Leonotis Leonurus Research Articles

In vivo validation of Aloe ferox (Mill). Elephantorrhiza elephantina Bruch. Skeels. and Leonotis leonurus (L) R. BR as potential anthelminthics and antiprotozoals against mixed infections of gastrointestinal nematodes in goats

Aloe ferox (Mill)., Elephantorrhiza elephantina Bruch. Skeels. and Leonotis leonurus (L) R. BR. are some of the plants used by farmers in the Eastern Cape Province to control worms in goats, but information on their efficacy is lacking. The study was conducted to determine efficacy of these plants on gastrointestinal nematodes in natural mixed infections in goats. Forty-eight male goats aged 8-12months were divided into eight groups (Treatments A-H) of six animals each, balanced in terms of liveweight and worm egg count. Treatments A to F received plant extracts, three animals in each group receiving doses of 250mg/kg and the other three receiving 500mg/kg at concentration of 100mg/ml, while those in G and H received Valbazen® (11.36% albendazole) at 10mg/kg, and 0.5ml/kg distilled water, respectively per os. Faecal samples were collected on days0, 3, 6 and 9 for faecal egg counts (FEC), and body weights recorded on days1 and 9. Results showed significant reductions (P < 0.05) in strongyle eggs by A. ferox extract at dose levels of 500mg/kg on days3, 6 and 9, while reductions in Eimeria spp. oocysts were observed on days3, 6 and 9 for animals that received 500mg/kg doses. E. elephantina caused significant reduction (P < 0.05) of Trichuris spp. eggs on days3 and 6, respectively at 250mg/kg dose level, whereas L. leonurus also caused significant reduction (P < 0.05) in FEC of Trichuris spp. and Eimeria spp. oocysts at 250mg/kg dose level on day9. Albendazole caused reductions (P < 0.05) in strongyle eggs on days3 and 6, Trichuris spp. on days3, 6 and 9, and on coccidia, it caused a reduction (P > 0.05) on day1, whereas on days6 and 9, there was an increase. On total mixed infections, highest FECR% were observed with the extract of A. ferox on days3 (53%), 6 (54%) and 9 (58%) at 500mg/kg,whereas albendazole had efficacy levels of 39%, 44% and 29% on days3, 6 and 9, respectively. Body weight of goats from days 1 to 9 were not significant different from the control. The study revealed efficacy of A. ferox, E. elephantina and L. leonurus against gastrointestinal parasites at high doses (500mg/kg), showing that the plants have the potential to be used as anthelminthics.

A Call for a New Connectivity

"Twisting the Lion's Tail" is a valuable and timely contribution to the literature on the need to break down silo thinking and acting. If we stay within a narrow silo by suggesting that researchers generate knowledge, practitioners use the knowledge and then researchers evaluate the results, we will not get to the system thinking view articulated in the lead paper. The author hopes his observations presented in this commentary add to the conversation.

Twisting the Lion's Tail: Collaborative Health Policy Making in British Columbia

The respective roles of government, academia and health authorities in supporting health systems and service delivery research in the context of health policy making have often been unclear. A new strategy is necessary, one that encompasses the interdependence of research and practice and respects different kinds of knowledge and the needs and capacity of all stakeholders. Reform efforts to date have focused mainly on structural change and genuine collaboration has been pushed to the back seat. A major challenge in the health policy making process is expressing not just what we think but how we think, which requires us to be self-aware and critically reflective on how we make sense of our day-to-day realities. Using an analogy with philosophical roots, this essay explores health services research in the context of the BC health system and examines how such research and related activities can be contextualized, understood and applied in health policy making.

Lion King or Aslan: A Tale from Narnia!

In the Chronicles of Narnia series by C.S. Lewis, Aslan the all-powerful but benevolent lion does not need to have his tail twisted; rather, he twists tails to create convergence and harmony in his dream world. In this issue's lead article, "Twisting the Lion's Tail: Collaborative Health Policy Making in British Columbia," the authors discuss the problems regarding better coordination of health services research, knowledge translation and policy making. The roles of academia, health authorities and government are presently unclear, with leadership differences, power discrepancies, conflicting agendas, lag times and systemic structural complexity. Exploring these issues in British Columbia, Lindstrom, MacLeod and Levy advocate a change in perspective from practice gaps to bridging knowledge boundaries. Recommendations include networking of academia, action research and strengthening of relationships between stakeholders. However, a key cohesive element seems missing. Health technology assessment (HTA) is a formidable, dynamic driving force. With over 20 years' experience in HTA, Canada has a number of world-class innovative agencies federally and provincially that actively involve academia to generate evidence for informed policy making. Increased use of evidence-based medicine in research and the clinic may be achieved by augmenting HTA's scientific capacity through the creation of pan-Canadian exchange forums and by boosting the demand for knowledge translation.

Antidiabetic activities of aqueous leaves extract of Leonotis leonurus in streptozotocin induced diabetic rats

The present study was carried out to investigate the antidiabetic properties of aqueous leaves extract of Leonotis leonurus in streptozotocin (45 mg/kg intraperitoneal) induced diabetic rats for 15 days. The induced diabetic rats exhibited high blood glucose level, cholesterol, high density lipoprotein (HDL) and triglycerides accompanied with weight loss while the level of low density lipoprotein (LDL) was very low. In addition, the water intake was remarkably high while feed intake was decreased as compared with normal control group. The continuous oral administration of the extract at the dose of 125, 250 and 500 mg/kg for 15 days was able to lower the blood glucose level, HDL, feed and water intake while that of LDL was increased. Also, the weight loss of diabetic rats (31 g) after extract treatment was near that of glibenclamide treated groups. The extract yielded high phenolics content (48 mg/g tannic acid equivalent) and flavonoids (4.8 mg/g quercetin equivalent). These compounds have been reported to potentiate insulin secretion. The present study revealed that aqueous extract of L. leonurus possesses antihyperglycemia and antilipidemic potential and thus could support ethnotherapeutic usage of this plant.

Quantitative determination of stachydrine via HPTLC in cardioactive Leonurus and Leonotis drugs

Tea preparations from aerial parts of the Central and Eastern European Lamiaceae Leonurus cardiaca L. are traditionally used as a remedy against tachyarrhythmia, heart failure, and other cardiac disorders [1–3]. Nevertheless, a scientific basis for these therapeutic effects had not been established [4] until just recently an antiarrhythmic refined extract was prepared from this drug via bioassay guided fractionation [1], making the development of improved methods of extract characterisation necessary. In Chin.Ph. [5] the „alkaloids“ of the tea preparation of the closely related and similarly used East Asian Leonurus japonicus Houtt. [6] are regarded as the active constituents and quantified photometrically after Reinecke's complexation, calculated as stachydrine. Unfortunately, both the quantification method by complexation and the accompanied TLC method of the Chin.Ph. are deemed to be „not reproducible“ by current experimental literature, such as Heuberger et al. 2008 [7]. Therefore, a state of the art HPTLC method was developed, using a CAMAG automatic HPTLC system with scanner and winCATS analysis software for reproducible stachydrine quantification. Silica gel 60 F254 HPTLC plates were scanned at 517nm after development with MeOH:CH2Cl2:NH325% (8:2:3) and derivatisation with Vágújfalvi solution. The related cardioactive [8–10] South African Leonotis leonurus (L.)R.Br. was co-investigated. These measurements revealed stachydrine contents (w/w) of 0.2 to 1.1% for the L. japonicus drug, 0.3% for the material from L. leonurus, 0.5 to 1.5% for the L. cardiaca samples, and 6.6% for the antiarrhythmic refined extract of L. cardiaca.

How globalization and market innovation challenge how we think about and respond to drug use: ‘Spice’ a case study

How globalization and market innovation challenge how we think about and respond to drug use: ‘Spice’ a case study

Rhizoctonia solani によるアルターナンセラ, レオノチス, ペンタスおよびシバザクラの新病害

Rhizoctonia solani によるアルターナンセラ, レオノチス, ペンタスおよびシバザクラの新病害

Effect of aqueous extract of Leonotis leonurus (L.) R. Br. leaves in male Wistar rats

The aqueous extract of the leaves of Leonotis leonurus (L.) R. Br. at the doses of 125, 250 and 500 mg/kg body weight was investigated for toxicity in male rats following administration on daily basis for 21 days. The extract did not significantly (p > .05) alter the levels of haemoglobin, packed cell volume, mean corpuscular volume, red cell distribution width, basophils, total protein, phosphorus, calcium and chloride ions of the animals. Whereas the levels of lymphocytes, eosinophils, monocytes, triacylglycerol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, atherogenic index, albumin as well as alkaline phosphatase and gamma glutamyl transferase activity were decreased by the extract, those of neutrophil, magnesium, total and conjugated bilirubin, alanine and aspartate aminotransferase as well as liver and kidney body weight ratios increased. There was decrease in the mean corpuscular haemoglobin, mean corpuscular haemoglobin concentration and cholesterol only at the 500 mg/kg body weight of the extract, whereas the large unstained cells, sodium ions, white blood cells and uric acid increased only at 250 and 500 mg/kg body weight of the extract, respectively. The urea, creatinine and potassium increased only at 125 mg/kg body weight of the extract while the globulin content was elevated only at 500 mg/kg body weight of the extract. The doses did not produce any definite pattern of effect on the red blood cells and platelets. These alterations by the aqueous extract of L. leonurus leaves on the haematological together with the liver and kidney functional indices suggests parameter and dose-selective effects of the extract and will have consequential effects on the normal functioning of the blood system, kidney and liver of the animals. The extract is also unlikely to predispose the animals to cardiovascular risk when repeatedly consumed on daily basis at the doses investigated for 21 days. Therefore, the aqueous extract of L. leonurus leaves may not be 'safe' as oral remedy in male rats.

Phytochemical and pharmacological studies on Leonotis leonurus

The present study aimed at isolation of the flavonoid constituents of Leonotis leonurus R. Br. (Lamiaceae) flowering aerial parts, identification of the isolated compounds, and evaluation of the hepatoprotective, anti-inflammatory and cytotoxic activities of the aqueous alcoholic and chloroform extracts. Isolation of the flavonoid constituents was performed using chromatographic techniques. Ten flavonoid compounds were isolated and identified as six flavone glycosides, two methylated flavones, and two flavone aglycons. The structures were established through chemical and spectral analysis. Paracetamol-induced hepatotoxicity, carrageenan-induced hind rat paw edema and sulforhodamine B (SRB) assay were used in the evaluation of hepatoprotective, anti-inflammatory and cytotoxic activities, respectively. The 70% methanol and chloroform extracts showed strong hepatoprotective and anti-inflammatory activity; no cytotoxic activity was observed at the chosen extract concentrations and they possess promising protective activity against paracetamol-induced hepatic damage and anti-inflammatory activity in rats. The flavonoids isolated from Leonotis leonurus in this study were found to be isolated for the first time from the genus Leonotis.

In-vitro anthelminthic activity of crude aqueous extracts of Aloe ferox, Leonotis leonurus and Elephantorrhiza elephantina against Haemonchus contortus

Aloe ferox (Mill), Leonotis leonurus (L) R. BR; and Elephantorrhiza elephantina (Burch.) Skeels are plants frequently used by resource-limited farmers in the Eastern Cape Province to control gastrointestinal parasites in goats. A study was conducted to validate their anthelminthic activities in-vitro on the egg and larvae of the nematode parasite Haemonchus contortus. The crude aqueous extracts of leaves of A. ferox and L. leonurus; and roots of E. elephantina were used. Eggs and larvae of the parasite were incubated at 25 degrees C in aqueous extracts at concentrations of 0.625-20 mg/ml for 48 h and 7 days for the egg hatch and larval development assays respectively. Albendazole and water were the positive and negative controls respectively. Inhibition of egg hatching and larval development increased significantly (P < 0.05) with increasing concentrations of the extracts. E. elephantina and L. leonurus extracts had 100% egg hatch inhibition at concentration as low as 2.5 mg/ml and 1.25 mg/ml respectively, whereas A. ferox extracts had 100% inhibition at concentrations of 20 mg/ml. At the lowest concentration tested (0.625 mg/ml), E. elephantina inhibited egg hatching >96% and this was comparable to albendazole at the same concentration. E. elephantina and L. leonurus also totally inhibited larval development at concentrations of 1.25 mg/ml. The study provided evidence that A. ferox, E. elephantina and L. leonurus extracts possess anthelminthic activity, thus justifying their use in the treatment of GI helminthosis. There is however need to assess the safety of these plants in vivo and also to undertake in vivo efficacy studies.

Two new isolated epimers seem to contribute to the bitter principle of Leonurus japonicus Houtt.

The aerial parts of Chinese motherwort (Leonurus japonicus Houtt) (Yimucao) are commonly used in traditional Chinese medicine (TCM) to regulate menses and to treat associated conditions. As the herb is more and more used in Europe, it has been started to cultivate the plant in Germany [1]. Since bitterness is an important sensory feature of the plant, the aim of the investigation was to isolate and identify the chemical constituents responsible for the bitter taste of Yimucao. It was found that the bitter principle can be extracted by n-hexane. Therefore, the n-hexane extract of Herba Leonuri has been fractionated using Fast Centrifugal Partition Chromatography (FCPC).This led to a fraction containing a mixture of two compounds which seemed to be responsible for the bitter taste of Yimucao. Structure elucidation by MS and NMR spectroscopy led to two new epimeric diterpenoid compounds 1 and 2 (exact mass 392,2), which are related to furanic labdane type lactones previously found in Leonurus japonicus, Leonurus cardiaca, Leonotis leonurus and Marrubium vulgare [2,3].

In vitro anti-HIV activity of five selected South African medicinal plant extracts

Aim of the study Five South African medicinal plants, Bulbine alooides (L.) Willd. (Asphodelaceae), Crinum macowani Baker (Amaryllidaceae), Hypoxis sobolifera var. sobolifera (Jacq.) Nel (Hypoxidaceae), Leonotis leonurus (L.) R.Br. (Lamiaceae) and Tulbaghia violacea Harv (Liliaceae) used for the treatment of various ailments, including infectious diseases, were screened for activity against human immunodeficiency virus (HIV). Materials and methods Aqueous and ethanol extracts were tested for inhibitory activity in HIV-1 infected CEM.NK R-CCR5 cells, and against HIV-1 reverse transcriptase (RT) and HIV-1 protease (PR). Results In CEM.NK R-CCR5 cells, ethanol extracts of Leonotis leonurus inhibited HIV-1 significantly (33% reduction in HIV-1 p24, P < 0.05). HIV-1 RT inhibition (≥50%) was shown for extracts of Bulbine alooides (aqueous and ethanol), Hypoxis sobolifera (aqueous and ethanol) and Leonotis leonurus (aqueous), but inhibitory activity was lost upon dereplication for removal of non-specific tannins/polysaccharides. HIV-1 PR inhibition was observed for extracts of Hypoxis sobolifera (aqueous), Bulbine alooides (aqueous and ethanol) and Leonotis leonurus (ethanol). Only ethanolic extracts of Bulbine alooides and Leonotis leonurus retained HIV-1 PR inhibition after dereplication with IC 50 of 94 μg/ml and 120 μg/ml, respectively. Conclusion The dereplicated ethanolic extracts of Leonotis leonurus and Bulbine alooides showed the greatest anti-HIV potential in this study through inhibition of HIV-1 PR.

Constituents of Leonotis leonurus flowering tops

Phytochemical investigation of flowering tops of Leonotis leonurus, yielded a new diterpene ester, 1,2,3-trihydroxy-3,7,11,15-tetramethylhexadecan-1-yl-palmitate along with five known metabolites. The structures of all compounds were determined by spectroscopic methods including 1D- and 2D NMR spectroscopy. All the isolated compounds were evaluated for antimalarial, cytotoxicity and for antimicrobial activities. Antimalarial activity for luteolin 7- O-β- d-glucopyranoside ( 4) (IC 50 = 2.2 μg/mL for the D6 clone and 1.8 μg/mL for the W2 clone) was observed. Chloroquine and artemisinin were used as positive controls which showed IC 50 of 0.016 and 0.0048 μg/mL for the D6 clone, respectively, and IC 50 of 0.14 and 0.0047 μg/mL for the W2 clone, respectively. None of the compounds were cytotoxic to Vero cells up to a concentration of 4.76 μg/mL.

Safety evaluation of the aqueous extract of Leonotis leonurus shoots in rats

The aqueous extract from Leonotis leonurus (L) R.Br. (Lamiaceae) shoots was evaluated in female rats for its acute, sub acute, and chronic toxicity together with hematological, biochemical, and histopathological changes. In the acute toxicity test, the extract caused death in animals receiving 3200 mg/kg dose. The extract also caused significant (P < 0.05) changes in red blood cells, packed cell volume, hemoglobin concentration, mean corpuscular volume, platelets, white blood cells and its differentials at doses of 1600 mg/kg in sub-acute toxicity and in as low as 200 mg/kg in chronic toxicity. In biochemical parameters, the extract caused a significant (P < 0.05) decrease in the levels of urea and creatinine at 1600 mg/kg dose and a significant (P < 0.05) reduction in urea, total bilirubin, total protein, albumin, globulin, glutamine transference gamma-glutamyl transferase (GGT), and alanine transminase in the 400 mg/kg dose in chronic toxicity. Changes were also noted in body weights, but no significant changes were observed in the levels of electrolytes (sodium, potassium, and chloride). Clinico-pathologically, starry hair coat, respiratory distress, and mortality were recorded. The extract also caused various histopathological changes in the organs. The study concluded that farmers need to exercise caution in the use of the plant for medicinal purposes.

Review on plants with CNS-effects used in traditional South African medicine against mental diseases

The majority of the population in South Africa use traditional health care to treat various mental conditions. In this review, we present ethnobotanical information on plants used by the traditional healers in South Africa to treat mental illnesses, specifically epilepsy, depression, age-related dementia and debilitative mental disorders. Details of the recent scientific studies conducted on some of these plants are reviewed. Extracts of Searsia chirindensis, Cotelydon orbiculata and Leonotis leonurus have shown in vivo anticonvulsant activity. Extracts from Searsia dentata and Searsia pyroides showed spontaneous epileptiform discharge in mouse cortical slices, and acted as NMDA-receptor antagonists. Apigenin, amentoflavone and agathisflavone with affinity to the benzodiazepine site on the GABA A-receptor were isolated from Searsia pyroides. Naringenin with affinity to the GABA A-benzodiazepine receptor was isolated from Mentha aquatica. Agapanthus campanulatus, Boophone disticha, Mondia whitei and Xysmalobium undulatum exhibited antidepressant-like activity in three in vivo models for depression. Amaryllidaceae alkaloids with activity to the serotonin transporter were isolated from Boophone disticha. The alkaloid mesembrine, which act as a serotonin reuptake inhibitor, was isolated from Sceletium tortuosum. Investigations of plants used to treat age-related dementia and debilitative mental disorders lead to the isolation of a number of Amaryllidaceae alkaloids with acetylcholinesterase inhibitory activity from Boophone disticha and Crinum species. Extracts of Mentha aquatica, Gasteria croucheri, Ruta graveolens and Scotia brachypetala inhibited MAO-B. Naringenin was isolated from Mentha aquatica as a MAO inhibitor. Only a small number of the more than 300 southern African plant species reported to treat or affect the CNS have been scientifically evaluated. Very few of the active compounds have been isolated and identified.

Antithrombotic/anticoagulant and anticancer activities of selected medicinal plants from South Africa

Nine plants available in the Eastern Cape Province of South Africa were tested for antithrombotic and/or anticoagulant activity. Organic (methanol) and aqueous (distilled water) extractions were performed on the various plant parts. The thrombin assay and clotting time assays (thrombin-induced and CaCl2-induced) were utilised. Several extracts displayed activity, but in most cases this was due to the presence of tannins. Only the aqueous extracts displayed activity after tannin removal. The Sutherlandia frutescens leaf extract displayed antithrombotic activity, with an IC50 value of 2.17 mg/ml. Gloriosa superba and Zantedeschia aethiopica leaf extracts displayed anticoagulant properties by inhibiting thrombin-induced clotting, with IC50 values of 2.97 and 3.05 mg/ml, respectively. The Leonotis leonurus root extract was found to decrease the CaCl2-induced clotting time by 50% at 8.88 mg/ml. A decrease in this value accompanied by a decrease in fibrin formation was preferable for the CaCl2- induced assay, since decreased fibrin formation may have a role in the prevention of cancer metastasis. As tannins were found to contribute minimally to the anticoagulant effect of L. leonurus, the cytotoxicity potential of the extracts of this species against five cell lines was determined. Only the organic extract yielded significant cytotoxity.

Constituents of Leonotis leonurus Flowering Tops

Leonotis leonurus L., also known as Lion's Tail or Wild Dagga, is a member of the Mint family (Lamiaceae). The plant is reported to have anticonvulsant [1], antinociceptive, anti-inflammatory and hypoglycemic activities [2]. Several labdane diterpenoids were reported in the leaves and aerial parts. However, no work has been reported on the flowers of this plant. A phytochemical study of the flowering tops of L. leonurus yielded a new diterpene ester 1,2,3-trihydroxy-3,7,11,15-tetramethylhexadecan-1-palmitate (1) along with providing new source for five known compounds identified as succinic acid (2), uracil (3), luteolin 7-O-glucoside (4), acteoside (5), and geniposidic acid (6). The structures of 1–6 were determined by spectroscopic methods including 1D- and 2D-NMR, IR, UV, MS etc. All six compounds were evaluated for their antimalarial and cytotoxic activities. Antimalarial activity was observed only for compound 4 (IC50 s = 2.2 µg/mL for D6 clone, and 2.6 µg/mL for W2 clone) [3]. Cytotoxicity was not observed for any of these compounds up to a concentration of 4.76 µg/mL. Acknowledgements: This work was supported in part by the United States Department of Agriculture, Agricultural Research Service, Specific Cooperative Agreement No 58-6408-2-0009 and Grant Number P20RR021929 from the National Center For Research Resources. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Center for Research Resources or the National Institutes of Health.

Plant compounds insecticide activity against Coleoptera pests of stored products

The objective of this work was to screen plants with insecticide activity, in order to isolate, identify and assess the bioactivity of insecticide compounds present in these plants, against Coleoptera pests of stored products: Oryzaephilus surinamensis L. (Silvanidae), Rhyzopertha dominica F. (Bostrichidae) and Sitophilus zeamais Mots. (Curculionidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetifolia (L.) R.Br.), jimson weed (Datura stramonium L.), baleeira herb (Cordia verbenacea L.), mint (Mentha piperita L.), wild balsam apple (Mormodica charantia L.), and billy goat weed or mentrasto (Ageratum conyzoides L.). The insecticide activity of hexane and ethanol extracts from those plants on R. dominica was evaluated. Among them, only hexane extract of A. conyzoides showed insecticide activity; the hexane extract of this species was successively fractionated by silica gel column chromatography, for isolation and purification of the active compounds. Compounds 5,6,7,8,3',4',5'-heptamethoxyflavone; 5,6,7,8,3'-pentamethoxy-4',5'-methilenedioxyflavone and coumarin were identified. However, only coumarin showed insecticide activity against three insect pests (LD50 from 2.72 to 39.71 mg g-1 a.i.). The increasing order of insects susceptibility to coumarin was R. dominica, S. zeamais and O. surinamensis.

Compounds from Ageratum conyzoides: isolation, structural elucidation and insecticidal activity

This work aimed at identifying plant compounds with insecticidal activity against Diaphania hyalinata (L.) (Lepidoptera: Pyralidae), Musca domestica (L.) (Diptera: Muscidae), Periplaneta americana (L.) (Blattodea: Blattidae) and Rhyzopertha dominica (F.) (Coleoptera: Bostrichidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetaefolia L.), Jimson weed (Datura stramonium L.), 'baleeira' herb (Cordia verbenaceae L.), mint (Mentha piperita L.), wild balsam apple (Mormodica charantia L.) and billy goat weed (Ageratum conyzoides L.). Firstly, the insecticidal activities of hexane and ethanol plant extracts were evaluated against adults of R. dominica. Among them, only the hexane extract of A. conyzoides showed insecticidal activity. The hexane extract of this plant species was therefore fractionated by silica gel column chromatography to isolate and purify its bioactive chemical constituents. Three compounds were identified using IR spectra, (1)H NMR, (13)C NMR, HMBC and NOE after gel chromatography: 5,6,7,8,3', 4', 5'-heptamethoxyflavone, 5,6,7,8,3'-pentamethoxy-4', 5'-methylenedioxyflavone and coumarin. The complete assignment of (13)C NMR to 5,6,7,8,3'-pentamethoxy-4', 5'-methylenedioxyflavone was successfully made for the first time. 5,6,7,8,3'-Pentamethoxy-4', 5'-methylenedioxyflavone did not show any insecticidal activity against the four insect species tested. 5,6,7,8,3', 4', 5'-Heptamethoxyflavone showed low activity against D. hyalinata and R. dominica and was not toxic to M. domestica or P. americana. In contrast, coumarin showed insecticidal activity against all four insect pest species tested, with the following order of susceptibility: R. dominica < P. americana < D. hyalinata < M. domestica after 24 h exposure.