The Cytotoxicity and Nephroprotective Activity of the Ethanol Extracts of Angelica keiskei Koidzumi Stems and Leaves against the NAPQI-Induced Human Embryonic Kidney (HEK293) Cell Line

Ethnopharmacological Relevance. In Indonesia, Angelica keiskei Koidzumi (ashitaba or Japanese celery) has been traditionally used to maintain health and to achieve longevity. Previously, the chlorophyll-rich extract of A. keiskei planted in Korea exhibited a strong antioxidant activity. The objective of the present study was to investigate the cytotoxicity and nephroprotective activity of the ethanol extract of A. keiskei Koidzumi on the N-acetyl-p-benzoquinone imine (NAPQI) induced human embryonic kidney (HEK293) cell line. Materials and Methods. A. keiskei Koidzumi plant was collected from Mount Rinjani, Lombok, Indonesia, and was identified at the School of Biology Sciences and Technology, Bandung Institute of Technology, Indonesia. Extraction of the stems (ASE) and leaves (ALE) was performed by employing ethanol 70% for 3 × 24 h at 26°C. The cytotoxicity study of the extracts was assessed using the water-soluble tetrazolium salt-8 (WST-8) reagent on the HEK293 cell line, while the nephroprotective activity assay was determined on the NAPQI-induced HEK293 cell line. Results. The WST-8 assay showed that the cytotoxicity IC50 of ASE = 2322 μg/mL and IC50 of ALE = 2283 μg/mL. The nephroprotective activity assay revealed that ASE possesses nephroprotective activity against the NAPQI-induced HEK293 cell line at 1161 μg/mL, while ALE does not show the nephroprotective activity. Conclusion. Taken together, lower concentrations of ASE and ALE (<2000 μg/mL) are not toxic to the HEK293 cell line, and only ASE indicates the activity to protect the HEK293 cell line against NAPQI damage. This Japanese celery could be further explored for its potential as a plant-based nephroprotective drug.

Inventory of leaf and flower odorants in plants associated with the life cycle of Japanese Papilio butterflies

The odorants of eight Japanese mainland native species (Citrus x deliciosa, Zanthoxylum ailanthoides Siebold & Zucc, Z. schinifolium Sieb. et Zucc., Z. piperitum L., Phellodendron amurense Ruprecht, Orixa japonica Thunb., Skimmia japonica Thunb., and Boenninghausenia albiflora (Hook.) Rchb. ex Meisn.), one tropical species (Euodia meliifolia (Hance) Benth.), and one invasive species (Ruta graveolens) of the Rutaceae family and three Japanese mainland native species (Angelica keiskei (Miq.) Koidz., Heracleum lanatum W. Bartram, Anthriscus sylvestris (Blume) DC), and one invasive species (Foeniculum vulgare Mill.) of the Apiaceae family were analyzed using gas chromatography–mass spectrometry with dynamic–headspace and thermal–desorption methods. These plants are hostplants to Japanese Papilio butterflies. Herein, these 14 plants were classified into six major groups based on the odorant volatiles, which did not correspond to the current phylogenetic classification. Similarly, floral odorant analysis of the six plant species (Clerodendrum trichotomum Thunb., Cayratia japonica (Thunb.) Gagnep., Robinia pseudoacacia L., Lonicera japonica Thunb., C. deliciosa, Z. ailanthoides) visited by Papilio butterflies for nectaring, revealed the presence of linalool in all the flowers. Floral volatiles in C. deliciosa and Z. ailanthoides exhibited moderate resemblance to their respective leaf volatiles. Interestingly, our results in C. trichotomum was not in complete agreement with previous reports, emphasizing the need for newer methods of extraction and analysis.

In vitro antimalarial activity assay of Ashitaba Leaf ethanolic extract (Angelica keiskei)

Introduction: The incidence of malaria is still very high in number in the world. Difficulty in treating malaria is caused by the resistance of malaria parasites to conventional drugs. An alternative treatment that can be used to treat malaria is to discover new drugs from natural ingredients. Aim: This study aimed to determine the activity of the Ashitaba leaf ethanolic extract as an antimalarial drug to Plasmodium falciparum strain 3D7. Methods: This study tested the activity of Ashitaba extract on the growth of P.falciparum in five concentrations, namely concentration of 0.01 ppm, 0.1 ppm, 1 ppm, 10 ppm, and 100 ppm. Results: The test results showed that the highest inhibitory effect was found on the concentration of 100 ppm with percent inhibition of 79.47 ± 26.91%. The 50% inhibition to parasites showed the half maximal inhibitory concentration (IC50) value of 2.09 ppm, compared to the positive control of which the IC50 of chloroquine was 0.007 ppm. Conclusion: Ashitaba leaf extract can be considered to have very active anti-malarial activity, because it has an IC50 value of less than 5 ppm.

Application of Simplex Lattice Design Method on The Optimisation of Deodorant Roll-on Formula of Ashitaba (Angelica keiskei)

Ashitaba is known to have antioxidant activity and gram-positive antibacterial activity that causes body odor. This is the potential activity for an active substance to be developed as deodorant. The appropriate formula is needed, so it is necessary to optimize the formula using the right method. This study aimed was to determine the application of the simplex lattice design method on the optimization of a deodorant roll-on formula of ashitaba extract. Ashitaba was extracted by the maceration method. The formula optimization design was determined using the simplex lattice design method by Design Expert®7.5.1. The components for optimization were the concentration of carbopol and concentration of TEA, and the optimization parameters were the spreadability test, sticky power, and pH test. The optimum formula of deodorant consists of 0.45% carbopol and 2.05% TEA. The responses of optimum formula obtained spreadability test 6.32 ± 0.33 cm, sticky power 44.67 ± 3.94 seconds, and pH 7.73 ± 0.17. These results meet the criteria for good preparation but need further testing related to the effectiveness of the preparation and the level of acceptance of the preparation by the user.

New Chalcone Derivatives as Effective Anti-SARS-CoV-2 Agents

Flavonoids and related compounds, such as quercetin-based antiviral drug Gene-Eden-VIR/Novirin, inhibit the protease of severe acute respiratory syndrome coronavirus (SARS-CoV-2). The alkylated chalcones isolated from Angelica keiskei inhibit SARS-CoV proteases. Hydroxychloroquine and Favipiravir have been used in many countries since the beginning of the pandemic with the thought that they may have antiviral activity against SARS CoV-2. In this study, we aimed to compare the anti-SARS CoV-2 activities of both newly synthesized chalcone derivatives and these two drugs.The current study aimed to determine the potent antiviral activity of newly synthesized chalcone derivatives against SARS-CoV-2 by calculating the RT-PCR cycling threshold (Ct) values. Antiviral activities of the compounds varied due to being dose dependent. Compound 6, 7, 9 and 16 were highly effective against SARS-CoV-2 at concentrations of 1.60 µg/mL. Structure-based virtual screening was carried out against the most important druggable SARS-CoV-2 targets, viral RNA-dependent RNA polymerase (RdRp), to identify putative inhibitors that could facilitate the development of potential anti-COVID-19 drug candidates. Computational analyses identified eight compounds inhibiting each target, with binding affinity scores ranging from − 4,370 to -2,748 kcal/mol along with their toxicological, ADME, and drug-like properties.