Activity Of Ethanolic Extract Research Articles

Antispasmodic potential of leaves, barks and fruits of Zanthoxylum armatum DC

Zanthoxylum armatum is a well known food product used as antispasmodic in traditional medicine system. In the present research work, the phytochemical composition of the leaves, barks and fruits was carried out showing that all parts are good source of alkaloids, saponin, tannins and flavonoids. The ethanolic and n-hexane extracts were tested for their antispasmodic potential using rabbit ileum tissues. The ethanolic and n-hexane extract of the leaves (ZLE and ZLH), barks (ZBE and ZBH) and fruits (ZFE and ZFH), demonstrated a dose dependant antispasmodic effect. In most of the tested extracts, the action of ethanolic extract was found more pronounced than the other. The most significant antispasmodic effect was observed with fruit extracts. In conclusion, the current study strongly supports the folkloric uses of the plant as antispasmodic. Key words: Zanthoxylum armatum, rabbit ileum, phytochemical studies, folkloric, antispasmodic.

Antinociceptive effect of the Orbignya speciosa Mart. (Babassu) leaves: Evidence for the involvement of apigenin

AimsBabassu is the common Brazilian name of Orbignya speciosa Mart. (Arecaceae). The fruits are used for several disorders. In the present study, the antinociceptive effects of the ethanol extract (EE) and dichloromethane fraction (DF) obtained from leaves were investigated, as well as apigenin using nociception models (acetic acid-induced abdominal writhing, formalin, and hot plate). Main methodsMice were treated with EE, DF (10, 30, and 100mg/kg, p.o.), apigenin (1mg/kg, p.o.), morphine (5mg/kg, s.c.), acetylsalicylic acid (100mg/kg, p.o.) or vehicle (0.1ml, p.o.). The EE and DF reduced the contortions induced by acetic acid. Both also reduced the licking response in the formalin model. In the hot plate model, the antinociceptive effects were, at least, equal to that shown by morphine. To elucidate the antinociceptive mechanism of action of EE, DF, and apigenin the animals were pre-treated with atropine (nonselective muscarinic receptor antagonist, 1mg/kg, s.c.), naloxone (opioid receptor antagonist, 1mg/kg, s.c.), l-nitro arginine methyl ester (L-NAME, nitric oxide synthase inhibitor, 3mg/kg, s.c.) or mecamylamine (nicotinic receptor antagonist, 2mg/kg, s.c.) and evaluated in the hot plate model. Key findingsThe antinociception produced by DF was abolished by atropine, naloxone or mecamylamine. The effect of apigenin was significantly blocked by atropine or naloxone. SignificanceThe results obtained indicated that EE and DF have antinociceptive activity that is mediated, at least in part, by opioid and cholinergic systems. This effect can be attributed to the presence of apigenin, a flavonoid in the dichloromethane fraction.

In vitro antibacterial potential of Eugenia jambolana seed extracts against multidrug-resistant human bacterial pathogens

The present study was carried out to evaluate the possible in vitro antibacterial potential of extracts of Eugenia jambolana seeds against multidrug-resistant human bacterial pathogens. Agar well diffusion and microbroth dilution assay methods were used for antibacterial susceptibility testing. Kill-kinetics study was done to know the rate and extent of bacterial killing. Phytochemical analysis and TLC-bioautography were performed by colour tests to characterize the putative compounds responsible for this antibacterial activity. Cytotoxic potential was evaluated on human erythrocytes by haemolytic assay method and acute oral toxicity study was done in mice. The plant extracts demonstrated varying degrees of strain specific antibacterial activity against all the test isolates. Further, ethyl acetate fraction obtained from fractionation of most active ethanol extract showed maximum antibacterial effect against all the test isolates. Phytochemical analysis and TLC-bioautography of ethyl acetate fraction revealed that phenolics were the major active phytoconstituents. Ethyl acetate fraction also demonstrated no haemolytic activity on human erythrocytes and no gross behavioural changes as well as toxic symptoms were observed in mice at recommended dosage level. The results provide justification for the use of E. jambolana in folk medicine to treat various infectious diseases and may contribute to the development of novel antimicrobial agents for the treatment of infections caused by these drug-resistant bacterial pathogens.

In Vitro Antiplasmodial and Cytotoxic Activities of Ethanol Extracts of Apical Stem of Phyllanthus amarus Schum. et Thonn. (Euphorbiaceae)

The in vitro antiplasmodial and cytotoxic activities of ethanol extracts from whole plant, fresh apical stems and calli from fresh apical stem of Phyllanthus amarus cultured on Murashige and Skoog (MS) medium supplemented with indole-butyric acid (IBA)/benzylaminopurine (BAP) 1:1, 1:2, 1:4 and 1:4, IBA/BAP/mannitol 1:1:0.5%, IBA/BAP/mannitol: 2% for three months were evaluated. Results indicated that all ethanol extracts showed an in vitro antiplasmodial activity at different extends. The most active ethanol extract was that from callus cultivated with IBA/BAP/mannitol 1:1:05% (IC50 < 0.19 µg/ml). The ethanol whole plant and intact apical stem extracts exhibited an activity with IC50 values of 2.5 ± 0.4 and 8.2 ± 1.9 µg/ml, respectively. Quercetin, lupeol and ellagic acid displayed an antiplasmodial activity with IC50 values of 3.2 ± 0.6, 8.3 ± 1.4 and 0.07 ± 0.02 µg/ml, respectively. All ethanol extracts and isolated compounds were considered to be non cytotoxic against MT-4 cell lines growth (CC50 > 32 µg/ml).

Postcoital interceptive activity of Wrightia tinctoria in Sprague–Dawley rats: a preliminary study

Background This study was aimed to investigate the pregnancy-interceptive activity of the stem bark of Wrightia tinctoria R.Br. (Family Apocynaceae) administered during the preimplantation, peri-implantation and early postimplantation periods by oral route in adult female Sprague–Dawley rats. Study Design The ethanolic extract of the stem bark and its serial fractions were administered to female rats on Days 1–7 or 1–5 postcoitum (Day 1: day of sperm-positive vaginal smear) by the oral route. At autopsy on Day 10 postcoitum, the number and status of corpora lutea and implantations were recorded. For estrogen-agonistic activity, immature rats ovariectomized 7 days earlier received the test extract or the vehicle once daily for 3 days and, at autopsy on Day 4, uterine weight, status of vaginal opening and extent of vaginal cornification were recorded. Results The ethanolic extract of the stem bark of W. tinctoria R.Br. inhibited pregnancy in 100% of rats when administered orally at a 250-mg/kg dose on Days 1–7 or 1–5 postcoitum. On fractionation, the hexane-soluble, chloroform-soluble, water-soluble and water-insoluble fractions showed 100% anti-implantation effect, while n-butanol-soluble fraction intercepted pregnancy in 75% of animals when administered in the Days 1–5 postcoitum schedule. In immature rat bioassay, the active ethanolic extract and its fractions exhibited moderate to potent estrogen-agonistic activity, which might be responsible for their contraceptive action in this species. Conclusions Findings demonstrate the antifertility activity of the ethanolic extract of the stem bark of W. tinctoria and its hexane-soluble, chloroform-soluble, water-soluble and water-insoluble fractions. Studies that pursue promising natural products (to identify contraceptive agents from natural sources lacking potent estrogenic activity) towards a fruitful conclusion for development/lead generation should continue.

홍삼 생약 복합물(KTNG0345)이 섬유아세포의 Procollagen 생합성과 Matrix metalloproteinase-1(MMP-1) 활성에 미치는 영향

본 실험은 홍삼, 사상자, 산수유를 이용하여 주름 예방 효과가 있는 건강기능 식품을 개발하기 위한 기초자료로 활용하기 위하여 개별추출물과 이들의 혼합물 WM1, WM3 (KTNG0345)에 대하여 사람의 섬유아세포를 이용한 세포증식, 콜라겐 생합성 정도, MMP-1 효소활성, 항산화 활성을 조사하였다. 사용된 시료는 <TEX>$1{\sim}10\;{\mu}g/ml$</TEX>의 농도로 첨가하여 세포를 배양했을 때 <TEX>$83{\sim}100%$</TEX>의 세포증식율을 나타내어 세포 독성을 나타내지 않았으며, 콜라겐 생합성 정도는 대조군이 474.8 ng/ml이었고 retinoic acid는 568.3 ng/ml이었으며, 5 ug/ml의 농도를 기준으로 할 때 홍삼은 533.9ng/ml, 사상자는 539.3 ng/ml, 산수유는 514.1 ng/ml이었다. 홍삼과 생약을 68:232의 비율로 혼합한 WM1은 474.6 ng/ml이었고 홍삼과 생약을 136:164의 비율로 혼합한 WM3는 561.4 ng/ml로 증가하였다. MMP-1활성은 10 ug/ml의 농도에서 홍삼(ER)은 31.9 ng/ml, 사상자(WT)는 32.85 ng/ml, 산수유(WC)는 32.0 ng/ml, WM1은 31.3 ng/ml이었고 WM3(KTNG0345)는 28.85 ng/ml으로 대조군의 88% 수준으로 감소하였다. SOD활성에서는 1000 ug/ml의 농도로 처리하였을 때 65-97% 항산화활성을 나타내었다. 이들의 결과를 종합해 보면 홍삼과 사상자, 산수유 및 이들 혼합물은 human dermal fibroblas에 대하여 세포 독성을 나타내지 않으면서 콜라겐 생합성을 촉진하고 MMP-1의 활성을 억제하였으며 홍삼과 생약 엑기스를 136:164의 비율로 혼합했을 때 그 효과가 증진되었다. WM3 (KTNG0345)는 지표성분으로서 ginsenoside-<TEX>$Rb_1$</TEX>, torilin, loganin을 각각 10.85 mg/g, 0.128 mg/g, 3.92 mg/g 함유하였다. Skin wrinkles are associated with collagen synthesis and matrix metalloproteinase-I (MMP-1) activity. This study was carried out to select optimum ratio of 3 herbs in skin health food for anti-wrinkle. Human dermal fibroblast cell was incubated with experimental samples, which were Korean red ginseng ethanol extracts (ER), Torilis fructus water extracts (WT), Corni fructus water extracts (WC) and their mixtures (WM1, WM3). And then we determined effects on collagen biosynthesis, MMP-1 activity and SOD activity in human dermal fibroblast cell. In control group, collagen biosynthesis was amounted at 474.8 ng/ml and 533.9 ng/ml, 539.3 ng/ml, 514.1 ng/ml in ER, WT and WC respectively. Furthermore, WM3 (KTNG0345) was increased to 561.45 ng/ml. MMP-1 activity of ER, WT, WC, WM1 were determined to 31.9 ng/ml, 32.85 ng/ml, 32.0 ng/ml, 31.3 ng/ml and WM3 (KTNG0345) was decreased to 28.85 ng/ml. In addition, the experimental samples showed a antioxidative activities. From this results, we conclude that Korean red ginseng ethanol extracts, Torilis fructus water extracts, Corni fructus water extracts and their mixtures have a anti-wrinkle effect and WM3 (KTNG0345) may be regarded as an optimum composition for synergic effect producing. The standardized components of KTNG0345, ginsenoside-<TEX>$Rb_1$</TEX>, torilin and loganin were identified at 10.85 mg/g, 0.128 mg/g and 3.92 mg/g respectively.

Pregnancy interceptive activity of the roots of Calotropis gigantea Linn. in rats

Objective We conducted this study to evaluate the pregnancy interceptive activity of the roots of Calotropis gigantea Linn. in colony-bred adult Sprague–Dawley rats when administered during the preimplantation and/or peri-implantation periods. Methods The ethanolic extract of the roots of C. gigantea Linn. and its hexane, chloroform, n-butanol-soluble and n-butanol-insoluble fractions were administered to rats on Day 1, Days 1–5, Days 1–7 or Days 5–7 postcoitum. Rats from the control group received an equal volume of the vehicle (Tween 80 in glass distilled water) only. At autopsy on Day 10 postcoitum, the final body weight and number as well as status of the corpora lutea and implantations in each animal were recorded. For estrogen agonistic and antagonistic activities, 21-day-old immature rats ovariectomized 7 days earlier were treated orally with the test agent or the vehicle for 3 days. In the case of estrogen antagonistic activity, the rats also received 0.05 mg/kg of 17α-ethinyl estradiol for 3 days. At autopsy 24 h after the last treatment, uterine fresh weight was taken and premature opening of the vagina as well as the extent of vaginal cornification, if any, were recorded. Results The ethanolic extract of the roots of C. gigantea Linn. exhibited 100% pregnancy interceptive activity in rats when administered as a single oral dose of 100 mg/kg on Day 1 postcoitum. The extract also exhibited 100% efficacy at the dose of 12.5 mg/kg when administered in the Days 1–5 and 1–7 postcoitum schedules. When administered during the peri-cum-early postimplantation period (i.e., Days 5–7 postcoitum at 250 mg/kg), most of the implantations showed signs of resorption. On fractionation, the chloroform fraction showed 100% activity at 100 mg/kg in the single-day (Day 1 postcoitum) schedule, whereas the hexane, n-butanol-soluble and n-butanol-insoluble fractions were found to be inactive at this dose. At autopsy on Day 10 postcoitum, 7–25% loss in body weight was recorded at the minimum effective contraceptive dose (MED) in rats treated with the ethanolic extract as well as its chloroform-soluble fraction on Days 1–7, 1–5 and 1 postcoitum, in comparison with the 6–7% increase in body weight observed in vehicle control rats. There was however no mortality in any of the treatment groups. The active ethanolic extract and its chloroform fraction were devoid of any estrogen agonistic or antagonistic activity at their respective MEDs in the ovariectomized immature rat bioassay. Efforts are being made to isolate the active principles devoid of effect on body weight. Conclusions The findings suggest the potential for developing products of this plant as contraceptives for human use and welfare. In addition, characterization of the agents responsible for body weight decrease and evaluation of their mechanism of action and safety profile, with or without contraceptive efficacy, might have added advantage for the management of obesity.

Laxative Activity of Cassia auriculata Pods in Rats

Objective: To evaluate ethanol extract of pods of Cassia auriculata Linn at different doses (100, 200 mg / kg, p.o.) for laxative activity in rats. Materials and Methods: The ethanol extract of pods of Cassia auriculata was obtained by continuous soxhlet extraction and further assessed for laxative activity by charcoal meal test and feacal output in experimental rats and compared with standard senna. The extract was subjected to qualitative chemical analysis to identify the phytoconstituents. Results: Upon evaluation of Laxative activity on experimental animals, the ethanol extract at the dose 200 mg / kg, p.o. showed significant (P<0.001) laxative activity as observed from different evaluation parameters. However, the same at the dose 100 mg / kg, p.o. was less significant. The ethanol extract showed the presence of flavonoids, triterenoids, tannins, sterols and anthracene derivatives. Conclusion: From the results, it is revealed that, the active ethanol extract (200 mg / kg, p.o.) of Cassia auriculata pods is worthwhile to develop the bioactive principle for laxative activity and it is also concluded that, the anthracene derivatives present, could be attributed for the laxative activity.

Radioprotective Property of Emblica officinalis. Fruit Ethanol Extract

The radioprotective activity of Emblica officinalis. Gaertn. (Euphorbiaceae) ethanol extract (EOE) has been studied using rat liver mitochondria and pBR 322 plasmid DNA as two model in vitro. systems. EOE could effectively prevent γ-ray–induced lipid peroxidation as assessed by measuring thiobarbituric acid reactive substrates, lipid hydroperoxide, and conjugated diene. It also protected mitochondrial SOD against γ-ray–induced damage. Likewise, it prevented radiation-induced DNA strand breaks in a concentration-dependent manner. The radioprotective activity of EOE could be attributed to its hydroxyl and superoxide radicals scavenging property along with its lymphoproliferative activity. The radical scavenging capacity of EOE could be attributed to its constituent phenolics. The in vitro. radioprotective activity of EOE was significantly better compared with the in vivo. results reported earlier by others with the aqueous extract or fruit pulp of E. officinalis.. The higher concentrations of the more bioavailable phenolics such as gallic acid and ellagic acid in EOE compared with the other preparations might possibly account for the results.

Activities of some Brazilian plants against larvae of the mosquito Aedes aegypti

The insecticidal activities of extracts and oils of seventeen medicinal plants of Brazil have been determined using an Aedes aegypti larvicidal bioassay. Oils from Anacardium occidentalis, Copaifera langsdorffii, Carapa guianensis, Cymbopogon winterianus and Ageratum conyzoides showed high activities with LC 50 values of 14.5, 41, 57, 98 and 148 μg/l, respectively. The most active ethanolic extract tested was that from the stem of Annona glabra which presented an LC 50 value of 27 μg/l. The potential application of cashew nut oil, an industrial by-product with low commercial value, in the control of the vector of dengue and yellow fever, may be proposed.

Effect of Cassia auriculata Linn Flowers Against Alloxan-Induced Diabetes in Rats

Objective : To evaluate the antidiabetic activity of flowers of Cassia auriculata Linn against alloxaninduced diabetes in rats and to isolate the bioactive constituents from the activity guided fraction. Materials and methods : The ethanola β sitosterol, was isolated from ethanol extract by column chromatography. Results : In alloxan-induced diabetic rats the ethanol extract (250 mg/kg, p.o.) showed significant (P<0.001) antidiabetic activity as observed from serum glucose level in diabetic rats. However, the aqueous extract (250 mg/kg, p.o.) did not significantly reduce the serum glucose level in diabetic rats. The ethanol extract showed the presence of sterols, triterpenoids, flavonoids and tannins. Conclusion : From the results, it is revealed that, the active ethanol extract of Cassia auriculata flowers is worthwhile to develop the bioactive principle for diabetes mellitus and it is also concluded that the isolated sterol; β sitosterol, could be attributed for antidiabetic activity.

Antiimplantation and pregnancy interruption efficacy of Rivea hypocrateriformis in the rat

Petroleum ether, chloroform, ethanol and distilled water extracts of the aerial parts of the plant Rivea hypocrateriformis (Convolvulaceae) were tested for antiimplantation and pregnancy interruption properties in female albino rats. Among these, the ethanol extract was found to be most effective in causing significant antiimplantation and interruption of early pregnancy. The antifertility activity of ethanol extract was reversible on exogenous administration of hydroxy progesterone. However, the same ethanol extract was found to be ineffective in interruption of late pregnancy. Among the four extracts subjected to preliminary phytochemical screening, the active ethanol extract showed positive tests for alkaloids, glycosides, saponins, tannins and phenolic compounds.

In-vivo antimalarial activity ofCassia occidentalism Morinda morindoidesandPhyllanthus niruri

The ethanolic, dichloromethane and lyophilized aqueous extracts of Cassia occidentalis root bark, Morinda morindoides leaves and whole plants of Phyllanthus niruri were evaluated for their antimalarial actvity in vivo, in 4-day, suppressive assays against Plasmodium berghei ANKA in mice. No toxic effect or mortality was observed in mice treated, orally, with any of the extracts as a single dose, of 500 mg/kg body weight, or as the same dose given twice weekly for 4 weeks (to give a total dose of 4 g/kg). No significant lesions were observed, by eye or during histopathological examinations, in the hearts, lungs, spleens, kidneys, livers, large intestines or brains of any mouse. At doses of 200 mg/kg, all the ethanolic and dichloromethane extracts produced significant chemosuppressions of parasitaemia (of > 60% for C. occidentalis root bark and Ph. niruri whole plant, and of 30% for M. morindoides leaves) when administered orally. The most active ethanolic extract, that of Ph. niruri, reduced parasitaemia by 73%. The dichloromethane extracts of M. morindoides and Ph. niruri produced similar reductions (74% and 72% chemosuppression, respectively), whereas that of C. occidentalis was slightly less active (60% chemosuppression). Each lyophilized aqueous extract was less active than the corresponding ethanolic extract.

3-Methoxysampangine, a novel antifungal copyrine alkaloid from Cleistopholis patens

Further examination of the active ethanolic extract of the root bark of Cleistopholis patens by using bioassay-directed fractionation resulted in the isolation of a new alkaloid, 3-methoxysampangine (compound I), together with three known alkaloids, eupolauridine (compound II), liriodenine (compound III), and eupolauridine N-oxide (compound IV). The proposed structure of compound I was based on its physicochemical properties and spectral data. 3-Methoxysampangine exhibited significant antifungal activity against Candida albicans, Aspergillus fumigatus, and Cryptococcus neoformans. This is the first report of the isolation of liriodenine (compound III) from the root bark of C. patens.

Spinosides A and B. Two cytotoxic cucurbitacin glycosides from Desfontainia spinosa

Fractionation of the active ethanol extract of Desfontainia spinosa based on cytotoxicity has led to the discovery of three new derivatives of the parent compound, 1 1-deoxocucurbitacin I. The structures of 23,24-dihydro-11-deoxocucurbitacin I and the glycosides, spinosides A and B were elucidated on the basis of extensive analysis of their high field 1H NMR, 13C NMR, high resolution mass spectra (fast atom bombardment, field desorption, chemical ionization, electron impact) and chemical interconversions. Spinosides A and B were cytotoxic in the KB cell culture assay.