Repellent efficacy of essential oils and plant extracts against Tribolium castaneum and Plodia interpunctella

This study was conducted to investigate the repellent efficacy of essential oils (Origanum vulgare, Pimpinella anisum, and Tanacetum cinerariifolium) and four plant extracts (Agastache rugosa, Capsicum annuum, Citrus reticulata, and Ginkgo biloba) against Tribolium castaneum (adults and larvae) and Plodia interpunctella (larvae). Gas chromatography/mass spectrometry analysis revealed the presence of carvacrol, anethole, and jasmolin I as the predominant constituent in O. vulgare, P. anisum, and T. cinerariifolium, respectively. Furthermore, ethyl hexopyranoside, 9,12‐octadecadienoic acid, cyclopentanol, and 2‐cresol were identified in A. rugosa, C. annuum, C. reticulata, and G. biloba, respectively. The repellent efficacy of each essential oil, plant extract, and the combination of oils was evaluated using a specially designed cylinder trap for 120 h. Among the three oils, O. vulgare and T. cinerariifolium had greatest repellent efficacy against P. interpunctella larvae. T. cinerariifolium exhibited effective repellence against the adults and larvae of T. castaneum. Therefore, O. vulgare (O) and T. cinerariifolium (T) were selected for further investigation of combined effects. Two essential oils were mixed in three different ratios of OT1 (1:3), OT2 (1:1), and OT3 (3:1). The repellent efficacies of OT1 and OT2 against the adults of T. castaneum were significantly greater than that of OT3. OT1 was effective against the larvae of T. castaneum, whereas OT2 was effective against the larvae of P. interpunctella. OT1 enhanced the repellent efficacy by approximately five times against larvae of T. castaneum, compared with that of T. cinerariifolium. Overall, OT1 was selected as the best repellent substance against all the tested insects.     

Chemical Composition and Insecticidal Activity against Tribolium Castaneum of Thapsia garganica L. Seed Essential Oil

Due to the several side effects of synthetic pesticides, including environmental pollution, threats to human health, and the development of pest resistance to insecticides, the use of alternative healthy, available and efficient agents in pest management strategies is necessary. Recently, the use of essential oil obtained from aromatic plants has shown significant potential for insect pest management. For this reason, the essential oil isolated from seeds of Thapsia garganica L. was investigated for the first time for its chemical profile, and its toxicity and repellency effects against Tribolium castaneum adults. Qualitative and quantitative analyses of the chemical composition by gas chromatography coupled to mass spectrometry (GC/MS) revealed the presence of 18 organic volatiles representing 96.8 % of the total constituents. The main compounds were 1,4-dimethylazulene (51.3 %) followed by methyl palmitate (8.2 %), methyl linoleate (6.2 %) and costol (5.1 %). Concerning the repellent effect, results revealed that SEO (Seed Essential Oil) was very repellent towards T. castaneum adults, with 100 % repellency after 2 h of exposure. Furthermore, the essential oil exhibited remarkable contact toxicity against T. castaneum (93.3 % of mortality) at the concentration of 10 % (v/v). The median lethal dose (LD₅₀) of the topical application of the seed essential oil was 4.4 %. These encouraging outcomes suggested that the essential oil from T. garganica seeds could be considered a potent natural alternative to residual persistent and toxic insecticides.     

Insecticidal and Repellent Activity of Thymus quinquecostatus Celak. Essential Oil and Major Compositions against Three Stored-Product Insects

Thymus quinquecostatus Celak. of the Lamiaceae family has a long history of dual use of medicine and food with high economic value, and has been proved to have good antioxidative, antimicrobial, and antidiabetic activities. Essential oil (EO) extracted from the aerial part of T. quinquecostatus was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC/MS) and GC. Totally 45 compounds were identified accounting for 98.5 % of the EO. The major constituents of the EO were linalool (52.003 %), borneol (10.911 %) and anethole (5.325 %). Fumigant, contact and repellent activity of T. quinquecostatus essential oil (EO) against Tribolium castaneum (Coleoptera: Tenebrionidae), Lasioderma Serricorne (Coleoptera: Anobiidae), Liposcelis bostrychophila (Psocoptera: Liposcelididae) were evaluated in this work. T. quinquecostatus EO and three major constituents showed varying degrees of insecticidal and repellent activities to three stored-product insects. Anethole stated the best fumigant and contact activity than others did to all three insect species. EO and compounds showed general repellent activity against three target insects. This work suggests that the EO of T. quinquecostatus has promising potential to be developed into botanical pesticides and repellents controlling pest damage in warehouses and grain stores.     

Chemical Composition,Toxicity and Repellency of Inula graveolens Essential Oils from Roots and Aerial Parts against Stored-Product Beetle Tribolium castaneum (Herbst)

In this work, essential oils extracted from roots and aerial parts of Inula graveolens by hydrodistillation and their fractions obtained by chromatographic simplification were first investigated for their chemical composition by GC/MS and then evaluated for the first time for their repellency and contact toxicity properties against Tribolium castaneumadults. Twenty-eight compounds were identified in roots essential oil (REO), which accounted for 97.9 % of the total oil composition, with modhephen-8-β-ol (24.7 %), cis-arteannuic alcohol (14.8 %), neryl isovalerate (10.6 %) and thymol isobutyrate (8.5 %) as major constituents. Twenty-two compounds were found in the essential oil from aerial parts (APEO), which accounted for 93.9 % of the total oil, with borneol (28.8 %), caryophylla-4(14),8(15)-dien-6-ol (11.5 %), caryophyllene oxide (10.9 %), τ-cadinol (10.5 %) and bornyl acetate (9.4 %) as main compounds.REO and APEO displayed stronger repellency after 2 h of exposure (80.0 and 90.0 %, respectively) against T. castaneum at the concentration of 0.12 μL/cm². After fractionation, fractions R₄ and R₅ exhibited greater effects (83.3 % and 93.3 %, respectively) than the roots essential oil. Furthermore, the fractions AP₂ and AP₃ showed higher repellency (93.3 and 96.6 %, respectively) than the aerial parts oil. The LD₅₀ values of oils from roots and aerial parts topically applied were 7.44 % and 4.88 %, respectively. Results from contact toxicity assay showed that fraction R₄ was more effective than the roots oil with LD₅₀ value of 6.65 %. These results suggests that essential oils of roots and aerial parts from I. graveolens may be explored as potential natural repellent and contact insecticides against T. castaneum in stored products.     

Evidence of Phytoalexins in Rhizome of Atractylodis Maceocephalae Koidz Infected with Sclerotium rolfsii sacc Following Treatment with the Polysaccharides of Chrysanthemum indicum

Atractylenolides compounds (atractylenolide‐I, atractylenolide‐II and atractylenolide‐III) extracted from Atractylenolides macrocephala were analysed for their differential presence in the rhizome of both the infected and healthy plants and its fungitoxicity on prophylactic treatment with polysaccharides of Chrysanthemum indicum against Sclerotium rolfsii. It was evident that the plant under stress by pathogen has instigated the significant synthesis and accumulation of atractylenolide‐II and atractylenolide‐III in the rhizome of plants as a result of elicitation with polysaccharides of C. indicum. Our results also showed that the absence of atractylenolide‐II in the rhizome made the plant susceptible to S. rolfsii. Furthermore, on in vitro antifungal studies, exogenous application of atractylenolide‐II with the concentration of 200 μg/ml showed a significant inhibitory effect on mycelial growth by achieving a 77.23% antifungal activity rate, and a minimal inhibitory effect at a concentration of 12.5 μg/ml with atractylenolide‐II. To our knowledge, this novel study on phytoalexins in A. macrocephala suggested that A. macrocephala plants produce elevated levels of atractylenolide‐II and atractylenolide‐III in a pattern typical of phytoalexins, in response to an eliciting treatment after infection.     

苍术素对大鼠心脏正性肌力的作用及其机制*

目的: 研究中药苍术的有效成分苍术素(Atractylodin)的正性肌力作用及其机理。方法: 随机选取6只雄性SD大鼠进行在体压力-容积环 (P-V loop)实验,加药前为Control组,经腹腔注射苍术素(3 mg/kg)后为苍术素组(自身对照),分析6只雄性大鼠加药后对大鼠左心室心输出量、容积及动脉压的作用;大鼠离体心脏灌流实验中,依次灌流给药:第一部分为Control→ 0.1→1→10 μmol/L苍术素浓度梯度灌流,第二部分为Control→200 nmol/L H89 (PKA抑制剂)→200 nmol/L H89+10 μmol/L 苍术素,第三部分为Control→500 nmol/L KN-93 (CaMKII抑制剂)→500 nmol/L KN-93+10 μmol/L 苍术素,第四部分为Control→10 nmol/L Calyculin A (PP1, PP2A抑制剂)→10 nmol/L Calyculin A+10 μmol/L 苍术素,加药前的正常空白组为Control组,分析每部分各6只雄性大鼠的组间左心室发展压的变化;在大鼠心肌细胞钙释放实验中,分组、给药的方法和浓度同离体心脏实验,分析来源于6个雄性大鼠6个左心室心肌细胞组间钙释放幅值的变化。结果: ①P-V loop实验表明:与Control组相比,苍术素组(3 mg/kg)腹腔注射30 min后,显著增加大鼠心输出量、搏出功及心率(P＜0.05),降低动脉舒张压(P＜0.05),而对收缩压无明显影响;②离体心脏实验表明:与Control组相比,苍术素组(0.1, 1, 10 μmol/L)灌流10 min后,能显著增加大鼠离体心脏左心室发展压(LVDP) (P＜0.05),其作用能被H89组(200 nmol/L)所阻断;③心肌细胞钙释放实验表明:与Control组相比,苍术素组(10 μmol/L)灌流10 min后,基于肌浆网钙泵(SERCA2a)显著增加大鼠心肌细胞钙释放幅值(P＜0.05),其作用能被H89组(200 nmol/L)所阻断。结论: 苍术素具有正性肌力作用,其血流动力学特点表现为降低在体大鼠动脉舒张压而不增加收缩压,苍术素的正性肌力作用机制是通过PKA-SERCA2a通路发挥的。     

Chemical Composition and Insecticidal Activity of Artemisia scoparia Essential Oil against Three Coleopteran Stored-Product Insects

Chemical composition of the essential oil from Artemisia scoparia Waldst et Kit, and its fumigant and repellent activity were investigated against three stored product insects, Callosobruchus maculatus (Fab.), Sitophilus oryzae (L.), and Tribolium castaneum (Herbst). Dry ground leaves were subjected to hydrodistillation using a modified clevenger-type apparatus and the chemical composition of the volatile oil was studied by GC-MS. Nineteen components (99.51% of the total composition) were identified. β-Pinene (19.01%), capillin (17.45%), limonene (15.11%), myrcene (10.95) were found to be the major constituents of the oil. The mortality of 1-7 day old adults of the insect pests increased with concentration from 37 to 926 μL per L air and with exposure time from 3 to 24 h. A concentration of 37 μL per L air and exposure time of 24 h was sufficient to obtain 100% kill of the insects. Callosobruchus maculatus was more susceptible than S. oryzae and T. castaneum. A second more detailed bioassay gave estimates for the LC₅₀ of C. maculatus as 1.46 μL per L air, S. oryzae 1.87 μL per L air and T. castaneum 2.05 μL per L air. Also, the essential oil was significantly more repellent to T. castaneum and S. oryzae than C. maculatus. However, half-life time of the oil for C. maculatus was longer than S. oryzae and T. castaneum. These results show the efficacy of A. scoparia oil for use in organic food protection.     

In vitro cytotoxic activity of extracts and isolated constituents of Salvia leriifolia Benth. against a panel of human cancer cell lines

In the course of recent efforts to identify new potential antiproliferative active principles, Salvia leriifolia extracts and isolated constituents were evaluated for their cytotoxic activity against a panel of human cancer cell lines, including renal adenocarcinoma (ACHN), amelanotic melanoma (C32), colorectal adenocarcinoma (Caco‐2), lung large cell carcinoma (COR‐L23), malignant melanoma (A375), lung carcinoma (A549), and hepatocellular carcinoma (Huh‐7D12) cells. The hexane and CH₂Cl₂ extracts showed the strongest cytotoxic activity against the C32 cell line with IC₅₀ values of 11.2 and 13.6 μg/ml, respectively, and the AcOEt extract was the most active extract against the COR‐L23 cell line (IC₅₀ of 20.9 μg/ml). Buchariol, a sesquiterpene obtained by biofractionation of the CH₂Cl₂ extract, exhibited a higher activity than the positive control vinblastine against the C32 and A549 cell lines (IC₅₀ values of 2.1 and 12.6 μM , resp.). Interesting results were also obtained for naringenin, a flavonoid isolated from the AcOEt extract, which exhibited a strong cytotoxic activity against the C32, LNCaP, and COR‐L23 cell lines (IC₅₀ values of 2.2, 7.7, and 33.4 μM , resp.), compared to vinblastine (IC₅₀ values of 3.3, 32.2, 50.0 μM , resp.). None of the tested compounds affected the proliferation of skin fibroblasts (142BR), suggesting a selective activity against tumor cells.     

Contact Toxicity and Repellency of the Essential Oil of Dictamnus dasycarpus Roots from China against Two Stored‐Product Insects

During our screening program for new agrochemicals from traditional medicinal herbs, Dictamnus dasycarpus was found to possess contact toxicity and repellent activity against the cigarette beetle Lasioderma serricorne and the booklouse Liposcelis bostrychophila. The essential oil obtained by hydrodistillation of D. dasycarpus roots was characterized by GC‐FID and GC/MS analyses, and the main components identified were syn‐7‐hydroxy‐7‐anisylnorbornene ( 1 , 49.9%), 1,3,4,5,6,7‐hexahydro‐2H‐inden‐2‐one ( 2 , 11.6%), 5,6‐diethenyl‐1‐methylcyclohexene ( 3 , 7.4%), and 3,9‐dimethyltricyclo[4.2.1.1^2,5]dec‐3‐en‐9‐ol ( 4 , 6.35%). The D. dasycarpus root oil exhibited strong contact toxicity against L. serricorne adults and L. bostrychophila, with LD₅₀ values of 12.4 μg/adult and 27.2 μg/cm², respectively. Moreover, the essential oil also showed strong repellency against both stored‐product insects tested.     

The antagonistic/synergistic effects of some medicinal plant essential oils,extracts and powders combined with Diatomaceous earth on red flour beetle,Tribolium castaneum Herbst (Coleoptera: Tenebrionidae)

Abstract

Red flour beetle, Tribolium castaneum Herbst (Coleoptera: Tenebrionidae) is a prominent pest of stored products particularly cereal flour. Since resistance of this pest to common chemical insecticides is well documented, we were examined the synergistic/antagonistic interaction between Satureja hortensis L., Trachyspermum ammi L., Ziziphora tenuior L., Cuminum cyminum L. and Foeniculum vulgare Miller essential oils, ethanolic extracts and powders with Diatomaceous earth (DE) against T. castaneum adults under laboratory conditions at 27 ± 1 °C, 65 ± 5% RH and continuous darkness. We assayed repellency of ethanolic extracts and essential oils of mentioned plants on the pest. Results showed that DE had high toxicity to the pest. Plant essential oils and ethanolic extracts (except ziziphora) synergized the performance of DE. Nevertheless, plant powders elicited antagonistic effects (except ziziphora that exhibited synergistic effect). The most repellent EO and extract was cumin which exhibited mean repellency value on adult insect equivalent to 92.58 and 51.47%, respectively.     

Chemical Constituents and Activities of the Essential Oil from Myristica fragrans against Cigarette Beetle Lasioderma serricorne

Essential oil extracted from nutmeg seeds (Myristica fragrans Houtt .) by hydrodistillation was subjected to GC/MS and GC analysis. A total of 27 constituents were identified, of which eugenol (19.9%), methylisoeugenol (16.8%), methyleugenol (16.7%), sabinene (11.8%), and terpinen‐4‐ol (8.5%) were the major components. The essential oil was tested against Lasioderma serricorne for insecticidal and repellent activity, the LD₅₀ value at the end of 24 h exposure period was 19.3 μg/adult. Six active compounds were isolated by bioassay‐guided fractionation. They were identified as eugenol ( 1 ), methyleugenol ( 2 ), methylisoeugenol ( 3 ), elemicin ( 4 ), myristicin ( 5 ), and safrole ( 6 ). Among these isolates, 4 showed the strongest contact toxicity against L. serricorne adults with an LD₅₀ value of 9.8 μg/adult. Repellency of crude oil and active compounds were also determined. Compounds 1, 2, 4 , and 5 were strongly repellent against the cigarette beetle and exhibited the same level of repellency compared with the positive control, DEET. The results indicate that the essential oil of M. fragrans and its active constituents have potential for development as natural insecticides and repellents to control L. serricorne.     

Contact and fumigant toxicities of calamusenone isolated from Acorus gramineus rhizome against adults of Sitophilus zeamais and Rhizopertha dominica

Abstract Calamusenone [3,8‐dimethyl‐5‐(1‐methylethylidene)‐1,2,3,4,5,6,7,8‐octahydroazulene‐6‐one, C₁₅H₂₂O] from Acorus gramineus Soland rhizome was tested in the laboratory for its insecticidal activities against adults of Sitophilus zeamais Motsch. and Rhizopertha dominica (Fab.), using dry film contact and fumigation methods. Responses varied with insect species, dosage and exposure time. In the dry film contact experiment, the highest insecticidal effects of calamusenone against S. zeamais and R. dominica adults were produced at 170.32 μg/cm² after treatment for 72 h, with 96.2% and 98.7% mortalities, respectively. The median lethal concentration (LC₅₀) (72 h) values of calamusenone against S. zeamais and R. dominica adults were 67.00 μg/cm² and 77.30 μg/cm², respectively. As a potential fumigant, calamusenone showed moderate insecticidal effect on the adults of S. zeamais and R. dominica in fumigation experiment, with their LC₅₀ (120 h) values of 125.71 μL/L and 93.64 μL/L respectively. Calamusenone isolated from A. gramineus rhizome showed promise as a novel pesticide candidate for stored‐product pest control.     

Fumigant toxicity of Laurus nobilis and Myrtus communis essential oils on larvae and adults of the Red flour beetle,Tribolium castaneum Herbst (Col.: Tenebrionidae)

Considering the invasion to food commodities by insects and harmful effect of chemical pesticides, essential oils are among the best known substances tested against stored product pests. These compounds may act as fumigants, contact insecticides, repellents or anti-feedants. In present study, fumigant toxicity of essential oils from Laurus nobilis L. and Myrtus communis L. was assessed on larvae and adults of Tribolium castaneum Herbst at 27?±?2?°C, 60?±?5% RH in darkness. Each essential oil was tested in five concentrations with three replicates. The LC₅₀ values of L. nobilis and M. communis against adults of beetle were calculated 243.78 and 56.11?μl/l and LC₉₅ values for them were 685.85 and 144.01?μl/l, respectively. For the larvae of T. castaneum, the LC₅₀ values for L. nobilis and M. communis were 211.64 and 69.63 and LC₉₅ values were 656.84 and 183.65?μl/l, respectively. Results showed that these essential oils may have potential as botanical control agents against larvae and adults of T. castaneum.     

Antimicrobial and Cytotoxic Activity of Extracts of Ferula heuffelii Griseb. ex Heuff. and Its Metabolites

The antimicrobial and cytotoxic activities of isolates (CHCl₃ and MeOH extracts and selected metabolites) obtained from the underground parts of the Balkan endemic plant Ferula heuffelii Griseb . ex Heuff . were assessed. The CHCl₃ and MeOH extracts exhibited moderate antimicrobial activity, being more pronounced against Gram‐positive than Gram‐negative bacteria, especially against Staphylococcus aureus (MIC=12.5 μg/ml for both extracts) and Micrococcus luteus (MIC=50 and 12.5 μg/ml, resp.). Among the tested metabolites, (6E)‐1‐(2,4‐dihydroxyphenyl)‐3,7,11‐trimethyl‐3‐vinyldodeca‐6,10‐dien‐1‐one ( 2 ) and (2S*,3R*)‐2‐[(3E)‐4,8‐dimethylnona‐3,7‐dien‐1‐yl]‐2,3‐dihydro‐7‐hydroxy‐2,3‐dimethylfuro[3,2‐c]coumarin ( 4 ) demonstrated the best antimicrobial activity. Compounds 2 and 4 both strongly inhibited the growth of M. luteus (MIC=11.2 and 5.2 μM , resp.) and Staphylococcus epidermidis (MIC=22.5 and 10.5 μM , resp.) and compound 2 additionally also the growth of Bacillus subtilis (MIC=11.2 μM ). The cytotoxic activity of the isolates was tested against three human cancer cell lines, viz., cervical adenocarcinoma (HeLa), chronic myelogenous leukemia (K562), and breast cancer (MCF‐7) cells. The CHCl₃ extract exhibited strong cytotoxic activity against all cell lines (IC₅₀<11.0 μg/ml). All compounds strongly inhibited the growth of the K562 and HeLa cell lines. Compound 4 exhibited also a strong activity against the MCF‐7 cell line, comparable to that of cisplatin (IC₅₀=22.32±1.32 vs. 18.67±0.75μM ).     

Toxic and repellent properties of Xylopia aethiopica (Dunal) A. Richard on Tribolium castaneum Herbst infesting stored millets,Pennisetum glaucum (L.) R. Br.

The toxicity and repellency of Xylopia aethiopica seed extract was investigated in the laboratory against Tribolium castaneum Herbst. Concentration and days after treatment (DAT) caused a significant increase in T. castaneum adult mortality with an interaction effect of both on mortality when filter paper was impregnated with X. aethiopica extract. At 0.2 ml/60 cm² extract, significant mortality was observed at three–seven DAT when compared with one DAT. At 0.4 ml/60cm², 100% mortality was recorded at the lowest exposure period of one DAT. When 0.2 ml extract was applied to 5 g millet seeds, mortality at five–seven DAT was significantly higher than mortality observed in the control. Although repellency was dose-dependent, the percentage of T. castaneum that were repelled from treated filter paper was not significant. At 0.4 ml/60 cm², Class II repellency (26.7%) was observed. The results suggest that X. aethiopica can only effectively control T. castaneum populations that have infested millet but do not prevent cross-infestation via repellency.     

Norlathyrane Diterpenes from the Root of Euphorbia kansuensis

Phytochemical investigation of the EtOH extract obtained from the root of the Euphorbia kansuensis Proch . grown in China resulted in the isolation of two novel norlathyrane diterpenes, named ekanpenoids A and B ( 1 and 2 , resp.). Their structures were established by extensive 1D‐ and 2D‐NMR spectroscopy, as well as other spectra. The isolated diterpenes exhibited potent cytotoxic activities against the HeLa and Hep‐G2 cell lines with the IC₅₀ values ranging from 3.6 to 9.7 μg/ml.     

Essential oils of medicinal plants from the central andes of Argentina: chemical composition, and antifungal, antibacterial, and insect-repellent activities

The antifungal, antibacterial, and insect‐repellent activities of the essential oils (EOs) of Acantholippia seriphioides, Artemisia mendozana, Gymnophyton polycephalum, Satureja parvifolia, Tagetes mendocina, and Lippia integrifolia, collected in the Central Andes area, province of San Juan, Argentina, were investigated. The dermatophytes Microsporum gypseum, Trichophyton mentagrophytes, and T. rubrum were inhibited by the EOs of G. polycephalum, L. integrifolia, and S. parvifolia, with minimum inhibitory concentrations (MICs) between 31.2 and 1000 μg/ml. Moreover, all EOs presented moderate activity against the bacteria tested, and the L. integrifolia and G. polycephalum EOs showed excellent repellent properties against Triatoma infestans, the Chagas disease vector, with repellency values between 60 and 100%. The A. seriphioides, G. polycephalum, and L. integrifolia EOs, obtained by hydrodistillation, were characterized by GC‐FID and GC/MS analyses. The highest number of components (40) was identified in L. integrifolia EO, which, along with that of A. seriphioides, contained important amounts of oxygenated monoterpenes (44.35 and 29.72%, resp.). Thymol (27.61%) and carvacrol (13.24%) were the main components of A. seriphioides EO, and borneol, lippifoli‐1(6)‐en‐5‐one, and terpinen‐4‐ol (>8.5%) were the principal compounds of L. integrifolia EO. These results support the idea that oxygenated monoterpenes are the bioactive fractions of the EOs. Finally, the study shows that these Andean species might be used to treat superficial fungal infections and to improve the local Chagas disease situation by vector‐control.     

Three New Phenylpropanoids from the Roots of Piper taiwanense and Their Inhibitory Activities on Platelet Aggregation and Mycobacterium tuberculosis

Bioassay‐guided fractionation of the active AcOEt‐soluble fraction from the roots of Piper taiwanense has led to the isolation of two new phenylpropanoids, taiwanensols A and B ( 1 and 2 , resp.), a new natural product, taiwanensol C ( 3 ), and 3‐acetoxy‐4‐hydroxy‐1‐allylbenzene ( 4 ). The compounds were obtained as two isomer mixtures ( 1 / 2 and 3 / 4 , resp.). Their structures were elucidated by spectroscopic analyses, including 1D‐ and 2D‐NMR spectroscopy and mass spectrometry, and by the comparison of their NMR data with those of related compounds. Compounds 1 – 4 were evaluated for their antiplatelet and antitubercular activities. The mixtures 1 / 2 and 3 / 4 showed potent inhibitory activities against platelet aggregation induced by collagen, with IC₅₀ values of 35.2 and 8.8 μM , respectively. In addition, 1 / 2 and 3 / 4 showed antitubercular activities against Mycobacterium tuberculosis H37Rv, with MIC values of 30.0 and 48.0 μg/ml, respectively.     

Melanogenesis‐Inhibitory and Cytotoxic Activities of Chemical Constituents from the Leaves of Sauropus androgynus L. Merr. (Euphorbiaceae)

A new steroid, 20‐hydroxyisofucosterol (stigmasta‐5,24(28)‐diene‐3β,20β‐diol) ( 7 ), along with six known compounds 1 – 6 were isolated from the MeOH extract of the leaves of Sauropus androgynus L. Merr . (Euphorbiaceae). The structure of new steroid was determined by HR‐APCI‐MS and various NMR techniques in combination with literature data. Subsequently, their anti‐inflammatory, cytotoxic activities against five human cell lines, as well as inhibitory activities against the α‐MSH induced melanogenesis on the B16 cell line were evaluated. As the results, steroid compounds, 6 and 7 exhibited moderate cytotoxic to HL60, AZ521, SKBR3, and A549 tumor cell lines (IC₅₀ 26.9 – 45.1 μm ) with high tumor selectivity for A549 relative to WI38 cell lines (SI 2.6 and 3.0, resp.). And, flavonoid compounds, 4 and 5 exhibited superior inhibitory activities against melanogenesis (67.0 – 94.7% melanin content), even with no or low toxicity to the cells (90.1 – 99.6% cell viability) at the concentrations from 10 to 100 μm . Furthermore, Western blot analysis suggested that compound 5 could inhibit melanogenesis by suppressing the protein expressions of MITF, TRP‐1, TRP‐2, and tyrosinase.     

Aerosol distribution and efficacy in a commercial food warehouse

A series of field trials were conducted in a commercial food storage facility to evaluate exposure of stored‐product insects to aerosol formulations of synergized pyrethrins and the insect growth regulator methoprene. When adults of Tribolium castaneum (Herbst), the red flour beetle, and Tribolium confusum (Jacqueline DuVal), the confused flour beetle were exposed with and without a food source to synergized pyrethrin aerosol, there was no difference in adult mortality with respect to availability of food at either 7 or 14 days after exposure (P≥ 0.05). However, mortality was lower in T. confusum (40.4% and 79.3% with flour at 7 and 14 days, 38.9% and 84.8% without flour at 7 and 14 days) compared to T. castaneum (96.5% and 99.8% with flour at 7 and 14 days, 91.0% and 98.7% without flour at 7 and 14 days). Few late‐stage larvae and pupae of either species exposed to the pyrethrin aerosol emerged as adults. In tests with methoprene aerosol, adult emergence of exposed 3‐and 4‐week‐old larvae of T. confusum was less than 2%. Only 0.3% of 4‐week‐old larvae of T. castaneum exposed in open and obstructed areas emerged as adults. Emergence of adults from eggs of Plodia interpunctella (Hübner), the Indianmeal moth, embedded in culture media and exposed to the methoprene aerosol was 13.2%± 3.5%. Results show that the aerosols evaluated in our study could give effective control of some of the major stored‐product insect pests in commercial food storage facilities, and may offer an alternative to fumigation.