Antipyretic activity of Calotropis gigantea, Vernonia cinerea,and Cissampelos pareiraextractsonlipopolysaccharide-induced pyrexia in rabbits

This study aims to evaluate the antipyretic activity of Calotropis gigantea (CG), Vernonia cinerea (VC), and Cissampelos pareira (CP)extracts. Rabbits were received an intravenous lipopolysaccharide (LPS) after being orally administered with the plant extracts or paracetamol, a reference drug. The treatment of CG and VC ethanolic extract (125 and 250 mg/kg) and paracetamol (150 mg/kg) significantly reduced LPS-induced pyrexia. Moreover, ethyl acetate fraction (50 mg/kg) of CG showed a more significant effect in lowering the hyperthermia than dichloromethane, n-butanol fraction, or water residue. In conclusion, this study demonstrated that CG and VC ethanolic extract possess antipyretic activity. Besides, the components in the ethyl acetate fraction of CG play an important role in the antipyretic property of this herb

Karakter Morfologi Dan Anatomi Sawilangit (Vernonia Cinera L.) Pada Ketinggian Yang Berbeda

Vernonia cinerea L. (sawilangit) is a wild plant that has potential as a medicinal plant because of the secondary metabolites in each organ. This research aimed to explore the morphological and anatomical characters of the sawilangit that grow at different altitudes in Banyumas, Cilacap, and Purbalingga. Plant samples were taken using the purposive random sampling method at an altitude of <350 masl, 350–700 masl, and >700 masl. Sawilangit growing at <350 masl has superior morphological and anatomical characters than sawilangit growing at the other two altitudes, which have the characteristics of taller, wider leaf, larger stem diameters, and darker flower color. The observation on quantitative of morphological and anatomical characters showed that sawilangit at <350 masl has an average height of 66.17 cm, root diameter of 0.33 cm, stem diameter 0.32 cm, leaf length and width of 5.7 cm and 2.14 cm, and stomata index of 0.28. These results indicated that altitude <350 masl is suitable for sawilangit growth because it can produce optimal morphological and anatomical characteristics.

Pengaruh Ketinggian Tempat Tumbuh Terhadap Kandungan Fitokimia dan Antioksidan Ekstrak Akar Sawi Langit (Vernonia cinerea L.)

This study aims to determine the effect of altitude on the phytochemical and antioxidant content of sawi langit (Vernonia cinerea L.) root. Sawi langit is a herbaceous plant that has potential as a medicinal plant. This plant can thrive in the tropics. In this study, sawi langit were taken from three altitudes, namely <400 masl, 401-800 masl and >801 masl in the Banyumas, central Java. The sample used was sawi langit root which was extracted using 3 types of solvents (methanol, ethyl acetate and n-hexan). Phytochemical tests showed positive results of the content of flavonoid, alkaloids, tannins, terpenoids and saponins compounds in the extract of sawi langit root from the three altitude with differences effectiveness of each solvent. At an altitude of <400 masl and extraction using methanol resulted strong antioxidant activity with an IC50 value 78.56 ± 3.2 μg/ml compared to an altitude of 401-800 masl and >801 masl

Antimicrobial activity of methanolic extracts of Vernonia cinerea against Xanthomonas oryzae and identification of their compounds using in silico techniques

Bacterial Leaf Blight (BLB) disease is an extremely ruinous disease in rice, caused by Xanthomonas oryzae pv. oryzae (Xoo). Although various chemicals are available to manage BLB, they are toxic to the environment as well as humans. Hence there is a need to develop new pesticides as alternatives to hazardous chemicals. Therefore, a study was carried out to discover new potent natural pesticides against Xoo from different solvent extracts of Vernonia cinerea. Among all the fractions, the methanolic extract showed the highest inhibition zone. Further, to gain mechanistic insight of inhibitory action, 40 molecules of methanolic extracts were subjected for in silico study against two enzymes D-alanine—D-alanine ligase (Ddl) and Peptide deformylase (PDF). In silico study showed Rutin and Methanone, [1,4-dimethyl-7-(1- methylethyl)-2- azulenyl]phenyl have a good binding affinity with Ddl while Phenol, 2,4-bis(1-phenylethyl)- and 1,2-Benzenedicarboxylic acid, diisooctyl ester showed an excellent binding affinity to PDF. Finally, the system biology approach was applied to understand the agrochemical’s effect in the cell system of bacteria against both the enzymes. Conclusively, these four-hit compounds may have strong potential against Xoo and can be used as biopesticides in the future.

Pre-clinical development of an anti-cancer drug ENZ302, a promising candidate for multiple cancer therapeutics.

e13053 Background: Vernonia cinerea extract has been known to be used for various haematological disorders including cancer. In the current study, using state-of-the-art extraction and bioanalytical tools we have identified an active compound having anti-tumor properties from the same plant Vernonia cinerea. The crude extract of Vernonia cinerea as well as the active molecule obtained through the chemical route (ENZ302) showed anti-tumor activity against various cancer models including CML, AML, ALL, HER2+ breast cancer, colon cancer, etc. Methods: Various methods including RP-HPLC, XRD, NMR, IR, cell based assay and LC-MS were used to elucidate the molecular structure of ENZ302. MTD, DRF, PK, and Xenograft study etc were carried out in murine model during the preclinical development of ENZ302. Results: ENZ302 resulted significant cytotoxic effect within 8 hrs of treatment in TNBC (Triple Negative Breast Cancer) model, MDA-MB-468 cells when compared with a known inhibitor Lapatinib. However, ENZ302 treatment in primary cells demonstrates no anti-proliferation activity, indicating the specificity of it’s mode of action. Interestingly, a dose-dependent decrease in tumor volumes was observed for ENZ302 in a xenograft model of TNBC while administered orally. ENZ302 did not cause any adverse changes even at 2gm/Kg dose, indicating the safety of the compound. Although a single-dose PK study showed that ENZ302 has a half-life of ̃40 mins, however, in vitro metabolism of the compound in mouse, rat, dog, and human hepatocytes/microsomes showed the molecule is stable in hepatocyte with very low clearance in microsomes (half-life > 30 min), indicating most of the clearance occurring through the kidney. Conclusions: Our preliminary data suggest that ENZ302 is a specific tyrosine kinase (e.g. Src) inhibitor and a promising therapeutic agent against several cancers. A comprehensive proteomic analysis is ongoing to understand the mechanism of action of ENZ302 that makes it effective against several cancers. The discovery of ENZ302 holds ample opportunities to develop a safe and efficacious treatment regimen against several cancers including TNBC.

The Dichloromethane Fraction of Vernonia cinerea Impart Pro-Apoptotic, Genotoxic, Cell Cycle Arrest, and Drug Efflux Inhibitory Effects on Human Adenocarcinoma Cells

Background: Vernonia cinerea (VC) is an important medicinal plant used in the indigenous system of therapy. In ethnomedicine, VC has demonstrated anticancer properties. However, the mechanisms of action VC is not known. Objective: To establish the anticancer mechanisms of ‘bioactive fractions of VC’ on human adenocarcinoma cells. Methods: The IC50 values of characterized VC extract and fractions in human adenocarcinoma and normal epithelial cells were determined using Sulforhodamine B (SRB) assay. Acridine Orange- Ethidium Bromide (AO-EB) assay/Hoechst 33342 assay, Comet assay, and Cell cycle analysis were used to determine apoptosis, genotoxicity, and cell cycle-specific changes in cancer cells, respectively. Rhodamine 123 (Rho-123) efflux assay and Mitoxantrone (MX) efflux assay were used to assess the inhibition of Multidrug Resistance (MDR) transporters. Results: The dichloromethane fraction of VC (VC-DM) imparted dose-dependent cytotoxicity in human adenocarcinoma cells with fewer effects in human normal epithelial cells. This ‘sesquiterpenoids’ enriched fraction (VC-DM) induced apoptosis, DNA damage, genotoxicity, and G2/M phase arrest in human adenocarcinoma cells. Interestingly, VC-DM significantly inhibited the functional activity of MDR transporters (ABCB1 and ABCG2) and caused ‘synergistic cytotoxic effects’ with anticancer drugs in human adenocarcinoma cells. Conclusion: The bioactivity guided fractionation of VC revealed that the specific ‘sesquiterpenoids enriched fraction’ (VC-DM) imparted cytotoxicity in human adenocarcinoma cells with fewer effects on normal cells. Mechanistic studies have shown that VC-DM induced apoptosis, DNA damage, genotoxicity, cell cycle arrest (G2/M), inhibited the functional activity of MDR transporters (ABCB1 and ABCG2), and produced ‘synergistic cytotoxic effects’ (combinatorial treatments with anticancer drugs) in human adenocarcinoma cells. Taken together, the findings of this study emphasize and validates VC-DM as a promising ‘anticancer agent’ against human adenocarcinomas, including those with a multi-drug resistant phenotype.

UJI EFEKTIVITAS SENYAWA FLAVONOID DARI EKSTRAK ETANOL DAUN SAWILANGIT (Vernonia cinerea (L.) Less) SEBAGAI ANTIPIRETIK PADA TIKUS PUTIH JANTAN GALUR WISTAR (Rattus norvegicus) YANG DIINDUKSI VAKSIN DPT

ABSTRACTSawilangit leaves (Vernonia Cinerea (L.) Less) is a plant that contains flavonoids as an antipyretic. The purpose of this study was to determine the effectiveness of flavonoid compounds from ethanol extract of sawilangit (Vernonia cinerea (L.) Less) leaves as an antipyretic in male white rats Wistar strain (Rattus norvegicus) induced by DPT vaccine. A total of 15 male rats were divided into 5 treatment groups, namely the negative control group (CMC 1%), the positive control group (paracetamol), and the ethanol extract group of sawilangit leaves with a dose of 200 mg, a dose of 400 mg, a dose of 800 mg. Each mouse was induced intramuscularly with a DPT vaccine at a dose of 0.3 ml. Temperature measurements were carried out before and after induction, then every 30 minutes after giving the test material from the 30th minute to the 180th minute. Data were analyzed statistically with One Way ANOVA and continued with LSD test to see significant differences between treatments. The results showed that the ethanol extract of sawilangit leaves had an antipyretic effect on male white rats Wistar strain..Key words: Antipyretics, Vernonia Cinerea, male white rats ABSTRAKDaun Sawilangit (Vernonia Cinerea (L.) Less) adalah salah satu tanaman yang mengandung zat Flavonoid sebagai antipiratik. Tujuan penelitian ini untuk mengetahui adanya efektivitas senyawa flavonoid dari ekstrak etanol daun sawilangit (Vernonia cinerea (L.) Less) sebagai antipiretik pada tikus putih jantan galur wistar (Rattus norvegicus) yang diinduksi vaksin DPT. Sebanyak 15 ekor tikus putih jantan dibagi 5 kelompok perlakuan yaitu kelompok kontrol negatif (CMC 1%), kelompok kontrol positif (parasetamol), dan kelompok ekstrak etanol daun sawilangit dosis 3,6 mg, dosis 7,2 mg, dosis 14,4 mg. setiap tikus diinduksi vaksin DPT dosis 0,3 ml secara intramuscular. Pengukuran suhu dilakuan sebelum dan sesudah induksi, kemudian setiap 30 menit setelah pemberian bahan uji dari menit ke-30 sampai menit ke-180. Data dianalisis secara statistika dengan One Way ANOVA dan dilanjutkan uji LSD untuk melihat beda nyata antar perlakuan. Hasil penelitian menunjukan bahwa Ekstrak etanol daun sawilangit mempunyai efek antipiretik terhadap tikus putih jantan galur wistar. Kata kunci: Antipiretik, Vernonia Cinerea, tikus putih jantan