Synthesis and Antiarrhythmic, Anticoagulant, Anthelmintic, and Larvicidal Activities of 4-(2-Alkoxyethyl)-2,2-Dimethyl-1,2-Dihydrobenzo[F] Isoquinoline Hydrochlorides

BackgroundHighlighting affordable alternative crops that are rich in bioactive phytoconstituents is essential for advancing nutrition and ensuring food security. Amaranthus blitum L. (AB) stands out as one such crop with a traditional history of being used to treat intestinal disorders, roundworm infections, and hemorrhage. This study aimed to evaluate the anthelmintic and hematologic activities across various extracts of AB and investigate the phytoconstituents responsible for these activities.MethodsIn vitro anthelmintic activity against Trichinella spiralis was evaluated in terms of larval viability reduction. The anti-platelet activities were assessed based on the inhibitory effect against induced platelet aggregation. Further, effects on the extrinsic pathway, the intrinsic pathway, and the ultimate common stage of blood coagulation, were monitored through measuring blood coagulation parameters: prothrombin time (PT), activated partial thromboplastin time (aPTT), and thrombin time (TT), respectively. The structures of isolated compounds were elucidated by spectroscopic analysis.ResultsInterestingly, a previously undescribed compound (19), N-(cis-p-coumaroyl)-ʟ-tryptophan, was isolated and identified along with 21 known compounds. Significant in vitro larvicidal activities were demonstrated by the investigated AB extracts at 1 mg/mL. Among tested compounds, compound 18 (rutin) displayed the highest larvicidal activity. Moreover, compounds 19 and 20 (N-(trans-p-coumaroyl)-ʟ-tryptophan) induced complete larval death within 48 h. The crude extract exhibited the minimal platelet aggregation of 43.42 ± 11.69%, compared with 76.22 ± 14.34% in the control plasma. Additionally, the crude extract and two compounds 19 and 20 significantly inhibited the extrinsic coagulation pathway.ConclusionsThese findings extend awareness about the nutritional value of AB as a food, with thrombosis-preventing capabilities and introducing a promising source for new anthelmintic and anticoagulant agents.

Anthelmintic, antimycobacterial, antifungal, larvicidal and cytotoxic activities of acetone leaf extracts, fractions and isolated compounds from Ptaeroxylon obliquum (Rutaceae)

This study’s primary objectives were to evaluate phytochemical screening and identify therapeutic uses for the herb Simarouba glauca. By employing a Soxhlet apparatus, the leaves were extracted using ethyl acetate. Standard techniques were used for preliminary phytochemical analysis to screen the presence of secondary metabolites. The agar plate method was used to test for antimicrobial activity against Escherichia coli and Bacillus subtilis. The antidiabetic activity aimed to identify the alpha-amylase enzyme inhibition that is most effective at regulating blood glucose levels. The DPPH assay was used to screen the antioxidant activity. The extract’s bioactive components were purified using column and thin-layer chromatography. Simarouba glauca extract was tested for its cytotoxic property on the lung cancer cell line (A549) using the MTT assay. To find the phytocompounds present in the extract, GC-MS analysis was carried out. Anticoagulation activity was carried out to assess the prothrombin time of blood and therapeutic applications such as anthelminthic activity were determined by determining the time of death of parasites like earthworms. The tested extract showed considerable cytotoxic, antibacterial, antioxidant, anthelmintic, and anticoagulant activity.

Phytochemical screening of Calicotome villosa ethanolic extracts in respect of phenolic compounds (HPLC method), antioxidant activity (DPPH and β-carotene tests), determination of total phenolic and total flavonoid contents, and evaluation of cytotoxic (against Artemia salina), larvicidal (against Culex pipiens and Musca domestica) and anthelmintic activity (against Tubifex tubifex) have been performed. The flower extract exhibited higher biological activity than the stem extracts in all assays (DPPH, 0.6 mg/mL, IC50, β-carotene, 75.12 ± 0.73 %). There was good correlation between the antioxidant activity and total phenolic and total flavonoid contents. The flower extract exhibited significant cytotoxic activity (against A. salina) with 0.312 mg/mL, LC50 larvicidal activity (against Cx. pipiens) with 0.330 mg/mL, LC50 and anthelmintic activity (against T. tubifex) with 1.32 mg/mL, LC50 . HPLC analysis showed that vanillic acid was major component in the flower extract. In conclusion, C. villosa has good biological activity for further studies in agriculture, medicine and pesticide industry.

Marine pharmacology in 2005–6: Marine compounds with anthelmintic, antibacterial, anticoagulant, antifungal, anti-inflammatory, antimalarial, antiprotozoal, antituberculosis, and antiviral activities; affecting the cardiovascular, immune and nervous systems, and other miscellaneous mechanisms of action

Marine pharmacology in 1999: compounds with antibacterial, anticoagulant, antifungal, anthelmintic, anti-inflammatory, antiplatelet, antiprotozoal and antiviral activities affecting the cardiovascular, endocrine, immune and nervous systems, and other miscellaneous mechanisms of action

Marine pharmacology in 2001–2002: Marine compounds with anthelmintic, antibacterial, anticoagulant, antidiabetic, antifungal, anti-inflammatory, antimalarial, antiplatelet, antiprotozoal, antituberculosis, and antiviral activities; affecting the cardiovascular, immune and nervous systems and other miscellaneous mechanisms of action

The present study was conducted to evaluate the stem bark and leaf of Sterculia diversifolia for larvicidal, leishmanicidal, insecticidal and anthelmintic activities. In the larvicidal activity, dichloromethane and ethyl acetate fractions of both stem bark and leaf showed significant results, while the ethyl acetate fraction showed mild activity (IC50: 70.09 ± 0.09 μg/mL; 71.25 ± 0.01 μg/mL). In the insecticidal activity of the stem bark, n-hexane fraction showed mild activity (20-40% mortality) against all three subjects, while the insecticidal activity of leaf, methanolic extract and n-hexane fractions showed moderate activity (60% mortality) against Rhyzopertha dominica and Callosobruchus analis. In the anthelmintic activity of stem bark and leaf, ethyl acetate fraction exhibited activity in a dose-dependent manner giving time of paralysis and death shorter followed by dichloromethane fraction with 200 mg/mL concentration. Hence, it is clear that S. diversifolia stem bark and leaf possess larvicidal, leishmanicidal, insecticidal and anthelmintic agents. Video Clip of Methodology: Anthelmintic Activity: 5 min 29 sec: Click to watch

Background: Cow urine is believed to have therapeutic value and used in many drug formulations. It has been used along with herbs to treat various ailments by traditional healers. Aim: The present study was aimed to evaluate and compare the antimicrobial, larvicidal, and anthelmintic activity of Zingiber officinale Rose. (ZO) with cow urine extracts. Materials and Methods: The antimicrobial activity was performed using five microbial strains, namely, Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Aspergillus niger, and Aspergillus flavus; larvicidal activity was evaluated using 3rd and 4th instar stage larvae; and anthelmintic activity using red earthworms (Lumbricus rubellus) for raw and photoactivated cow urine. Results: Antimicrobial activity of ZO photoactivated cow urine extract (ZOPUE) at 20 μg/ml concentration was found to show better minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values (MIC: 13.8 μg/ml for E. coli, MBC value >25 μg/ml) when compared with ZO raw cow urine extract (ZOUE) (MIC: 14.3 μg/ml for E. coli, MBC value >25 μg/ml). Larvicidal activity of ZOPUE at a concentration of 25% v/v showed a better mortality rate of 38.6% v/v when compared with ZOUE at a concentration of 25% v/v as 35.2% v/v. Anthelmintic activity of ZOPUE was found to show better paralysis and death rate at a concentration of 10 mg/ml, that is, 38.2 min for paralysis and 58.9 min when compared with ZOUE, that is, 39.6 min paralysis rate at a concentration of 10 μg/ml and death time observed was 59 min at 10 μg/ml concentration. Conclusion: Antimicrobial, larvicidal, and anthelmintic activity of ZOPUE were more significant when compared with ZO extract prepared with raw cow urine.

Helminthosis is one of the greatest causes of parasitic disease and loss in animal productivity. As such, the control of helminth parasites is of critical importance. This study was aimed to investigate the in vitro anthelmintic activity of Dennettia tripetala G. Baker (Annonaceae) fruits against Haemonchus contortus. Using in vitro techniques, the anthelmintic activity of extracts and fractions of D. tripetala G. Baker (Annonaceae) was evaluated for ovicidal (Egg hatch inhibition test) and larvicidal (larval mortality test) activity. Besides, the maximum tolerated dose was determined in adult albino rats administered, 300, 400, and 500mg/kg body weight of the CME fraction, and observed over a period of 48h for signs of toxicity and mortality. Phytochemical screening uncovered the occurrence of flavonoids, steroids/triterpenes, cardiac glycosides, saponins, tannins, carbohydrates, and alkaloids in the crude methanol extract (CME), the ethyl acetate fraction (EAF), and butanol fraction. The maximum tolerated dose of the CME of D. tripetala did not produce observable signs of toxicity or death in all the rats given up to 500mg/kg. The CME and EAF of D. tripetala fruits produced a significant ( ) reduction in the hatchability of H. contortus eggs in a concentration-dependent manner, while the CME at concentrations between 12.5 and 100mg/ml completely inhibited the hatching of H. contortus eggs. Similarly, EAF at doses of 25, 50, and 100mg/ml completely inhibited the hatching of H. contortus eggs. The CME and EAF of D. tripetala fruits produced significant ( ) larvicidal activity against L3 of H. contortus in a concentration-dependent manner while the CME at concentrations between 6.25 and 100mg/ml caused larval mortality of H. contortus L3 larvae completely. This study suggests that methanol extract and fractions of D. tripetala fruits possess beneficial anthelmintic (ovicidal and larvicidal) activity against H. contortus, and may be a suitable alternative anthelmintic candidate for the control of nematodes.

Galloyl flavonoids from Acacia farnesiana pods possess potent anthelmintic activity against Haemonchus contortus eggs and infective larvae.

Anthelmintic effect of Pterogyne nitens (Fabaceae) on eggs and larvae of Haemonchus contortus: Analyses of structure-activity relationships based on phenolic compounds

A study was aimed to evaluate the different extracts of Ailanthus excelsa (Ardu) bark and pods for their antioxidant, antibacterial and anthelmintic activities. Phytochemical analysis showed higher concentrations of phenols, flavonoids, total tannin and saponin (6.37, 4.12, 5.70 and 18.94 mg/g, respectively) in methanol extract of pod as compared to bark (0.22, 0.79, 0.09 and 5.21 mg/g, respectively). A total of 12 phyto-compounds were identified with predominance of 5-(hydroxymethyl)-2-(dimethoxymethyl) furan in methanol extract of bark and 4-phyto-compounds with predominance of 2,3-butanediol, [R-(R*R*)]- in methanol extract of pod. Antioxidant activity was 93.61 and 9.83% in methanol extract of pods and bark, respectively. Methanol extract of pod showed good antibacterial activity against E. coli. On in vitro egg hatch assay, >90% inhibition of egg embryonation was observed by both methanol (@ 0.31 to 5.00 mg/ml) and hydroalcohol (@ 1.25 to 5.00 mg/ml) extracts of bark. Except for the aqueous extract, all other extracts caused >95% egg hatch inhibition at a concentration of 0.63 to 10.00 mg/ml. Among extracts of pods, only hydroalcohol extract (@ 5.00 to 10.00 mg/ml) caused >90% inhibitory activity on egg embryonation; however, at similar concentrations, all the extracts showed >98% inhibition of egg hatching. On larval mortality assay, all the extracts (except aqueous) showed excellent (100%) larvicidal activity at 0.63 to 10.00 mg/ml concentrations. The results indicated that A. excelsa bark and pods have higher antioxidant, antibacterial activity against E. coli and anthelmintic activities against infective larvae of H. contortus.

The lack of anthelmintic products licensed for donkeys and the rising number of small donkey milk farms in the countries of Western Europe and Italy have led to an increased interest in the study of reliable and safe plant-derived treatment alternatives. In this study, the aqueous extracts of Achillea millefolium L. (flowers), Artemisia absinthium L. (aerial parts), Centaurium erythraea Rafn. (flowers), Gentiana asclepiadea L. (rhizomes and roots), Inula helenium L. (rhizomes and roots) and Tanacetum vulgare L. (aerial parts), have been tested in vitro for their potential ovicidal and larvicidal activity against donkey nematodes. An egg-hatching assay (EHA) and larval development assay (LDA) were performed for the in vitro study, and median lethal concentration (LC-50) values for both EHA and LDA were calculated using probit analysis. All tested plant extracts showed strong anthelmintic activity against strongyle eggs and larvae at concentrations ranging between 125 and 1.95 mg/ml, except for C. erythraea, which exhibited very little or no effect at all at the tested concentrations. A strong ovicidal effect was observed in A. absinthium, with an LC-50 value of 0.486 mg/ml (95% confidence interval (CI) 0.21-1.09). Gentiana asclepiadea showed high efficacy against strongyle larvae, with an LC-50 value of 0.041 mg/ml (95% CI 0.01-0.16). The most significant (P < 0.01) anthelmintic activity was exhibited by I. helenium, with an LC-50 value of 0.041 mg/ml (95% CI 0.01-0.16) for EHA and 0.41 mg/ml (95% CI 0.27-0.62) for LDA. The results proved the anthelmintic efficacy of the tested plant extracts, highlighting the need for further research into plant bioactive molecules both in vitro and in vivo.

In vitro anthelmintic activity of the crude hydroalcoholic extract of Piper cubeba fruits and isolated natural products against gastrointestinal nematodes in sheep