Kom. (C. heracleifolia) is a popular traditional Chinese medicine, which has been extensively used in Asian countries for its anti-inflammatory, antipyretic and analgesic activities. However, further utilization and application of C. heracleifolia have been hampered due to a lack of full understanding of its active ingredients. Aim of study The present study aims for clarification of the systematical chemical profile of C. heracleifolia and the immunomodulatory effect of its main bioavailable component. Materials and methods Comprehensive chemical profile of C. heracleifolia was systematically analyzed by ultra-performance liquid chromatography hyphenated with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF/MS). Xenobiotics after oral administration of C. heracleifolia extracts were investigated to hunt for bioavailable components. The immunomodulatory activity evaluation of cimigenoside was achieved on poly(I:C)-induced airway inflammation mouse and BEAS-2B cell models from aspects of neutrophil infiltration, lung inflammation by using microscope analysis, quantification of production and expression of inflammatory cytokine and chemokines by using ELISA and quantitative PCR. Results By UPLC-Q-TOF/MS analysis, 110 compounds (including 81 triterpenoids, 21 cinnamic acid derivatives, and 8 other structure types) were identified or tentatively characterized in ethanolic extract of C. heracleifolia. Based on the data of chemical profile, xenobiotics of C. heracleifolia were subsequently analyzed, and triterpene glycosides were detected as the major bioavailable ingredients. Oral administration of cimigenoside, a representative triterpene glycoside, could prevent neutrophils infiltration in the lung due to suppression of the production of CXCL2 and CXCL10, and the expression of P-selectin, VCAM1 in poly(I:C)-induced airway inflammation model mice. Moreover, cimigenoside also inhibited the productions of inflammatory cytokines and chemokines from human airway epithelial cell line (BEAS-2B cells) induced by poly(I:C). Conclusion Triterpene glycosides were the main components of C. heracleifolia extract, and cimigenoside was considered as the effective component with immunomodulatory effect on the pulmonary immune system by oral administration.

Ethnopharmacological relevance Chiang-Da, Gymnema inodorum (Lour.) Decne. (GI), is an ethnomedicinal plant that has been used for diabetic treatment since ancient times. One of the anti-diabetic mechanisms is possibly related to the actions of triterpene glycoside, (3β, 16β)-16,28-dihydroxyolean-12-en-3-yl-O-β-D-glucopyranosyl-β-D-glucopyranosiduronic acid (GIA1) in decreasing carbohydrate digestive enzymes and intestinal glucose absorption in the gut system. Aims of the study To observe the amount of GIA1 in GI leaf extracts obtained from different ethanol concentrations and to investigate the anti-hyperglycemic mechanisms of the extracts and GIA1. Materials and methods The crude extracts were prepared using 50%v/v to 95%v/v ethanol solutions and used for GIA1 isolation. The anti-hyperglycemic models included in our study examined the inhibitory activities of α-amylase/α-glucosidase and intestinal glucose absorption related to sodium glucose cotransporter type 1 (SGLT1) using Caco-2 cells. Results GIA1 was found about 8%w/w to 18%w/w in the GI extract depending on ethanol concentrations. The GI extracts and GIA1 showed less inhibitory activities on α-amylase. The extracts from 75%v/v and 95%v/v ethanol and GIA1 significantly delayed the glycemic absorption by lowering α-glucosidase activity and glucose transportation of SGLT1. However, the 50%v/v ethanolic extract markedly decreased the α-glucosidase activity than the SGLT1 function. Conclusion Differences in the GIA1 contents and anti-glycemic properties of the GI leaf extract was dependent on ethanol concentrations. Furthermore, the inhibitory effects of the 75%v/v and 95%v/v ethanolic extracts on α-glucosidase and SGLT1 were relevant to GIA1 content.

Ethnopharmalogical relevance Callicarpa nudiflora Hook. & Arn. is a perennial evergreen shrub or low arbor in the Genus Callicarpa. Its dried aerial parts are used as traditional Chinese herbal medicine, Luo-hua-zi-zhu (Callicarpa nudiflora), which has been widely used in anti-bacteria and anti-ulcer in China (Commission, 2015; Development, 1994; Ming-Sheng, 2008). Aim of the study The present paper reviewed findings in phytochemistry and pharmacology of Callicarpa nudiflora. Methods Chinese and English studies on Callicarpa nudiflora were collected from databases including Web of Science, SciFinder, PubMed, Elsevier, and CNKI (Chinese), and the phytochemical and pharmacological studies of Callicarpa nudiflora were reviewed. Results A total of 300 small molecules, 173 of which are volatile oils, have been isolated from Callicarpa nudiflora. These small molecules could be divided into seven structural types — phenylpropanoids, flavonoids, triterpenes, diterpenes, iridoid glycosides, volatile oils, and other small molecules. Different types of compounds in Callicarpa nudiflora were summarized as follow: a) diterpenoid compounds can inhibit the generation of nitric oxide (NO) for exerting the function of anti-inflammation; b) triterpene compounds can play a role of anti-thrombus via inhibiting platelet aggregation and oleanane type and arbutane type pentacyclic triterpenes have the hepatoprotective activities; c) iridoid glycosides have cytotoxicity to tumor cells, and phenylpropanoids compounds have an antioxidant effect and could improve the function of memory. Our group further studied the antiviral activities of Callicarpa nudiflora finding that it has significant effects on RSV, EV71, COXB5, and HSV-1.

Ethnopharmacological relevance Ficus racemosa (FR) has been used for thousands of years in Ayurvedic system of medicine in India and is closely associated with prevention, treatment and cure of various human ailments like obesity and diabetes. It is popularly known as gular. A vast and wide range of chemical compounds like polyphenols, friedelane-type triterpenes, norfriedelane type triterpene, eudesmane-type sesquiterpene including various glycosides had been isolated from this plant. However, no detail studies related to isolation of flavonoids has been reported previously with their antidiabetic, hypolipidemic and toxicological consequences. Aim of the study The present study was undertaken to evaluate antidiabetic, hypolipidemic and toxicological assessments of flavonoids isolated from Ficus racemosa (FR) stem bark. Materials and methods We isolated four flavonoids from stem bark of FR and structures were confirmed by Infrared spectroscopy (IR), Nuclear Magnetic Resonance (NMR) (both 1D and 2D), mass spectroscopy (MS). Later, these flavonoids were administered to streptozotocin (STZ) rats once in a day for a period of seven days at 100 mg/kg dose. We measured blood glucose level and body weight changes at different days (1st, 3rd, 5th and 7th days). Serum lipid profiles were also estimated to investigate the hypolipidemic potential of flavonoids in the similar experiment. Various oxidative stress parameters in pancreas and liver and hepatic biomarker enzymes in plasma were also determined to investigate the toxicity potential of isolated flavonoids. Finally, we performed docking studies to find out the mechanism of action. Results Our results collectively suggested that four flavonoids reduced blood glucose level and restored body weight, signifying antidiabetic action. There were reduction of other lipid profile parameters and increase of high density lipoprotein (HDL) during administration of flavonoids, also signifying hypolipidemic action. Various oxidative stress biomarkers and hepatic enzymes levels were also normalized with respect to diabetic control at the same time. Docking studies revealed that isolated flavonoids showed their antidiabetic potential via binding to PPARγ and GLUT1 receptors. Conclusion The isolated four flavonoids demonstrated good antidiabetic, hypolipidemic and antioxidant properties in STZ diabetic rats which supported the use of FR stem bark as useful supplementary drug for future antidiabetic therapy.

Ethnopharmacological relevance Combretum leprosum Mart. is a native species of the Caatinga, an important biome in the Brazilian semi-arid region. This species is commonly used in Brazil as a healing agent, as well as for the treatment of skin diseases. Aim of the study This study investigated the healing potential of the ethanolic extract (EECL) and the bioactive triterpene 3β, 6β, 16β-trihydroxylup-20 (29)-ene (CLF-1) isolated from the leaves of C. leprosum . Materials and methods Skin wounds (1 cm 2 ) were created in the dorsal zone of mice with a scalpel blade number 15. The treatment consisted in a daily topical application of 100 μl of 150 mM NaCl, EECL and CLF-1 (at 10 μg/100 μl) for 12 days. The lesions were then macro and microscopically evaluated. Results On postoperative day (POD) 2, the lesions treated with EECL and CLF-1 showed a moderate presence of vessels of the granulation tissue progressing in the dermis. The same effect was not observed in the control group. The treatment with EECL and CLF-1 stimulated angiogenesis, resulting in a rapid deposition of extracellular matrix (ECM). Moreover, the animals treated with EECL and CLF-1 showed smaller lesions on POD 7, primarily due to the contraction in the reticular dermis induced by organization of myofibroblasts, which was not observed in the group treated with NaCl. In addition, the lesions treated with EECL and CLF-1 showed ECM restructuration and presence of epithelium coating, which was not observed in the group treated with NaCl, in which the lesions showed no epithelial lining, suggesting delayed healing. Conclusion CLF-1 isolated from the leaves of C. leprosum may be considered to be an important molecule for the treatment of skin lesions. However, further investigations are necessary to establish its role in chronic lesions and to elucidate the mechanism of action involved in the cutaneous healing process. To the best of our knowledge, this is the first report describing the pro-healing activity of the ethanolic extract and the triterpene 3β, 6β, 16β-trihydroxylup-20(29)-ene isolated from leaves of C. leprosum .

Ethnopharmacological relevance Ethnobotanical studies have been of very great importance in recognizing plants that contain substances that modulate the heterodimer T1R2-T1R3 sweet taste receptor, inclusive of Stevia rebaudiana (Asteraceae) and Siraitia grosvenorii (Cucurbitaceae). Aim of the review In addition to reviewing relevant ethnobotanical literature, inclusive of original field work conducted, the authors have provided a progress report on the ultimate regulatory acceptance of highly sweet ent-kaurane (steviol) diterpene glycosides from S. rebaudiana leaves (“stevia”) and cucurbitane triterpene glycosides (mogrosides) from the fruits of S. grosvenorii (popularly known as “monk fruit”). Despite their relatively high prices relative to that of sucrose, the steviol glycosides and mogrosides are of current great interest for further more extensive utilization on the market as sweet-tasting non-caloric food additives, due to increases in the rates of obesity and diabetes all over the world. Recent phytochemical work on the sweet principles of these two species is highlighted, including the important “next-generation” sweetener, rebaudioside M, from S. rebaudiana. Results Initial observations on the ethnobotany of both S. rebaudiana and S. grosvenorii have proved crucial to indicating the presence of their sweet-tasting principles to the wider scientific community. Conclusions Ethnobotanical observations have been pivotal in enabling the discovery of many sweet-tasting plant constituents, with those of S. rebaudiana and S. grosvenorii both being examples. Extractives prepared from these species are now commercially used widely in the U.S. as additives for the sweetening of foods and beverages.

Ethnopharmacological relevance Twenty six species of the genus Clematis (Ranunculaceae) have been traditionally used in various systems of medicine for the treatment of ailments such as nervous disorders, syphilis, gout, malaria, dysentry, rheumatism, asthma, and as analgesic, anti-inflammatory, diuretic, antitumour, antibacterial and anticancer. Aim of the review To emphasize on ethnopharmacology, chemical constituents, pharmacology, toxicology and clinical studies of various species of the genus Clematis . Materials and methods The available information on Clematis species was collected through electronic search of major scientific databases. Results A survey of literature revealed that triterpene saponins, alkaloids, flavonoids, lignans, steroids, coumarins, macrocyclic compounds, phenolic glycosides, anemonin and volatile oils constitute major classes of chemical constituents in the genus Clematis . Preliminary analgesic, anticancer, anti-inflammatory, diuretic, antiarthritis, hepatoprotective, hypotensive and HIV-1 protease inhibitor activity studies have been carried out on crude extracts of 26 traditionally used and medicinally promising species of Clematis genus. Conclusions The species of the genus Clematis emerged as good source of traditional medicine for the treatment of various ailments. Although few experimental studies validated their traditional claims, but employed uncharacterized crude extracts. Such Clematis species need to be explored properly following bioactivity-directed fractionation with a view to isolate bioactive constituents, and to evaluate their possible mode of actions. These species hold great potential for detailed clinical studies so that these could be exploited as potential drugs. The review will help researchers to select medicinally potential species of Clematis genus for future research.

Aim of the study The objective of this study was to identify the antiplasmodial constituents from the bark of Cornus florida L., a plant traditionally used in North America for the treatment of malaria. Methods and materials Dried and powdered bark was extracted with 95% ethanol. The resultant extract was subjected to in vitro antiplasmodial-guided fractionation against Plasmodium falciparum (D10 strain). Antiplasmodial IC50 values were calculated for pure compounds. Compounds were also assayed against Leishmania tarentolae, and rat skeletal myoblast L6 cells to assess antileishmanial activity and cytotoxicity, respectively. Results Antiplasmodial-guided fractionation afforded 8 compounds: betulinic acid (1), ursolic acid (2), β-sitosterol (3), ergosta-4,6,8,22-tetraene-3-one (4), 3β-O-acetyl betulinic acid (5), 3-epideoxyflindissol (6), 3β-O-cis-coumaroyl betulinic acid (7), 3β-O-trans-coumaroyl betulinic acid (8), of which, (6) is for the first time here isolated from a natural product and (4), (7) and (8) are reported for the first time from this genus. In vitro IC50 values against P. falciparum for (4) (61.0 μM) (6) (128.0 μM), (7) (10.4 μM), (8) (15.3 μM) are reported for the first time. Antileishmanial IC50 values are reported here for the first time for (4) (11.5 μM), (6) (1.8 μM), (7) (8.3 μM) and (8) (2.2 μM). Cytotoxicity against L6 cells is reported for all compounds. Conclusions The compounds isolated in this study, while displaying moderate in vitro antiplasmodial activity, do not fully support the historical importance of C. florida as an antimalarial remedy in North America. The traditional remedy may exert its well documented effects by mechanisms unrelated to direct antiplasmodial action. While not traditionally used to treat Leishmania, this work shows that several constituents of C. florida possess promising in vitro antileishmanial activity.

Ethnopharmacological relevance The 3β, 6β, 16β-trihydroxylup-20(29)-ene (TTHL) is a pentacyclic triterpene obtained from a medicinal plant named Combretum leprosum . In folk medicine, this plant is used to treat several diseases associated with inflammation and pain. We previously demonstrated that TTHL presents a significant antinociceptive effect, suggesting the involvement of the glutamatergic system. Aim of the study This study was designed to investigate the effect of TTHL on nociception and vascular permeability induced by acetic acid. We also evaluated the effect of TTHL on carrageenan-induced peritonitis and the levels of cytokines (interleukin 1-β [IL-1β], tumor necrosis factor α [TNF-α] and interleukin 10 [IL-10]) on peritoneal fluid. Materials and methods TTHL was administered orally by intra-gastric gavage (i.g.) 60 min prior to experimentation. Abdominal contractions and vascular permeability were induced by an intraperitoneal (i.p.) injection of acetic acid (0.6%). We also investigated whether TTHL decreases carrageenan-induced peritonitis (750 μg/cavity) by measuring leukocyte migration and vascular permeability. In addition, we evaluated the effects of TTHL on TNF-α, IL-1β and IL-10 release induced by carrageenan on peritoneal fluid. The levels of these cytokines were measured by ELISA. Results TTHL (0.01–10 mg/kg) administered by intra-gastric (i.g.) gavage inhibited (69±3%) acetic acid-induced abdominal constrictions, with an ID 50 of 0.15 (0.03–0.8) mg/kg. TTHL (10 mg/kg) also reduced the leukocyte infiltration induced by acetic acid, with an inhibition of 59±9 but had no effect on abdominal vascular permeability. In addition, indomethacin (10 mg/kg, i.p.) reduced the nociceptive behavior (92±1%), total leukocyte migration (29±3%) and capillary permeability (71±3%) induced by acetic acid. While the glucocorticoid dexamethasone (2 mg/kg, s.c.) reduced partially but significantly the nociception (31±1%), besides to promote a marked reduction on total leukocyte migration (60±2%) to the peritoneal cavity caused by acetic acid. In a model of peritonitis induced by carrageenan, TTHL also reduced total leukocyte migration, mainly neutrophils (inhibition of 84±3% and 85±2% at 30 mg/kg and 100 mg/kg, respectively). Likewise, dexamethasone (0.5 mg/kg, i.p.) resulted in an inhibition of 93±3%. Nevertheless, carrageenan-induced abdominal vascular permeability was reduced by dexamethasone but was not altered by TTHL. Furthermore, dexamethasone and TTHL significantly reduced the TNF-α and IL-1β levels in peritoneal fluid, whereas the IL-10 levels were unchanged. Conclusions Altogether, our data confirm the antinociceptive effect of TTHL and demonstrate its effect in inflammatory animal models, providing novel data about this compound, which could be useful as an anti-inflammatory drug.

Aim of the study In a preliminary screen of extracts from plants used as antimalarial remedies used in Europe in the 16th and 17th, the ethyl acetate extract of Alisma plantago-aquatica L. (Alismataceae) was active against Plasmodium falciparum K1 strain with 77% growth inhibition at 4.9 μg/ml. The aim of this study was to isolate and identify the substances responsible for this antiplasmodial activity. Materials and methods With HPLC-based activity profiling in combination with HPLC hyphenated methods (HPLC–PDA, –MSn, HR–MS, and off-line microprobe NMR) the activity was assigned to time windows, and the substances contained therein were characterised chemically. The active compounds were isolated with semi-preparative HPLC and structures were elucidated with high resolution mass spectrometry, and 1D and 2D NMR spectroscopy. Results Four compounds were isolated and identified as protostane triterpenoids alisol A, alisol B 11-monoacetate, alisol B 23-monoacetate, and alisol G. Their IC 50 s against Plasmodium falciparum ranged from 5.4 to 13.8 μM. Conclusions This is the first report of antiplasmodial activity from protostanes triterpenoids, and the first result of our ongoing project of screening for antiprotozoal natural products from remedies used in European renaissance medicine.

Ethnopharmacological relevance The stem bark of Symplocos paniculata Thunb. has been used to check abortion in folk medicine in India. Aim of the study The present study was undertaken to isolate the phytochemicals from the plant together with the evaluation of antimicrobial, analgesic and anti-inflammatory activities of the plant extract and isolated compounds. Materials and methods The plant extract was subjected to column chromatography for isolation of phytochemicals. The agar diffusion method was adopted for antimicrobial activity to determine MICs. Ethanolic extract and isolated compounds were selected for investigating their analgesic activity on acetic acid-induced writhing response in mice. The anti-inflammatory activity was performed on carrageenan-induced paw edema in rats. Results The stem bark of the plant afforded seven compounds, 4-(8-hydroxyethyl) cyclohexan-1-oic acid ( 1 ); androst-5(6)-ene 17-one 3β-O-(β- d -glucopyranoside) ( 2 ); 9β,25-cyclo 3β-O-(β- d glucopyranosyl)-echynocystic acid ( 3 ); 9β,19-cyclo 24-methylcholan-5,22-diene 3β-O-{β- d -glucopyranosyl (1 → 6) α- l -rhamnopyranoside} ( 4 ); 30-ethyl 2α,16α-dihydroxy 3β-O-(β- d -glucopyranosyl) hopan-24-oic acid ( 5 ); 32,33,34-trimethyl-bacteriohopan-16-ene 3-O-β- d -glucopyranoside ( 6 ) and flavone 3′,4′,5′,6-tetramethoxy 7-O-β- d -glucopyranosyl (1 → 3) β- d -glucopyranoside ( 7 ). The extract and isolated compounds exhibited antimicrobial, analgesic and anti-inflammatory activities. Conclusion The present study concludes that ethanolic extract of the plant and its constituents having significant antimicrobial, analgesic and anti-inflammatory activities.

Aim of the study Investigate the hypoglycaemic activity of the four isolated compounds from a crude acetone extract of the root bark of Euclea undulata var. myrtina, which is used by traditional healers in the Venda area, Limpopo Province in the treatment of diabetes. Material and methods The hypoglycaemic activity of the four compounds isolated from Euclea undulata was determined by in vitro screening of glucose utilization by C2C12 myocytes at a concentration of 25 μg/ml or 50 μg/ml. The inhibition of α-glucosidase was also tested at concentrations ranging from 0.02 to 200.00 μg/ml. Results Assay-guided isolation of the crude acetone extract of the root bark of Euclea undulata var. myrtina afforded a new triterpene, α-amyrin-3O-β-(5-hydroxy) ferulic acid (1), in addition to three known compounds; betulin (2), lupeol (3) and epicatechin (4). The in vitro results on C2C12 myocytes suggest that compound 4 may have some effect to lowers blood glucose levels, whereas compound 1 has the ability to inhibit α-glucosidase at a concentration of 200.0 μg/ml with an IC50 value of 4.79 that correlates with that of the positive control acarbose IC50 value 4.75. Conclusion The results suggest that 4 may have some ability to lower blood glucose levels, whereas 1 has the ability to inhibit α-glucosidase. Ethnopharmacological relevance These findings corroborate the ethnomedicinal use of Euclea undulata by traditional healers for the treatment of diabetes as two substances was isolated from the acetone plant extract that exhibit hypoglycaemic activity.

Ethnopharmacological relevance Quillaja saponaria bark contains a high percentage of triterpene saponins and has been used for centuries as a cleansing and analgesic agent in Chilean folk medicine. Aim of the study The topical and systemic analgesic effects of a commercial partially purified saponin extract, 3β,16α-dihydroxy-23-oxoolean-12-en-28-oic acid (quillaic acid), methyl 3β,16α-dihydroxy-23-oxoolean-12-en-28-oate and methyl 4-nor-3,16-dioxoolean-12-en-28-oate. Materials and methods The samples were assessed in mice using the topical tail-flick and i.p. hot-plate tests, respectively. Results All the samples showed activity in both analgesic tests in a dose-dependent manner. The most active against tail flick test was commercial partially purified saponin extract (EC50 27.9 mg%, w/v) and more than the ibuprofen sodium. On hot-plate test, methyl 4-nor-3, 16-dioxoolean-12-en-28-oate was the most active (ED50 12.2 mg/kg) and more than the ibuprofen sodium. Conclusions The results of the present study demonstrated that Quillaja saponaria saponins, quillaic acid, its methyl ester, and one of the oxidized derivatives of the latter, elicit dose-dependent antinociceptive effects in two murine thermal models.

Ethnopharmacological relevance: Gynostemma pentaphyllum (Thunb.) tea was used in Vietnamese folk medicine as anti-diabetic agent. Aim of the study: This study was aimed to investigate the inhibitory activities of fractions and constituents isolated from Gynostemma pentaphyllum on protein tyrosine phosphatase 1B (PTP1B) since it has been proposed as a treatment therapy for type 2 diabetes and obesity. Materials and methods: The 70% EtOH extract, CHCl3 fraction, EtOAc fraction, BuOH fraction, and seven isolated dammarane triterpenes were evaluated for their inhibitory activity in protein phosphatase enzymes (PTP1B and VHR). Results: CHCl3-soluble fraction showed a dose-dependent inhibitory activity of the PTP1B enzyme with the IC50 value of 30.5g/mL. Among seven tested compounds, compounds 6 showed the most potent PTP1B inhibitory activity with IC50 value of 5.3 ± 0.4M compared to a range 15.7–28.5M for the other six compounds. The inhibition mode of 6 was competitive toward p-NPP with a Ki value of 2.8M. Conclusion: These study results suggested that the PTP1B inhibitory activity of these dammaranes may enable this plant to play an important role in the treatment of diabetes. © 2009 Elsevier Ireland Ltd. All rights reserved.

Anew jatrophone derivative (6), jatrophone (3), jatropholone A (4) and jatropholone B (5), acetyl aleuritolic acid (1), cyperenoic acid (2) and a monoterpene were isolated from the rhizomes of the Paraguayan crude drug Jatropha isabelli. The compounds were characterized by spectroscopic means. The gastroprotective effect of jatrophone, jatropholone A and B as well as 9 beta,13 alpha-dihydroxyisabellione 6 and the triterpene 1 was assessed in the HCl/EtOH-induced gastric lesions model in mice. Jatrophone elicited a strong gastroprotective effect with no significant differences between 25, 50 or 100 mg/kg and reducing lesions from 88 to 93%. The jatropholones A and B showed remarkable differences in the gastroprotective assay. Jatropholone A presented a dose-related response, with maximum effect (54% lesion reduction) at the highest dose (100 mg/kg), jatropholone B showed a strong action at all the doses, reducing lesions by 83-91%. The cytotoxicity of the compounds was assessed towards fibroblasts and AGS cells. Jatrophone was toxic against both cell lines (IC50 values: 2.8 and 2.5 mu M, respectively). Jatropholone B (5) was not cytotoxic while jatropholone A (4) displayed a selective effect against AGS cells (IC50: 49 mu M). The relevance of stereochemistry in the biological effects is clear comparing the effect of jatropholone A and B against AGS cells, with IC50 values of 49 and g 1000 mu M for the beta and alpha C-16 isomers, respectively. The results provide scientific support for the use of qyagua rovaq as a gastroprotective crude drug in Paraguayan traditional medicine. (c) 2007 Elsevier Ireland Ltd. All rights reserved.

As the Mycobacterium tuberculosis strains resistant to multiple drugs are increasing at an alarming rate, there is an urgent need for alternative anti-tuberculosis drugs. In a bioassay-guided search for antimycobacterial compounds obtained from higher plants, the study of the hexane extract from the aerial parts of Lantana hispida was performed and the biological activity of the plant products were tested against Mycobacterium tuberculosis H37Rv strain by microdilution alamar blue assay. Activity of the primary fractions led to the isolation of three pentacyclic triterpenoids with oleanane nucleous, together with beta-sitosterol. The molecular structures of the compounds were characterized as 3-acetoxy-22-(2'-methyl-2Z-butenyloxy)-12-oleanen-28-oic acid (1), 3-hydroxy-22 beta-(2'-methyl-2Z-butenoyloxy)-12-oleanen-28-oic acid (reduced lantadene A) (2) and oleanolic acid (3). MIC values for compounds 1 and 2 were 50 microg/ml, and for compound 3 the MIC=25 microg/ml.

International audience; Methanolic extracts prepared from the leaves, twigs and the roots of Vismia laurentii De Wild as well as nine compounds isolated from these crude extracts, were tested for their antimicrobial activity against Gram-positive bacteria (six species), Gram-negative bacteria (12 species) and two Candida species using disc diffusion and well micro-dilution methods. The disc diffusion assay indicated that the crude extract was active against all the pathogens tested, whereas isolated compounds showed selective activities. The degree of sensitivity of the test organisms to purified compounds varied from 25 to 90%. Fridelin (8) was found to be the most active compound, while Bivismiaquinone (3) was the least active. The lowest minimum inhibition concentration (MIC) values as obtained by the micro-dilution assays were 19.53 and 1.22 microg/ml for the crude extracts and purified compounds, respectively. The lowest value for the purified compounds (1.22 microg/ml) was obtained with O(1)-demethyl-3',4'-deoxypsorospermin-3',4'-diol (6) on Candida gabrata and Bacillus subtilis; 1,8-dihydroxy-6-methoxy-3-methylanthraquinone (5) on Bacillus subtilis and 6-deoxyisojacareubin (7) on Bacillus stearothermophilus. These results provide promising baseline information for the potential use of these crude extracts as well as some of the isolated compounds in the treatment of bacterial and fungal infections.

Ethnopharmacological relevance Ginsenosides are natural product steroid glycosides and triterpene saponins obtained from the Panax species. Panax ginseng has been widely used as a traditional Chinese medicine (TCM) for around a thousand years, especially in East Asian countries. Ginseng, the root and rhizome of the most popular species P. ginseng , used as tonic, prophylactic agent and restorative. In TCM, ginseng is highly valued herb and has been applied to a variety of pathological conditions and illnesses such as hypodynamia, anorexia, shortness of breath, palpitation, insomnia, impotence, hemorrhage and diabetes. Aim of the study The basic aim of this study was to evaluate the anti-Alzheimer's disease activities of selected ginsenosides (Rb1, Rb2, Rc, Re, Rg1, and Rg3) according to peroxynitrite (ONOO ‒ ) scavenging activity and inhibitory activity of ONOO − -mediated nitrotyrosine formation as a measure of changes in oxidative stress. In addition, molecular docking simulation studies were performed to predict binding energies of the ginsenosides with β-site amyloid precursor protein cleaving enzyme 1 (BACE1, β-secretase) and identify the interacting residues. Materials and methods In vitro cholinesterase enzyme assays by using acetylcholinesterase (AChE), butyrylcholinesterase ( BChE), and BACE1 were performed. In vitro authentic peroxynitrite scavenging activity and inhibitory activity against ONOO − -mediated nitrotyrosine formation were also performed. Molecular docking simulation studies were performed with Autodock Vina software and Discovery studio 4.1. Results In vitro enzyme assays demonstrated that ginsenosides have significant inhibitory potential against AChE, BChE, and BACE1, as well as ONOO − and nitrotyrosine formation. Most importantly, significant AChE inhibitory activities were observed for Re; BChE for Rg3; and BACE1 for Rc, with IC 50 values of 29.86±3.20, 16.80±0.36, and 59.81±2.74 μg/mL, respectively. Among the tested ginsenosides, Rb1 exhibited a higher scavenging activity against ONOO − with an IC 50 value of 27.86±1.34 μg/mL, while Rc and Rg3 exhibited impressive inhibitory activity against the formation of nitrotyrosine. In addition, molecular docking studies revealed potential BACE1 inhibitory activity of ginsenosides, especially Rb1 and Rb2, which exhibited good binding affinities towards BACE1, with docking scores of −10 kcal/mol. Conclusion The findings of the present study suggest the potential of ginsenosides (Rb1, Rb2, Rc, Re, Rg1, and Rg3) for use in the development of therapeutic or preventive agents for Alzheimer's disease, especially through inhibition of AChE, BChE and BACE1 activities, as well as scavenging of ONOO − and inhibition of nitrotyrosine formation.

Ethnopharmacological relevance Alismatis rhizoma (AR), a Traditional Chinese Medicine with lipid-regulating properties, is usually used to treat hyperlipidemia. Lysophosphatidylcholines (Lyso PCs) play a crucial role in lipid metabolism disorders. In this study, the triterpene fraction purified from boiling water extract of AR was evaluated for its lipid lowering activity using mice with high-fat diet (HFD) induced hyperlipidemia. The metabolic changes of individual Lyso PCs treated with the triterpene fraction were detected by ultra-high performance liquid chromatography–triple quadrupole-linear ion trap mass spectrometer (UHPLC–QTRAP-MS/MS). Materials and methods HFD induced hyperlipidemia mice were administrated with triterpene and non-triterpene fractions at doses of 180, 360 and 720 mg/kg body weight/day for 4 weeks, respectively. Total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C) and atherogenic Index (AI) in mice serum were measured. The chemical components in the lipid-lowering fraction were characterized by ultra-high performance liquid chromatography–quadrupole time of flight tandem mass spectrometry (UHPLC–QTOF-MS/MS). The changes of Lyso PC in the serum of mice treated with the lipid-lowering fraction were quantified by UHPLC–QTRAP-MS/MS. Results A total of 18 alisol derivatives were identified in the triterpene fraction. The hyperlipidemia mice treated with the triterpene fraction showed a significant decrease in serum TC, LDL-C and AI after continuous consumption of HFD for 4 weeks. The results also showed that 27 serum Lyso PCs in mice fed with HFD were down-regulated, and 19 were up-regulated. The abnormal serum level of Lyso PCs associated with hyperlipidemia was intervened by the alisol derivatives, with increase of unsaturated Lyso PCs and decrease of saturated ones. Conclusions The study demonstrated for the first time that triterpenes from the AR extract can lower serum lipid level in HFD induced hyperlipidemia mice. These metabolism changes of Lyso PCs could further improve our understanding of the potential mechanism of lipid lowering effect of AR.

For the first time a biossay-directed study of triterpenoids isolated from the leaves of Olea europaea from Greece, from wild African olive and from a cultivar of O. europaea grown in Cape Town was reported. The experiment was undertaken since our preliminary analyses showed that the African wild olive leave is rich in triterpenoids and contain only traces of the glycoside oleuropein, which is typical for the European olive leaves. The isolate of the African wild olive leaves (AO) used in the experiments was found to contain 0.27% 1:1 mixture of oleanolic acid and ursolic acid, named oleuafricein. The isolate of Greek olive leaves (GO) was found to contain 0.71% oleanolic acid, and the Cape Town cultivar (CT) contained 2.47% oleanolic acid. No ursolic acid was found in either GO or CT. The antihypertensive, diuretic, antiatherosclerotic, antioxidant and hypoglycemic effects of authentic oleanolic and ursolic acid and the three isolates (GO, AO and CT) were studied on Dahl salt-sensitive (DSS), insulin-resistant rat genetic model of hypertension. All three isolates, in a dose 60 mg/kg b.w. for 6 weeks treatment, prevented the development of severe hypertension and atherosclerosis and improved the insulin resistance of the experimental animals. GO, OA and CT isolates could provide an effective and cheap treatment of this particular, most common type of salt-sensitive hypertension in the African population.

This report describes the isolation of two triterpenes from the stems of Tinospora crispa, namely, cycloeucalenol (1). and cycloeucalenone (2). for the first time. It was found that cycloeucalenol (1). slightly increased the right atrial force of contraction whereas it showed an initial reduction followed by sustained reduction of about 10% on the left atria of the rat in vitro. Cycloeucalenone showed slight change from the control on the right and left atrial force. These results suggest that cycloeucalenol and cycloeucalenone produced mild cardiotonic effects.

An easy methodology for triterpene isolation is shown. Evaluation in rats for antiulcer activity of friedelan-3beta-ol 1 and friedelin 2. The two triterpenes isolated from the leaves of Maytenus ilicifolia, did not decrease gastric ulcers when tested on indometacine induced ulcer model in rats.

The alcoholic extracts of the aerial portion and fruits of Aglaia roxburghiana (W.& A.) Miq. var. beddomei and the triterpenes roxburghiadiol A and B isolated from this plant were investigated for their anti-inflammatory activity in rats by carrageenin induced rat paw oedema and cotton pellet granuloma methods. They were also studied for their effect on mast cell degranulation induced by compound 48/80. Potent anti-inflammatory activity was observed for the extracts of the aerial portion and fruits of A. roxburghiana as well as for the triterpenes roxburghiadiol A and B. The mast cell degranulation induced by compound 48/80 was significantly reduced by A. roxburghiana extracts and the triterpenes. The triterpenes roxburghiadiol A and B may play a significant role in the observed anti-inflammatory effect of A. roxburghiana.

Oleanolic acid and ursolic acid are triterpenoid compounds that exist widely in food, medicinal herbs and other plants. This review summarizes the pharmacological studies on these two triterpenoids. Both oleanolic acid and ursolic acid are effective in protecting against chemically induced liver injury in laboratory animals. Oleanolic acid has been marketed in China as an oral drug for human liver disorders. The mechanism of hepatoprotection by these two compounds may involve the inhibition of toxicant activation and the enhancement of the body defense systems. Oleanolic acid and ursolic acid have also been long-recognized to have antiinflammatory and antihyperlipidemic properties in laboratory animals, and more research is warranted to develop a therapy for patients. Recently, both compounds have been noted for their antitumor-promotion effects, which are stimulating additional research in this field. Oleanolic acid and ursolic acid are relatively non-toxic, and have been used in cosmetics and health products. The possible mechanisms for the pharmacological effects and the prospects for these two compounds are discussed.

Ethnopharmacological relevance Rosemary is a species used worldwide as a common spice, but also in folk medicine for their therapeutic properties against abdominal pain. The rationale of this study was to examine the involvement of triterpenes and to compare their effectiveness in the antinociceptive effect of an ethanol extract of Rosmarinus officinalis L. (Lamiaceae). Material and methods Fractionation and HPLC analyses allowed the identification of a mixture of micromeric (121 mg/g), oleanolic (64 mg/g) and ursolic (83 mg/g) acids as partial antinociceptive responsible in an ethyl acetate fraction of R. officinalis by using the acetic acid-induced abdominal constrictions model in mice. Results These triterpenes individually evaluated produced a significant and dose-dependent antinociceptive response with similar potency as follows: ED 50 =1.1 mg/kg (0.9–1.3 mg/kg), 2.1 mg/kg (1.6–2.6 mg/kg) and 1.6 mg/kg (1.1–2.1 mg/kg), respectively, by using the intraperitoneal (i.p.) route of administration in mice. Their maximal antinociceptive efficacy resembled that produced by ketorolac (10 mg/kg, i.p.), a common clinic analgesic. Conclusion Our results provide evidence that these triterpenes participate in the antinociceptive activity of R. officinalis . In addition, each individual triterpene showed a similar potency to that observed with ketorolac, a non-steroidal anti-inflammatory drug, in this experimental model.

Cimicifuga foetida L., a traditional Chinese medicine, has been used as an anti-inflammatory, antipyretic and analgesic remedy. The primary active constituents are believed to be present in the triterpene glycoside fraction.To develop an LC-MS/MS assay for four major cimicifugosides [cimicifugoside H-1 (Cim A), 23-epi-26-deoxyactein (Cim B), cimigenolxyloside (Cim C) and 25-O-acetylcimigenoside (Cim D)] obtained from C. foetida L. and apply it to investigate their pharmacokinetic (PK) properties and bioavailabilities through oral administration of C. foetida L. extract (12.5, 25 and 50mg/kg) and single intravenous (i.v.) doses (5mg/kg) of the individual cimicifugosides in rat. PK parameters were estimated by non-compartmental analysis.All calibration curves showed excellent linear regressions (all r0.995) within the range of tested concentrations. The intra- and inter-day variations were15% in terms of RSD. The molar ratio of Cims A, B, C, and D in the extract was 20.7:1.4:2.9:1. PK parameters for Cims A, B, C, and D following oral administration of the extract were respectively: C(max) 4.05-17.69, 90.93-395.7, 407.1-1180 and 21.56-45.09pmol/mL; T(max) 0.46-1.28, 2.00-4.67, 14.67-19.67 and 8.08-14.27h; absolute oral bioavailability (F) 1.86-6.97%, 26.8-48.5%, 238-319% and 32.9-48%. PK parameters after i.v. administration of individual cimicifugosides were respectively: elimination half-life 1.1, 2.5, 5.7 and 4.2h; clearance 15.7, 0.48, 0.24 and 1.13mL/hkg.Systemic exposure to Cims B, C and D following oral administration of the extract was significantly greater than to Cim A despite the predominance of Cim A in the extract. Significantly different clearance and interconversion from Cim A to Cim C probably accounts for the different exposure to the four cimicifugosides.

The roots and rhizomes of Clematis are commonly used as an analgesic, abirritative, antibacterial, antiphlogistic, anticancer and diuretic agent. The Naxi people traditionally used Clematis ganpiniana's (Lévl. Et Vant.) as a diuretic agent, an anti-inflammatory and anticancer remedy.To investigate the cytotoxic and antibacterial components from Clematis ganpiniana.The aboveground part of Clematis ganpiniana was isolated by chromatographic techniques. Structures of isolated compounds were identified by spectroscopic methods and comparison with published data. Their cytotoxic, apoptosis and antibacterial activities of purified components were also performed.By bioassay-guided fractionation techniques and chemical characterization, four triterpene glycosides were isolated and their cytotoxicity against cancer cells and antibacterial activity were tested. They showed significant inhibitory activities against MCF-7, MDA-MB-231 with IC50 value of 0.7-16.5 microg/ml, and significant apoptosis for MCF-7 and MDA-MB-231. Moreover, compound 4 showed weak wide-spectrum antibacterial activity.These results provide promising baseline information for the potential use of Clematis ganpiniana as well as some of the isolated compounds in the treatment of cancer and infectious disease.

Ethnopharmacological relevance Ampelozizyphus amazonicus Ducke is a plant used in Brazilian folk medicine to both prevent malaria and act as a depurative. Aim of the study We have investigated the effects of an ethanol crude extract of roots of Ampelozizyphus amazonicus (CE Aa D), a chemically characterized saponin mixture (SAP Aa D), as well as a saponin-free fraction (SAP Aa D-free) obtained from CE Aa D on diuresis in rats. Materials and methods Wistar rats under ad libitum water conditions or water deprivation for 12 h prior to the start of the experiment were volume-expanded with 0.9% NaCl (4% body weight, by gavage) containing either CE Aa D, SAP Aa D, or SAP Aa D-free at the doses indicated in the text. Rats were individually housed in metabolic cages, and urine volume was measured every 30 min throughout the experiment (3 h). Results CE Aa D increased urine volume in rats under conditions of both free access to water and under water deprivation. In the latter condition, CE Aa D (150 mg/kg) increased the urine volume from zero to 0.9 ± 0.1 ml/120 min, n = 6). Similarly, the SAP Aa D-free (50–200 mg/kg) mixture also increased the urine volume. In contrast, SAP Aa D (12.5–1000 mg/kg) produced a significant reduction ( p Conclusion Our data indicate that CE Aa D contains compounds that cause both diuresis and antidiuresis and that the antidiuretic effect is due mainly to the presence of saponins.

Aim of study The fruit of Melia toosendan Sieb. et Zucc. (MTF) is a traditional Chinese herbal medicine in the treatment of stomachache and many acute or chronic inflammations, as well as ascariasis. This paper aimed to investigate the anti-inflammatory and analgesic activities of the MTF extract and two main limonoid-type triterpenoids isolated from MTF. Materials and methods The ethanolic extract of MTF and two limonoids, isotoosendanin ( 1 ) and 1- O -tigloyl-1- O -debenzoylohchinal ( 2 ) were evaluated for their anti-inflammatory and analgesic activities. Acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests in mice were used to investigate anti-inflammatory activity; and acetic acid-induced writhing and hot-plate tests in mice were used to determine analgesic effect. Results Both the ethanolic extract and two limonoids displayed significant anti-inflammatory effects. Although the ethanolic extract showed remarkable analgesic effects in both writhing and hot-plate tests, the two limonoids had analgesic effects just in writhing test. Conclusion The results suggested that the ethanolic extract of MTF had obvious anti-inflammatory and analgesic activities, and the two limonoids were the active constituents contributing to the anti-inflammatory and analgesic effects of MTF.

Alchornea cordifolia is one of the most widely-used plants in traditional medicine throughout Africa, principally for inflammatory, antimicrobial and parasitic diseases. In continuation of our investigations on its anti-inflammatory activity, we fractionated the leaf and root bark extracts and isolated six compounds which exhibited significant topical anti-inflammatory activity in the mouse ear oedema model using croton oil at a dose of 90 microg/cm2. Daucosterol (2), acetyl aleuritolic acid (4), N1,N2-diisopentenyl guanidine (5) and N1,N2,N3-triisopentenyl guanidine (6) were shown to be more active than indomethacin, while beta-sitosterol (1) and di(2-ethylhexyl) phthalate (3) were less effective. This is the first report on the presence of compounds 1, 2, 3 and 4 in this plant and of the anti-inflammatory activity of 3, 5 and 6. These compounds may account, at least in part, for the use of A. cordifolia in folk medicine to treat inflammation.

Combretum imberbe is used widely in Africa inter alia for treating bacterial infections. In addition to four known triterpenoids, 1alpha,3beta-dihydroxy-12-oleanen-29-oic (1), 1-hydroxy-12-olean-30-oic acid (2), 3,30-dihydroxyl-12-oleanen-22-one (3), and 1,3,24-trihydroxyl-12-olean-29-oic acid (4), a new pentacyclic triterpenoid (1alpha,23-dihydroxy-12-oleanen-29-oic acid-3beta-O-2,4-di-acetyl-L-rhamnopyranoside) 5 has been isolated through a bioassay-guided procedure from the leaves of Combretum imberbe. The structures of the compounds were elucidated on the basis of 1D and 2D NMR experiments, as well as mass spectrometric data. All compounds isolated had moderate (62 microg/ml) to strong (16 microg/ml) antibacterial activity (MIC values) against Staphylococcus aureus and Escherichia coli, with 1 and 5 being most active. Compounds 1 and 5 also showed very strong inhibition of 3alpha-hydroxysteroid dehydrogenase with an IC(50) of 0.3 microg/ml. Compound 5 indicated a moderate anti-proliferative (GI(50)=16.5 and 13.2 microg/ml) and cytotoxic activity (CC(50)=17.6 micro/ml) against K-562, L-929 and HeLa cell lines, respectively. The results of this study give credence to the ethnomedicinal use of Combretum imberbe and expand our knowledge on the biological activity of its metabolites.

The leaves of Buddleja madagascariensis are traditionally used to treat asthma, coughs and bronchitis. In this report we describe, for the first time, the identification of mimengoside B, a triterpenoid saponin, in the leaves of this plant.

Boswellic acids are the main well-known active components of the resin of Boswellia carteri (Burseraceae) and these are still dealing with the ethnomedicinal use for the treatment of rheumatoid arthritis and other inflammatory diseases. Although several studies have already been reported on the pharmacological properties, especially on the anti-inflammatory activity, of Boswellia carteri resin and boswellic acids, the ethnomedicinal importance of Boswellia carteri and its components, boswellic acids, prompted us to undertake detailed investigation on the constituents of the resin and their anti-inflammatory activity. Fifteen triterpene acids, viz., seven of the beta-boswellic acids (ursane-type) (1-7), two of the alpha-boswellic acids (oleanane-type) (8, 9), two of the lupeolic acids (lupane-type) (10, 11), and four of the tirucallane-type (12-14, 16), along with two cembrane-type diterpenes (17, 18), were isolated and identified from the methanol extract of the resin of Boswellia carteri. Upon evaluation of 17 compounds, 1-14 and 16-18, and compound 15, semi-synthesized from 14 by acetylation, for their inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice, all of the compounds, except for 18, exhibited marked anti-inflammatory activity with a 50% inhibitory dose (ID(50)) of 0.05-0.49 mg/ear.

Extracts of six selected Malaysian plants with a reputation of usefulness in treating diabetes were examined for alpha-amylase inhibition using an in vitro model. Inhibitory activity studied by two different protocols (with and without pre-incubation) showed that Phyllanthus amarus hexane extract had alpha-amylase inhibitory properties. Hexane and dichloromethane extracts of Anacardium occidentale, Lagerstroemia speciosa, Averrhoa bilimbiPithecellobium jiringa and Parkia speciosa were not active when tested without pre-incubation. Extraction and fractionation of Phyllanthus amarus hexane extract led to the isolation of dotriacontanyl docosanoate, triacontanol and a mixture of oleanolic acid and ursolic acid. Dotriacontanyl docosanoate and the mixture of oleanolic acid and ursolic acid are reported from this plant species for the first time. All compounds were tested in the alpha-amylase inhibition assay and the results revealed that the oleanolic acid and ursolic acid (2:1) mixture was a potent alpha-amylase inhibitor with IC(50)=2.01 microg/ml (4.41 microM) and that it contributes significantly to the alpha-amylase inhibition activity of the extract. Three pure pentacyclic triterpenoids, oleanolic acid, ursolic acid and lupeol were shown to inhibit alpha-amylase.