Ethanol Extract Of Whole Plant Research Articles

Phytochemical investigation, in-vitro antiplasmodial assessment and cytotoxic effect of ethanol extract of whole plant of Crotalaria arenaria (Benth)

Crotataria arenaria (Benth) is a native plant from Northern part of Nigeria which is employed as antimalarial herb in traditional medicine in the communities where it grows. The phytochemical composition, In-vitro antiplasmodial activity and in-vitro cytotoxic effect of the extract and fractions of the whole plant of Crotalaria arenaria were investigated. The mature and fresh whole plant of C. arenaria were collected, air dried and pulverized. The pulverized form of the plant were soaked in ethanol for two weeks and later decanted, filtered and concentrated using rotatory evaporator at 40oC and evaporated to dryness and labeled CRA-1. The dried ethanol solid extract (CRA-1) was patitioned/fractionated using water, chloroform, ethyl acetate, 18% aqueous methanol, n-hexane which afforded chloroform fraction (CRA-1-01), water fraction (CRA-1-02), ethyl acetate fraction (CRA-1-03) aqueous methanol fraction (CRA-1-04) and n-hexane (CRA - 1- 05) and they were dried and tested for their photochemicals and In-vitro antiplasmdial activity against Plasmodium falciparum strain (K1). The ethanol extract and its fractions were found to significantly inhibited/suppressed multi-drug resistant strain of P. falciparium (K1) in the range of 86.73% - 65.31% at varied concentrations of 5000 µg/ml, 2000 µg/ml, 1000 µg/ml and 500 µg/ml. The ethanol extract and its fractions showed the presence of tannins, saponins and alkaloids which could be responsible for the In-vitro antiplasmodial activity of the whole plant extract of C. arenaria and each of its fractions. Ethanol crude extracts of whole plant of Crotalaria arenaria and its fractions were investigated for cytotoxicity in Brine shrimp lethality Test (BSLT). Larvicidal activities were noticed with dosage concentration from 1000 µg/ml down to 10 µg/ml of the plant extract and all its fractions. The relative cytotoxic effects of extract and fractions obtained from whole plant of Crotalaria arenaria were found to be dose-dependent because higher dosage brought about an increase in mortality of Artemia salina Leach. Sea salty water of the crude ethanol extract and its fractions served as the negative control. The chloroform fraction was observed to be most cytotoxic killing 30% of brine shrimp larvae at lowest concentration of 10 µg/ml with average percentage lethality of 46.67%. Aqueous methanol and ethanol crude extract appears to show similar and closely related activities against brine shrimp larvae at highest concentration of 1000 µg/ml. The ethanol crude extract and aqueous methanol fractions are toxic at higher dosage as they were found to induce significant mortality effect (In-vitro) against Artemia salina Leach particularly at concentration of 1000 µg/ml and therefore not safe for oral consumption especially at higher uncontrolled doses but at relatively low/moderate doses. The findings in this present study demonstrated that the extract of C. arenaria (whole plant) and fractions have significant in vitro antiplasmodial activity and this has justified the traditional use of the whole plant extract of Crotaria arenaria in the folklore medicine to cure malaria related illness. The results obtained in this study may serve as key data for utilization of Crotalaria arenaria in the development of bioactive agents which could be used as antimalarial, anticancer, pesticidal, insecticidal and anti-proliferation agents. The study recommended in-vivo antiplasmodial assay of the extract of the whole plant of Crotalaria arenaria to further substantiate the findings of this present study.

Physicochemical Constituent, Phytochemical Analysis and Antimicrobial Activity in Ethanolic Extract of Cyanotis Axillaris

Cyanotis axillaris belong to family Commellianaceae. The present investigation deal with the physicochemical constituent, phytochemical analysis and antimicrobial activity in ethanolic extract of whole plant of Cynotis axillaris. The plant part decoction used in Ayurveda to cure many diseases [2]. The evaluation of physicochemical constituents was carried out by ash value, extractive value and phytochemical constituent in plant. The antibacterial activity was tested by cup plate agar diffusion method. The antibacterial activity carried out against E. coli, Staphylococcus Aureus, Bacilis subtilis and Proteus species

IMMUNOMODULATORY ACTIVITY OF PORTULACA QUADRIFIDA IN MALE ALBINO WISTAR RATS

Immunomodulators are substances that stimulate, restore, suppress, or help to produce (adjuvant) or increase the desired immune response. Portulaca quadrifida is a traditional plant in the Ayurvedic system of medicine which has been reported to show a variety of therapeutic activities. This study was performed to investigate the immunomodulatory activity of P. quadrifida. Ethanolic extract of whole plant was administered orally at doses of 200 mg kg-1 and 400 mg kg-1 and septilin was used as reference standard. Septilin from Himalaya herbals is an ayurvedic polyherbal formulation. Septilin contains extracts and powders of Balsamodendron mukul and Shankh bhasma, and extracts of Maharasnadi quath, Tinospora cordifolia, Rubia cordifolia, Emblica officinalis, Moringa pterygosperma and Glycyrrhiza glabra. Septilin has been reported to possess immunomodulatory and antibacterial activity and it has been used in treatment of acute and chronic infections. The activity was determined by measuring delayed-type hypersensitivity, antibody titre, neutrophil adhesion and haematological parameters in sensitized rats. The study showed that there was significant increase in the total white blood cell count, antibody titre strength and neutrophil adhesion. The results clearly indicate that P. quadrifida shows potential immunostimulant activity at doses of 200 mg kg-1 and 400 mg kg-1.

In vivo Antioxidant and Lipid Peroxidation Effect of Ethanolic Extract of whole Plant of Ziziphus Xylopyrus Retz. In Rats Fed with High Fat Diet.

In vivo Antioxidant and Lipid Peroxidation Effect of Ethanolic Extract of whole Plant of Ziziphus Xylopyrus Retz. In Rats Fed with High Fat Diet.

Amides and lignans from Solanum lyratum

Sixteen non-steroidal compounds including four amides, six lignans, two sesquiterpenoids and three flavonoids, were isolated from the 80 % ethanol extract of whole plants of Solanum lyratum Thunb. Their structures were assigned based on analyses of extensive spectroscopic data (including MS, 1D/2D NMR and ORD) or comparisons of the NMR data with those reported. Among them, there were a new lignan namely isolariciresinol-9-acetate (5), a new natural amide compound (E)-N-(2-hydroxy-2-(4-hydroxyphenyl)ethyl)-3-(4-hydroxyphenyl)acrylamide (1), and two known lignans officinalioside (6) and alangilignoside B (7), together with other twelve known compounds. 6 and 7 were isolated from S. lyratum for the first time, In addition, in vitro anticancer activities of all these isolates were evaluated by MTT assay and the result indicated that compounds 3 [(E)-3-(4-hydroxy-3-methoxyphenyl)-N-(2-(4-hydroxyphenyl)-2-methoxyethyl)acrylamide] and 6 significantly inhibited the activities of HepG2 liver cancer cells.

Phytochemical and Pharmacological Evaluation of Alternanthera pungens

The aim of the present study was to evaluate pharmacognostical and antimicrobial, antioxidant, anti-inflammatory activity of ethanolic leaf extracts of Alternanthera pungens. The collected plants were washed, dried, cut and ground into coarse powder and macerated with ethanol and extract was dried by rotary vacuum. Phytochemical screening of ethanol extract revealed the presence of steroids, flavonoids, saponins, glycoside, phenols, and proteins. However, alkaloids and glycosides were absence in this species. The ethanolic extract of whole plant of A. pungens was subjected to column chromatography to separate pure compounds. Invitro antioxidant activity was performed by 2, 2 -diphenyl- 1- picrylhydrazyl (DPPH) assay, hydroxy radical scavenging method and superoxide radical scavenging activity. The ethanolic extract of A. pungens was evaluated against antimicrobial activity against two fungal and four bacterial strains. The extracts showed remarkable inhibition of zone of bacterial and results were comparable with that of standard drugs against the organism tested.

Antifungal activity of ethanolic extract of Sphaeranthus indicus Linn. against Dermatophytes and Candida species

Background: Sphaeranthus indicus as an entire plant or the specific parts like roots, leaves, flowers are used for treating helminthiasis, jaundice, diabetes, dyspepsia, fever, cough, hernia, gastritis, hemorrhoids, migraine, leprosy and skin diseases. The objective of this study was to evaluate the antifungal activity of ethanolic extract of the whole plant Sphaeranthus indicus Linn. Methods: The antifungal activity of ethanolic extract of the whole plant Sphaeranthus indicus Linn was evaluated by incorporating the extract in Sabourauds dextrose agar. This property was studied in vitro using the ethanolic extract on Candida albicans, Microsporum gypseum, Trichophyton mentagrophytes and Epidermophyton floccosum by using Clotrimazole as standard drug.Results: This study revealed that the ethanolic extract of Sphaeranthus indicus is having good antifungal activity against Dermatophytes and Candida species. Conclusions: This study demonstrates the promising antifungal action of ethanolic extract of whole plant of Sphaeranthus indicus Linn. This feature can be exploited in the development of a newer antifungal agent from plant.

In vitro evaluation of antibacterial activity in ethanolic extract of whole plant Sphaeranthus indicus Linn.

Background: Sphaeranthus indicus Linn is a widely used medicinal plant in Indian traditional system of medicine against human pathogens. Alarming bacterial resistance is urging scientist to search for newer anti-microbial substances from the medicinal plants. The objective of the study was to evaluate the antibacterial activity of ethanolic extract of the whole plant Sphaeranthus indicus Linn (Asteraceae).Methods: The antibacterial activity of ethanolic extract of whole plant of Sphaeranthus indicus Linn was done against Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Staphylococcus aureus in Mueller Hinton Agar (MHA) and compared with ciprofloxacin as standard by disc diffusion method.Results: The study revealed that there was no zone of inhibition in doses of 100 mcg, 200 mcg and 300 mcg of ethanolic whole plant extract of Sphaeranthus indicus in MHA plates compared with ciprofloxacin 30 mcg.Conclusions: Ethanolic extract of Sphaeranthus indicus does not have antibacterial activity. Further studies are needed in different extracts and parts of the plant. Simultaneous studies can be done in different places to evaluate environmental factors and regional variations.

PHYTOCHEMICAL SCREENING OF ETHANOLIC EXTRACT OF WHOLE PLANT OF SIDA GLUTINOSA

Objective: The aim of the present study is to screen for the phytochemical constituents which are of pharmacological importance present in the ethanolic extract of whole plant of Sida glutinosa (SG). 
 Methods: The ethanolic extract of the dried whole plant of SG is subjected to preliminary phytochemical screening which showed the presence of major phytoconstituents such as phenols, flavonoids, and alkaloids. The extract was screened for its antioxidant activity by 2,2-diphenyl-1- picrylhydrazyl, hydroxyl radical, Iron (III) to Iron (II) reducing activity, and nitric oxide scavenging assay. Further, the ethanolic extract was subjected to fingerprinting technique high-pressure thin-layer chromatography (HPTLC). Reverse phase high-pressure liquid chromatography (Rp-HPLC) was performed to estimate the amount of total phenolics, flavonoids, and alkaloids quantitatively in isocratic mode.
 Results: Phytochemical screening of the ethanolic extract of the plant showed the presence of pharmacologically important constituents such as alkaloids, flavonoids, phenolics, and terpenoids. The study also revealed the potential antioxidant activity of the extract with IC50 value. The extract fingerprinting through HPTLC revealed the presence of various phytoconstituents. Rp-HPLC showed 0.35±0.12 μg/ml of total phenolics, 0.0013±0.05μg/ml of alkaloids, and 0.00081±0.08 μg/ml of flavonoids.
 Conclusion: Scientific evaluation of SG which has therapeutic significance was carried out which is an important concept for the standardization of the plant-based drug. Further, there is a need for isolation and characterization of the lead molecules their systemic evaluation for its pharmacological activities.

Evaluation of Antidiabetic Activity of Ethanolic Extract of Ajuga Parviflora in Diabetic Rats

The aim of the study was to evaluate the antidiabetic activity of ethanolic extract of whole plant of Ajuga parviflora in diabetic induced Sprague Dawley rats. Acute toxicity study was done on screened rats for 14 days. The rats were divided into four groups like normal, diabetic, treated and standard (diabetes treated with Glibenclamide). Streptozocin 160mg /kg body weight was administered intra peritoneally to rat for the induction of diabetes. After the confirmation of diabetes, the rats were subjected to further in-vivo studies. The formulation obtained by ethanolic extract of whole plant of Ajuga parviflora (60mg/kg) were administered orally to diabetic rats for 28 days. The body weight and fasted blood glucose level measured in diabetic and non-diabetic rats at the end of experiments. The formulation shows significant reduction in blood glucose level in Streptozocin induced rats that is comparable to Glibenclamide.. Methanolic extract of medicinal herb Ajuga parviflora Benth. was evaluated for phytochemical screening the plant extract showed the presence of aromatic compounds, carbohydrates and others. Keywords: Ajuga parviflora, Sprague Dawley rat, Streptozocin , Phytochemical screnning.

Sonchus oleraceus Linn protects against LPS-induced sepsis and inhibits inflammatory responses in RAW264.7 cells

Ethnopharmacological relevanceSonchus oleraceus Linn (SOL) belongs to family of Asteraceae, is a traditional medicinal plant, which has been used to treat tumor, inflammatory diseases, infection and so on in Chinese folk culture. Aim of the studyThis work investigated the influence of aqueous ethanol extract of whole plant of SOL and contribution of its main components on inflammation Methods and resultsOral administration of SOL (10 mg/kg) to mice reduced the expression of inflammatory cytokines including IL-6, IL-1β, and TNF-α, in the LPS-induced sepsis mouse model. Major phenolics in SOL were isolated and determined by HPLC. Results indicate that SOL at the concentration range from 25 to 100 μg/mL and its main components, chlorogenic acid, caffeic acid (25–100 μM) significantly reduced the pro-inflammatory cytokine IL-1β, IL-6, TNF-α, attenuated iNOS and COX-2 expression in LPS-stimulated Macrophages. In addition, western blot analysis showed SOL suppressed inducible nitric oxide synthase (iNOS) protein expression and the phosphorylation of extracellular signal-regulated kinase (ERK), p38, c-Jun N-terminal kinase (JNK). ConclusionThe underlying mechanism of anti-inflammation might be in according with the inhibition of MAPKs activation as well as down regulation of iNOS and cyclooxygenase-2 (COX-2).

Ameliorative Potential of Eclipta alba on Gentamycin Induced Renal Toxicity in Rats

Nephrotoxicity is a common event, which can cause significant morbidity and can be easily overlooked. Gentamycin is an antimicrobial agent which can cause nephrotoxicity on prolonged use. A large number of herbs have traditionally been used to treat drug or toxin-induced renal diseases. The present study was a similar attempt in that direction to evaluate the nephroprotective activity of ethanolic extract of whole plant of Eclipta alba against gentamycin induced nephrotoxicity. The animals were divided into five groups (n=6) consisting of normal control, toxic control and three test groups which received different doses of the extract (100,200 & 400mg/kg, p.o). Nephroprotective effect of ethanolic extract of Eclipta alba was evaluated by assessing the blood parameters and histopathological studies of kidney. Elevated levels of serum urea, serum creatinine, total protein and uric acid have been significantly reduced in dose depending manner by oral administration of ethanolic extract of whole plant of Eclipta alba. These observations were supported by histopathological studies.

Studies on the Antimicrobial Activity of Ethanolic Extract of Whole Plant of Saccharum Spontaneum (Linn.)

Studies on the Antimicrobial Activity of Ethanolic Extract of Whole Plant of Saccharum Spontaneum (Linn.)

Preliminary Phytochemical Analysis and Invitro Antiviral Activity of Ethanolic extract of Whole plant of Tinospora cordifolia (Thunb.) Miers against Hepatitis-A Virus

Preliminary Phytochemical Analysis and Invitro Antiviral Activity of Ethanolic extract of Whole plant of Tinospora cordifolia (Thunb.) Miers against Hepatitis-A Virus

DETERMINATION OF BIOACTIVE COMPONENTS OF CARALLUMA UMBELLATA HAW. (APOCYNACEAE) BY GAS CHROMATOGRAPHY AND MASS SPECTROSCOPY ANALYSIS

Objective: The aim of this study was to carry out Gas Chromatography and Mass Spectroscopy (GC–MS) studies and to determine the bioactive compounds of Caralluma umbellata whole plant extract.Methods: Whole plant of C. umbellata was cleaned, shade dried, and pulverized to powder in a mechanical grinder. Required quantity of powder sample was weighed and transferred to stoppered flask separately and treated with ethanol until the powder is fully immersed. The flask was shaken every hour for the first 6 h and then it was kept aside and again shaken after 24 h. This process was repeated for 3 days and then the extracts were filtered. The extracts were collected and evaporated to dryness using vacuum distillation unit.Results: A total of 29 components of C. umbellata whole plant were identified. The prevailing components in the ethanol extract of whole plant were betulin (16.11%), campesterol (11.69%), 5α-Ergost-8(14)-ene (10.16%), 5-androsten-17α-ethynyl-3β, 17β-diol (9.06%), β-sitosterol (8.17%), cholestane-3,7,12,25-tetrol, tetraacetate (3α,5β,7α,12α) (7.94%), β-amyrin (7.02%), stigmasterol (6.78%), 13,16-octadecadiynoic acid, methyl ester (3.53%), lanosterol (3.51%), trans-geranylgeraniol (3.25%), Vitamin E (2.90%) and retinol, acetate (2.81%).Conclusion: The application of C. umbellata for various ailments is confirmed by the presence of various bioactive compounds by traditional practitioners.

Antiurolithic and antioxidant activity of ethanol extract of whole-plant Biophytum sensitivum (Linn.) DC in Ethylene-Glycol-induced urolithiasis in rats

Background: Biophytum sensitivum Linn. DC is considered as one of the ten sacred plants called as “Dasapushpam” of Kerala state in India. Grounded leaves of this plant have been used conventionally as antiurolithic and diuretic. 'However, enough scientific evidences were not available about the effect of this plant as nephroprotective and antiurolithic. Objective: The present study was undertaken to investigate antiurolithic and antioxidant activity of ethanol extract of whole plant B. sensitivum Linn. DC (EEBS) on ethylene-glycol (EG)-induced urolithiasis in Wistar albino rats. Materials and Methods: EG 0.75% v/v in drinking water was fed to all groups, except the control group for 28 days to induce urolithiasis in rats. Groups I, II, and III served as control, toxic control, and standard Cystone groups, respectively. Animals in Group IV were administered with EEBS from 15th day to 28th day, while Group V animals were administered with EEBS from 1st day to 28th day. Several renal functional and injury markers in urine and serum were determined. Antioxidant enzyme activities were also recorded. Results: Co-administration with EEBS exhibited protective effect against EG-induced proteinuria, hypercalciuria, hypomagnesuria hypercalcemia, and hyperphosphatemia. Serum protein levels were significantly increased, whereas blood urea nitrogen, creatinine, and uric acid levels were significantly lowered. EEBS-treated rats significantly attenuated the aberrations in the antioxidant enzyme activities, body weight, kidney weight, urine output, and urine pH compared to toxic control animals. Conclusion: Hence, this study confirmed the usefulness of B. sensitivum as an antiurolithic and antioxidant agent. Abbreviations Used: EEBS: Ethanol extract of Biophytum sensitivum, EG: Ethylene-glycol, B.wt: Body weight, TP: Total protein, Ca: Calcium, Mg: Magnesium, BUN: Blood urea nitrogen, K.wt: Kidney weight, SOD: Superoxide dismutase, GPx: Glutathione peroxidase, GSH: Reduced glutathione, MDA: Malondialdehyde.

Effect of Ethanolic Extract Fractions of Boerhaavia diffusa in Doxorubicin-induced Myocardial Toxicity in Albino Rats

: Background: Doxorubicin is a Anthracycline derivative and has proven efficacy in various malignancies. It is the most effective cytotoxic agent in current use. The clinical usefulness is limited due to its cardiac toxicity. Objectives: To study the preventive role of ethanolic extract fractions of Boerhaavia diffusa (BD) against doxorubicin (Dox) induced myocardial toxicity in albino rats. Methods: The ethanolic extract of whole plant of Boerhaavia diffusa was prepared by hot extraction method and further fractionated into Petroleum ether (PEBD), Chloroform (CLBD), Ethyl acetate (EABD) and Aqueous (AQBD) fractions by increasing in order of polarity. Cardiotoxicity was produced by cumulative administration of Dox (2.5 mg/kg, i.p. alternative day for two weeks). All four fractions (PEBD-20 mg/kg, CLBD-25 mg/kg, EABD-30 mg/kg and AQBD-25 mg/kg) and vitamin E as standard (100 mg/kg) were administered orally as pretreatment for two weeks followed by Dox on alternative days for two weeks. The general observations, biomarker enzymes like lactate dehydrogenase (LDH), Creatine kinase (CK-MB) and Troponin-I (cTnI), biochemical parameters such as aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were monitored after three weeks of last dose. Myocardial toxicity was also evaluated by histopathologic studies. Results: Repeated administration of Dox-induced cardiomyopathy characterized with an increased level of biomarkers and antioxidant deficit. Pretreatment with the EABD and Vit-E significantly protected myocardium from the toxic effects of Dox by reducing the elevated level of biomarker enzymes like LDH, CK-MB, biochemical parameters such as AST and ALT, absence of cTnI and restoring of disorganized myocardial tissue to normal. Conclusion: The biomarker, biochemical and histopathological data evidently substantiate the cardioprotective effect of EABD, which could be attributed to flavanoids present in the ethyl acetate fraction.Key words: Boerhaavia Diffusa, Cardiotoxicity, Doxorubicin, Troponin-I, CKMB.

Effect of Solanum nigrum Linn on Acute and Sub-Acute Models of Inflammation

Objective: The aim of the study was to see the effect of ethanolic extract of Solanum nigrum Linn on Acute and Sub-acute inflammation. Method: Wistar rats weighing 150-200gms were used, divided into four groups Group 1 was control group, two groups Group 2 and 3 treated with the plant extracts at 100 & 200 mg/kg b.w and Group 4 treated with indomethacin, 10 mg/kg b.w. Acute inflammation was induced by injecting 0.1 mL of 1% homogenized carrageenan suspension in normal saline to the right hind paw of the rats prior to which drug treatment was given and paw volume was measured using a digital plethysmometer. Sub-acute anti-inflammatory studies were carried out as described by winter and Porter and hematological parameters were estimated. The granuloma tissue formed during the proliferative process was isolated and wet and dry exudates formation was estimated in various treatment groups. The effect of extract and indomethacin on vital organs like liver, kidney, stomach was also studied by performing histological studies. Results: Study shows that the hydroalcoholic extract of whole plant of Solanum nigrum L. is effective only at higher dose effectively suppressing carrageenan induced inflammation suggesting the inhibition of release of prostaglandin, bradykinin, leukotrienes and polymorphonuclear cells. The histological studies further confirm the anti-inflammatory property of the extract while simultaneously maintaining normal cellular architecture of vital organs than as compared to indomethacin treated group. Conclusion: The ethanolic extract of whole plant of Solanum nigrum Linn shows promising anti-inflammatory activity on both acute and sub-acute stages of inflammation. Key words: Acute Inflammation, Sub-acute Inflammation, Anti-inflammatory activity, Solanum nigrum , Hematological parameters, Histological studies.

Three new C-27-carboxylated-lupane-triterpenoid derivatives from Potentilla discolor Bunge and their in vitro antitumor activities

Three new lupane-triterpenoids (1–3) along with six known compounds (4–9) were isolated from the ethanolic extract of whole plant of Potentilla discolor Bunge. The structures of Compounds 1–3 were established by extensive 1D and 2D NMR together with other spectrum analysis, indicating that their C-27 positions were highly oxygenated, which were rarely found in nature. Their in vitro anti-proliferative activities against HepG-2, MCF-7 and T-84 cell lines were evaluated by Cell Counting Kit-8 (CCK-8) assay, and the results showed different activities for three cell lines with IC50 values ranging from 17.84 to 40.64 μM. In addition, the results from Hoechst 33258 and AO/EB staining as well as annexinV-FITC assays exhibited Compound 1 caused a markedly increased HepG-2 cellular apoptosis in a dose-dependent manner. The further mechanisms of Compound 1-induced cellular apoptosis were confirmed that 1 induced the production of ROS and the alteration of pro- and anti-apoptotic proteins, which led to the dysfunction of mitochondria and activation of caspase-9 and caspase-3 and finally caused cellular apoptosis. These results would be useful in search for new potential antitumor agents and for developing semisynthetic lupane-triterpenoid derivatives with high antitumor activity.

Anemone rivularis inhibits pyruvate dehydrogenase kinase activity and tumor growth

Ethnopharmacological relevanceAnemone rivularis Buch.-Ham. ex DC. (Ranunculaceae) have been used as a traditional remedy for treatment of inflammation and cancer. However, there is no report demonstrating experimental evidence on anti-tumor action of A. rivularis. Aim of studyThe Warburg's effect, preference of aerobic glycolysis rather than oxidative phosphorylation (OXPHOS) even in oxygen rich condition, is focused as one of major characteristics of malignant tumor. Thus, we investigated the effect of A. rivularis on the Pyruvate dehydrogenase (PDH) kinases (PDHKs), a major molecular targets for reducing aerobic glycolysis. Materials and methodsThe ethanol extract of whole plant of A. rivularis (ARE), fingerprinted by high performance liquid chromatography (HPLC), was applied to in vitro and cell-based PDHK activity assays. The effect of ARE on cell viabilities of several tumor cells was estimated by MTT assay. The expression of phosphor-PDH, PDH and PDHK1 were measured by Western blot analysis. The production of reactive oxygen species (ROS) and apoptosis was measured by fluorescence-activated cell sorting analysis, using 5-(and-6)-carboxy-2′,7′-dichlorodihydrofluorescein diacetate (carboxy-H2DCFDA) and Annexin V/propidium iodide (PI) staining, respectively. Mitochondrial membrane potential was examined by tetramethylrhodamine methyl ester (TMRM) staining. In vivo anti-tumor efficacy of ARE was estimated by means of tumor volume and weight using allograft injection of murine Lewis lung carcinoma (LLC) cells to dorsa of C57BL/6 mice. ResultsARE inhibited the viabilities of several cancer cells, including MDA-MB321, K562, HT29, Hep3B, DLD-1, and LLC. ARE suppressed PDHK activity in in vitro kinase assay, and also inhibited aerobic glycolysis by reducing phosphorylation of PDHA in human DLD-1 colon cancer and murine LLC cells. The expression of PDHK1, a major isoform of PDHKs in cancer, was not affected by ARE treatment. Moreover, ARE increased the both ROS production and mitochondrial damage. In addition, ARE suppressed the in vitro tumor growth through mitochondria-mediated apoptosis. The growth rates of allograft LLC cells were also reduced by ARE treatment. ConclusionsHere, we firstly report that ARE inhibits PDHK activity and growth of tumor in both in vitro and in vivo experiments. Therefore, we suggest ARE as a potential candidate for developing anti-cancer drugs.