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Cucurbitacins, widely found in plants belonging to the family of Cucurbitaceae, are highly oxidized tetracyclic triterpenes with various bioactivities, such as anticancer, anti-inflammatory, and liver protection. Among which, the anticancer activity of cucurbitacins is well studied. Cucurbitacins have been reported to promote apoptosis through the...
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... is reported that triterpenoids can induce cell death. A related group of compounds in this family is cucurbitacins, which widely exist in Cucurbitaceae family plants, for example, cucumber, pumpkin, melon and watermelon (Fig. 1). Cucurbitacins have attracted attentions for more than 50 years due to their biological activities since the 1960s (Gallily, Shohat, Kalish, Gitter, & Lavie, 1962;Gitter, Gallily, Shohat, & Lavie, 1961). To date, more than 100 species of cucurbitacins and their derivatives have been isolated from about 30 genera of Cucurbitaceae ...
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... in the case of achieving the same effect, the dose can be reduced to reduce cytotoxicity and drug resistance (Eyol, Tanriverdi, Karakus, Yilmaz, & Unuvar, 2016). In the treatment of colon cancer, cucurbitacin I can be used as an adjuvant chemotherapy drug to enhance anti-migration and invasion effects and increase the sensitivity of cells to chemical drugs (Song et al., 2015). ...
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... combination of cucurbitacin B with DOC increases the antitumor activity by inhibiting the expression of p-STAT3, Bcl-2 and cyclin B1 in Hep-2 cells ( Liu et al., 2008). Cucurbitacin I reduces the radiation resistance of head and neck squamous cell carcinoma (HNSCC), so it can be used as a radiation sensitizer (Chen, Meng et al., 2010). ...
Context 4
... is reported that triterpenoids can induce cell death. A related group of compounds in this family is cucurbitacins, which widely exist in Cucurbitaceae family plants, for example, cucumber, pumpkin, melon and watermelon (Fig. 1). Cucurbitacins have attracted attentions for more than 50 years due to their biological activities since the 1960s (Gallily, Shohat, Kalish, Gitter, & Lavie, 1962;Gitter, Gallily, Shohat, & Lavie, 1961). To date, more than 100 species of cucurbitacins and their derivatives have been isolated from about 30 genera of Cucurbitaceae ...
Context 5
... in the case of achieving the same effect, the dose can be reduced to reduce cytotoxicity and drug resistance (Eyol, Tanriverdi, Karakus, Yilmaz, & Unuvar, 2016). In the treatment of colon cancer, cucurbitacin I can be used as an adjuvant chemotherapy drug to enhance anti-migration and invasion effects and increase the sensitivity of cells to chemical drugs (Song et al., 2015). ...
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... combination of cucurbitacin B with DOC increases the antitumor activity by inhibiting the expression of p-STAT3, Bcl-2 and cyclin B1 in Hep-2 cells ( Liu et al., 2008). Cucurbitacin I reduces the radiation resistance of head and neck squamous cell carcinoma (HNSCC), so it can be used as a radiation sensitizer (Chen, Meng et al., 2010). ...
Citations
... These vegetables contain multi-sized nutrients, antioxidants, vitamins, amino acids, and small anti-nutrients [7]. It carries non-trivial ethnobotanical significance and has been in use in the treatment of multiple diseases since ancient times [8][9][10][11][12] with weaker side effects, good safety, and multiple healing pathways [13]. Especially, cucurbitacin B has been found to possess anti-Herpes simplex virus 1 biological activity with IC 50 of 0.94 ± 0.2 μM [14] and forms the basis for the selection of this class of organic compound with possibly similar pharmacophore. ...
Background
Cucurbitacins are present in some common vegetables as secondary metabolites and are used by the plants against harmful microbes. Exploration of this capability of natural product based substances against wide variety of microbes seems relevant due to the ease of availability of the resources and safety. In this regard, considering the current pandemic, the antiviral properties of these molecules with a subset of Cucurbitacin I structural derivatives have been screened. The inhibition potential of the phytochemicals was assessed by the stability of the protein–ligand complex formed with the nucleocapsid protein (PDB ID: 7CDZ) of SARS-CoV-2 by computational methods. The proposition of an alternate antiviral candidate that is cost-effective and efficient relative to existing formulations is the main objective of this work.
Results
Server-based molecular docking experiments revealed CBN19 (PubChem CID: 125125068) as a hit candidate among 101 test compounds, a reference molecule (K31), and 5 FDA-approved drugs in terms of binding affinities sorted out based on total energies. The molecular dynamics simulations (MDS) showed moderate stability of the protein-CBN19 complex as implied by various geometrical parameters RMSD, R g , RMSF, SASA and hydrogen bond count. The ligand RMSD of 3.0 ± 0.5 Å, RMSF of C α of protein with less than 5 Å, and smooth nature of SASA and R g curves were calculated for the adduct. The binding free energy (− 47.19 ± 6.24 kcal/mol) extracted from the MDS trajectory using the MMGBSA method indicated spontaneity of the reaction between CBN19 and the protein. The multiple ADMET studies of the phytochemicals predicted some drug-like properties with minimal toxicity that mandate experimental verification.
Conclusions
Based on all the preliminary in silico results, Cucurbitacin, CBN19 could be proposed as a potential inhibitor of nucleocapsid protein theoretically capable of curing the disease. The proposed molecule is recommended for further in vitro and in vivo trials in the quest to develop effective and alternate therapeutics from plant-based resources against COVID-19.
... It has been reported that cucurbitacins show strong cytotoxic effects in many carcinogenic cell types and show anticancer properties by acting on multiple signaling pathways such as JAK/STAT3 Farooqi, 2021, Uremis et al., 2023), Ras/Raf/MEK/ERK (Chan et al., 2010), MAPK (Uremis et al., 2022b), PI3K/ AKT/mTOR (Uremis et al., 2022a), and autophagy (Song et al., 2020). Furthermore, it has been reported that the signaling pathways targeted by cucurbitacins are similar to those targeted by chemotherapeutic drugs, and their combination with small-molecule antineoplastic drugs has been shown to increase the efficacy of drugs by decreasing cell resistance (Jing et al., 2020). ...
... CuD and CuI are natural compounds with antioxidant, anti-inflammatory, immune-modulatory, and anticancer activities (Silvestre et al., 2022, Uremis et al., 2022a, Uremis et al., 2022b. Moreover, their combined effects have been investigated in various cancer types to increase the efficacy of antineoplastic drugs since CuD and CuI show anticancer effects by suppressing multiple signaling pathways at low concentrations (Jing et al., 2020). In a study, the combined application of CuD with gefitinib, an EGFR and tyrosine kinase inhibitor, was investigated in lung cancer cells. ...
Sorafenib, which is a type of systemic multi-kinase inhibitor drug, is used for first-line therapy in treating hepatocellular carcinoma (HCC). In this study, the anticarcinogenic effects of sorafenib–cucurbitacin D and sorafenib–cucurbitacin I combination on HepG2 cell line were investigated. Cell inhibition, migration, apoptosis, cell cycle distribution, mitochondrial membrane potential (ΔΨm), colony formation, and wound healing were investigated by applying cucurbitacin D and I alone or in combination with sorafenib to HepG2 cells. In addition, in order to reveal how cucurbitacins affect the signal pathways known to affect sorafenib; proteins and genes involved in VEGF, EGFR, MMP-2, caspase cascade, PI3K/AKT/mTOR, Raf/MEK/ERK signaling pathways were assessed by western blot and qRT-PCR. It has been shown that cucurbitacin D and I have an antiproliferative effect at low concentrations and show a synergistic effect when combined with sorafenib. Combined administrations induced apoptosis by increasing caspase-9, Bax activity and inhibiting Bcl-xL activation, blocking the cell cycle in G2/M phase and causing loss of ΔΨm. The combinations also suppressed MMP-2 and VEGF, reduced cell migration. The combined cucurbitacin-sorafenib applications inhibited the expression of proteins and genes involved in EGFR and PI3K/AKT/mTOR, Raf/MEK/ERK signaling pathways. Due to showing the synergetic effect of cucurbitacins with sorafenib and their targeting of similar signaling pathways reveal that their combination may increase the efficacy of sorafenib by suppressing angiogenic, metastatic and proliferative activity in HCC.
Graphical abstract
... As a result, researchers have turned to chemical synthesis to overcome these limitations and enhance their potential in clinical settings. In addition, innovative drug delivery strategies, such as nanocarrier systems, have emerged to improve the solubility, stability, and targeted delivery of cucurbitacin to tumor sites [3,7]. Further elucidation of the intricate molecular mechanisms and exploration of synergistic effects with other small-molecule drugs may expand the therapeutic applications of cucurbitacins [3,8]. ...
... They exert anticancer effects through various mechanisms, such as inhibiting tumor cell proliferation, inducing cell cycle arrest and apoptosis (programmed cell death), inhibiting invasion and metastasis, and disrupting the protein backbone ( Figure 7) [92,93,147]. Regarding proliferation inhibition, cucurbitacins exhibit antiproliferative activity in many cell lines, without significant cellular and tissue specificity [7]. In addition, it has been shown that they can, inhibit angiogenesis (the formation of new blood vessels that supply blood to the tumor) and affect the migration and invasion of tumor cells. ...
... Cucurbitacin B has been observed to arrest the cell cycle at the G2/M phase, effectively stopping the division and growth of malignant breast cancer cells [152]. The disruption of the cell cycle renders cancer cells more susceptible to the effects of chemotherapeutic agents [7]. Cucurbitacin D induces G2/M phase arrest and apoptosis via the ROS/p38 pathway in the Capan-1 pancreatic cancer cell line [153]. ...
Cucurbitacins are tetracyclic triterpenoid secondary metabolites, widely distributed in the Cucurbitaceae family. These bitter-tasting compounds act primarily as defense mechanisms against external injuries, and thus against herbivores, and furthermore, they have also found use in folk medicine in the treatment of various diseases. Many studies have acknowledged significant biological activities of cucurbitacins, such as antioxidant and anti-inflammatory activities, antimicrobial properties, or antitumor potential. Overall, cucurbitacins have the ability to inhibit cell proliferation and induce apoptosis in various cancer cell lines. Both in vitro and in vivo studies were performed to evaluate the anticancer activity of varied cucurbitacins. Cucurbitacins offer a promising avenue for future cancer treatment strategies, and their diverse mechanisms of action make them attractive candidates for further investigation. The aim of the present study is to shed light on the chemical diversity of this group of compounds by providing the sources of origin of selected compounds and their chemical structure, as well as insight into their anticancer potential. In addition, within this paper molecular targets for cucurbitacins and signalling pathways important for cancer cell proliferation and/or survival that are affected by the described class of compounds have been presented.
... Cucurbitacin B (Figure 7) is a triterpene obtained from the Cucurbitaceae family which possesses several bioactivities, such as anti-inflammatory, anticancer, and hepatoprotective properties [379]. In lung cancer, cucurbitacin B has been shown to reduce cell proliferation, migration, invasion, and metastasis in A549 cells. ...
Simple Summary
Lung cancer is the leading cause of mortality in cancer patients, causing an estimated 1.8 million deaths in the year 2020. However, the available therapeutic options exert numerous adverse effects and adequate therapeutic activity is still to be achieved. Therefore, there is a need for the development of safe and effective treatment for lung cancer. Phytochemicals are well documented for their anticancer potential against lung cancer and have a strong rationale for further investigation as a potential chemotherapeutic agent. Notably, phytochemicals act by modulating several signaling pathways, promoting apoptosis, oxidative stress, and disruption of the mitochondrial membrane, inhibiting angiogenesis, and regulating transcription factors. Therefore, an exhaustive and detailed review was carried out to establish the potential role of phytochemicals by conducting a critical analysis of in vitro, in vivo, and clinical evidence in mitigating lung cancer, with emphasis on their impact on signaling pathways.
Abstract
Lung cancer is a heterogeneous group of malignancies with high incidence worldwide. It is the most frequently occurring cancer in men and the second most common in women. Due to its frequent diagnosis and variable response to treatment, lung cancer was reported as the top cause of cancer-related deaths worldwide in 2020. Many aberrant signaling cascades are implicated in the pathogenesis of lung cancer, including those involved in apoptosis (B cell lymphoma protein, Bcl-2-associated X protein, first apoptosis signal ligand), growth inhibition (tumor suppressor protein or gene and serine/threonine kinase 11), and growth promotion (epidermal growth factor receptor/proto-oncogenes/phosphatidylinositol-3 kinase). Accordingly, these pathways and their signaling molecules have become promising targets for chemopreventive and chemotherapeutic agents. Recent research provides compelling evidence for the use of plant-based compounds, known collectively as phytochemicals, as anticancer agents. This review discusses major contributing signaling pathways involved in the pathophysiology of lung cancer, as well as currently available treatments and prospective drug candidates. The anticancer potential of naturally occurring bioactive compounds in the context of lung cancer is also discussed, with critical analysis of their mechanistic actions presented by preclinical and clinical studies.
... Among saponins for which broadspectrum pharmacological bioactivities have been reported, cucurbitacins are the most widely known (Alghasham 2013). Different studies have shown that these compounds, present in plants from the Cucurbitaceae family and used in traditional Chinese medicine, have different biological properties with particular relevance for their anticancer, anti-inflammatory, and hepatoprotective activity (Jing et al. 2020;Liu et al. 2021). Cucurbitacins exhibit anticancer activity through a variety of mechanisms, including the promotion of apoptosis through the Janus kinase/signal (Jing et al. 2020). ...
... Different studies have shown that these compounds, present in plants from the Cucurbitaceae family and used in traditional Chinese medicine, have different biological properties with particular relevance for their anticancer, anti-inflammatory, and hepatoprotective activity (Jing et al. 2020;Liu et al. 2021). Cucurbitacins exhibit anticancer activity through a variety of mechanisms, including the promotion of apoptosis through the Janus kinase/signal (Jing et al. 2020). These highly oxidised tetracyclic triterpenes have shown synergistic effects when combined with some drugs and also have been proposed as potential chemotherapy before the onset of lung cancer (Jing et al. 2020;Liu et al. 2021). ...
... Cucurbitacins exhibit anticancer activity through a variety of mechanisms, including the promotion of apoptosis through the Janus kinase/signal (Jing et al. 2020). These highly oxidised tetracyclic triterpenes have shown synergistic effects when combined with some drugs and also have been proposed as potential chemotherapy before the onset of lung cancer (Jing et al. 2020;Liu et al. 2021). ...
Terpenes are the largest and most diverse group of naturally occurring compounds found in plants. They can be classified according to the number of isoprene units, the most common being monoterpenes (C10), sesquiterpenes (C15), diterpenes (C20), and triterpenes (C30). Besides being the principal constituents of essential oils and playing fundamental roles in plants, many terpenes are extensively used in pharmaceutical and industrial applications ranging from flavours to fragrances and medicines. Several studies have already demonstrated the diversity of terpenes’ biological properties, including cancer chemopreventive effects, antimicrobial, antiviral, analgesic, anti-inflammatory, antifungal, antiparasitic, and other activities. This chapter compiles the various terpenes isolated from plants, their sources, biological activities and beneficial health effects, mechanism of action, extraction and applications, and the future perspective for using the terpenes as lead molecules in several areas of the industry.
... This combination acts on essential proteins such as Akt farnesyl-transferase, platelet-derived growth factors, cyclin A2, CDK2, etc [88]. Cucurbitacin E with doxorubicin successfully induced apoptosis, cell-cycle arrest and autophagy [89]. Recent advances in the study of cucurbitacin IIb (CuIIb) and kinoin A (KinA) from Ibervillea sonorae (S.Watson) Greene highlight the ability of these molecules to reduce proliferation and to tempt apoptotic and cell-cycle apprehension in tumors; also, the levels of STAT3 expression were downregulated after treatment with CuIIb. ...
Cucurbitacins constitute a group of cucumber-derived dietary lipids, highly oxidized tetracyclic triterpenoids, with potential medical uses. These compounds are known to interact with a variety of recognized cellular targets to impede the growth of cancer cells. Accumulating evidence has suggested that inhibition of tumor cell growth via induction of apoptosis, cell-cycle arrest, anti-metastasis and anti-angiogenesis are major promising chemo-preventive actions of cucurbitacins. Cucurbitacins may be a potential choice for investigations of synergism with other drugs to reverse cancer cells’ treatment resistance. The detailed molecular mechanisms underlying these effects include interactions between cucurbitacins and numerous cellular targets (Bcl-2/Bax, caspases, STAT3, cyclins, NF-κB, COX-2, MMP-9, VEGF/R, etc.) as well as control of a variety of intracellular signal transduction pathways. The current study is focused on the efforts undertaken to find possible molecular targets for cucurbitacins in suppressing diverse malignant processes. The review is distinctive since it presents all potential molecular targets of cucurbitacins in cancer on one common podium.
... Cucurbitacin-B is a tetracyclic triterpenoid derived naturally from plants belonging to the Cucurbitaceae family and which previously has been reported to have anticancer effects against human osteosarcoma alone and in combinatorial approach with methotrexate [20,21]. Subsequently, Cucurbitacin-B has also been reviewed exhaustively for its anticancer effects against different carcinomas [22,23]. Thus, we tried to explore the mechanistic insight into the anticancer efficacy of Cur-B against the prostate cancer PC3 cell line. ...
... Intriguingly, instigation of apoptosis in tumors has now become a well-accepted strategy for clinical management of different carcinomas [19,20,24,25]. Several reports have previously substantiated that apoptosis instigation is concomitantly followed by disrupted nuclear and cytoplasmic morphology, resulting in cell apoptosis [21,22,26,27]. The observations reported herewith were indicative of Cur-B-instigated apoptosis in PC-3 cells by initiating abruption within nuclear morphology, especially fragmentation and condensation as seen in the DAPI-and Hoechst-33342-stained fluorescent photomicrographs. ...
Cucurbitacin-B (Cur-B) is an analogue triterpenoid belonging to the Cucurbitaceae family. Previous reports have explicitly outlined various biological activities of Cucurbitaceae family members, including the anticancer activity of Cur-B. In the present study, we tried to elucidate the anticancer efficacy of Cur-B against prostate cancer PC3 cells. PC3 cells were exposed to purified Cur-B at 5, 10, 15, 20 and 25 µM for 24. Cur-B exposure reduced cell viability of PC3 cells at 5 µM (p < 0.05), with further reduction with increased Cur-B concentration (15 µM, p < 0.01 and 25 µM, p < 0.001). Cur-B also succeeded in instigating nuclear fragmentation and condensation, followed by activation of caspase-8, -9 and -3 proportionally with increasing concentrations of Cur-B. Treatment with Cur-B also instigated ROS-mediated oxidative stress both qualitatively and quantitatively at 5 µM, p < 0.05; 15 µM, p < 0.01 and 25 µM, p < 0.001. Increased ROS after Cur-B treatment also led to dissipation of mitochondrial membrane potential, thereby resulting in considerable apoptosis (p < 0.001), which, again, was proportionally dependent on Cur-B concentration. Cur-B exposure to PC3 cells was concomitantly followed by reduced cyclin D1, cyclin-dependent kinase 4 (CDK4) expression and augmented mRNA expression of CDK inhibitor p21Cip1. Intriguingly, Cur-B exposure also led to considerable downregulation of the JAK/STAT signaling cascade, which may be the reason behind Cur-B-mediated apoptosis and cell cycle arrest within PC3 cells. Therefore, these observations explicitly establish that Cur-B could serve in the prevention of prostate cancer.
... LD50 value of Cucurbitachin S was slightly lower than resveratrol but slightly higher than Anakinra Bioavailability of Cucurbitachin S was higher than Anakinra. Other Cucurbitacins especially cucurbitacin B and cucurbitacin E have been studied earlier for their anti-inflammatory, antioxidant and immunomodulatory mechanisms [32], [34]. Resveratrol(PubChem CID: 445154) shows some side effects like nausea, vomiting, diarrhoea, liver dysfunction etc. when taking a dose which is more than 2.5g per day [32], [34], [41]. ...
... Other Cucurbitacins especially cucurbitacin B and cucurbitacin E have been studied earlier for their anti-inflammatory, antioxidant and immunomodulatory mechanisms [32], [34]. Resveratrol(PubChem CID: 445154) shows some side effects like nausea, vomiting, diarrhoea, liver dysfunction etc. when taking a dose which is more than 2.5g per day [32], [34], [41]. Anakinra(Drug bank accession no: DB00026) also shows some side effects like flu symptoms, joint pain etc. Side -effects specifically for Cucurbitacin S have not yet been studied. ...
Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is a causative agent for global pandemic disease nCOVID’19, has directed the attention of the scientific community towards the development of effective vaccines and drugs. Attempts are being made for repurposing existing drugs known for their antiviral activities, and test the traditional herbal medicines, natural compounds, nutraceuticals known for their health benefiting and immune-boosting activity against SARSCoV-2. Multidimensional approach is employed to find effective drugs against SARS-CoV2. In this study, 108 natural compounds were examined in inhibiting human protein targets which are responsible for worsening the condition of COVID-19 through a virtual screening approach. This study has screened the natural compounds 3-Hydroxydecanedioic acid, Cucurbitacin S, Diosgenin which may exhibit inhibitory activity against IL-1 receptor,IL-6 receptor respectively. It has also revealed that Dihydro-beta-ergocryptine and cucurbitacin S may exhibit inhibitory activity against TNF-alpha receptor. Further it concluded that exfoliazone shows better inhibitory activity against P38-MAPK and NF-κB pathway inhibitory proteins. These natural compounds could lead the way for future drug discovery, design and development. This will help researchers to scout new drugs in drug discovery(in-vitro and in-vivo studies).
... To treat chapped hands, burns and hemorrhoids Liniment Mshelia et al. (2017) To treat AIDS Bot et al. (2007) abundant in Bryonia, Citrullus, Cucumis, Cucurbita, Echinocystis, Lagenaria, Luffa and Momordica genera (Kaushik et al. 2015). Several cucurbitacins have been also isolated from other plant families, including Brassicaceae, Begoniaceae, Rosaceae, Scrophulariaceae and Thymelaeaceae (Kaushik et al. 2015;Jing et al. 2020). Cucurbitacins are bitter compounds and for this reason, they are likely to be synthetized as oviposition or feeding deterrents for many insects, or as a defense role to protect plants against herbivores (Ríos et al. 2005). ...
... They were able to induce the apoptotic pathways and block cell cycle by inhibiting cyclins. Their ability to increase autophagy and to inhibit the invasion and migration of cancer cells as well their synergistic interaction when combined with anticancer drugs, in several cancer cells, have also been reported (Ateba et al. 2018;Jing et al. 2020). Herein, we will focus on the ability of cucurbitane-type triterpenoids as multidrug resistance reversers in cancer. ...
Momordica balsamina L. (Cucurbitaceae), frequently named balsam apple, southern balsam pear or African pumpkin, is a vegetable with high nutritional value, being mostly used as food in sub-Saharan Africa. It has also been largely used in traditional medicine to treat several diseases, such as malaria fevers and diabetes. As a member of the Cucurbitaceae family, the main constituents are cucurbitane-type triterpenoids, with different oxidation patterns, named cucurbitacins. This review aims at summarizing our contribution to the phytochemical study of M. balsamina and the evaluation of the
isolated cucurbitacins and derivatives as multidrug resistance reversers in cancer cells and bacteria. In this way, the selective antiproliferative activity against multidrug resistant cancer cells of cucurbitacins obtained from M. balsamina, their ability as P-glycoprotein inhibitors in cancer cells overexpressing this ABC transporter, as well as efflux pump inhibitors in resistant bacteria strains are reviewed. Moreover, the in vitro antimalarial activity of cucurbitacins and acyl derivatives against the blood and liver-stages of Plasmodium strains, and the in vivo activity of selected compounds is also reviewed. Besides our work, edible and medicinal uses, and other studies mainly reporting the biological activities of M. balsamina extracts, such as antidiabetic, antibacterial,
anti-inflammatory, and antioxidant properties are also addressed.
... Senyawa Kukurbitasin dari daun A. ilicifolius memiliki aktivitas antibakteri yang lemah. Beberapa penelitian sebelumnya menunjukkan bahwa senyawa ini memiliki beberapa bioaktivitas sebagai antitumor, anti-inflamasi, antidiabetes, Aterosklerosis, Promotor sirkulasi darah, dan Immunosuppressant (Jian et al., 2005;Jing et al., 2020;Kaushik et al., 2015).Kukurbitasin memiliki beberapa analog yang memiliki bioakvitas yang berbeda. Kukurbitasin B diketahui memiliki aktivitas antibakteri terhadap S. aureus (Hassan et al., 2017), sedangkan Kukurbitasin E memiliki potensi antibakteri terhadap bakteri gram positif dan sedang terhadap bakteri gram negatif (Chawech et al., 2015). ...
Staphylococcus aureus dan Escherichiacoli merupakan mikroba patogen penyebab infeksi kulit dan diare. Infeksi bisa diatasi dengan penggunaan antibiotik alami. Penelitian sebelumnya menunjukkan A. ilicifoliusberpotensi sebagai antibiotik alami karena beberapa bagian tanaman ini memiliki antimikroba aktif.Tujuan penelitian ini untuk mengisolasi senyawa bioaktif dari ekstrak etanol daun A. ilicifolius dan menguji bioaktivitasnya sebagai antibakteri terhadap S. aureus dan E.coli. Isolasi senyawa dengan Kromatografi Vakum Cair (KVC). Selanjutnya dilakukan pengujian aktivitas antibakterinya dengan menggunakan metode disc-diffusion. Hasilnya diperoleh 12 fraksi menggunakan KVC dimana fraksi 3 (F3) didapatkan kristal. Kristal tersebut direkristalisasi dengan n-heksana, untuk mendapatkan isolat F3. Kemurnian isolat diuji dengan tiga eluen Kromatografi Lapis Tipis (KLT), kemudian dilanjutkan dengan karakterisasi dan uji antibakteri. Interpretasi skrining fitokimia dan analisis dengan UV-Vis menunjukkan isolat F3 merupakan senyawa triterpenoid, yang diperkuat dengan hasil Fourier-Transform Infrared (FTIR) bahwa terdapat gugus fungsi -OH (3321,96 cm-1), -CH alifatik (2954,95 cm-1), -C = C (1661,16 cm-1), -CH (1447.93 cm-1, 1378,11cm-1), -CO (1050,54 cm-1), -C = C alkena (881,11 cm-1). Hasil spektrum UV-Vis mengindikasikan isolat F3 memiliki panjang gelombang maksimum (? max) pada 208 nm dan 230 nm yang menunjukkan adanya gugus C=C terkonjugasi. Dari hasil uji aktivitas antibakteri didapatkan bahwa isolat F3 memiliki aktivitas antibakteri yang lemah terhadap E. coli dan S. aureus.
Kata kunci: antibakteri, E. coli, jeruju (A. ilicifolius), S. aureus, triterpenoid.
Staphylococcus aureus and Escherichia coli are pathogenic microbes cause of skin infection and diarrhoea. Infections can be resolved with use of natural antibiotics. Previous research has shown A. ilicifolius has potential as a natural antibiotic because some parts of this plant have antimicrobial actives. This study aimed to isolate the bioactive compound from the ethanol extract of A. ilicifolius leaf and test the antibacterial bioactivity against S. aureus and E. coli. The isolation of the compounds was carried out by Vacuum Liquid Chromatography (VLC) and the antibacterial activity was tested using disc diffusion method. Twelve fractions were obtained from the VLC, where crystals were gained for the fraction 3 (F3). The crystals are recrystallized with n-hexane to obtain F3 isolates. The purity of the isolates was tested by Thin Layer Chromatography (TLC) by using 3 eluents followed by characterization and antibacterial assay. Fourier-Transform Infrared (FTIR) interpretation indicated that F3 isolate was triterpenoid compound having -OH group (3321.96 cm-1), -CH aliphatic (2954.95 cm-1), -C=C (1661.16 cm-1), -CH (1447.93 cm-1, 1378.11cm-1), -CO (1050.54 cm-1), -C=C alkenes (881.11 cm-1). UV-Vis spectrum showed that the F3 isolate had a maximum wavelength (? max) at 208 nm and 230 nm which indicated the presence of a conjugated C=C group. The results of antibacterial activity test showed that F3 isolate had low antibacterial activity against E. coli and S. aureus.
Keywords: antibacterial, E. coli, jeruju (A. ilicifolius), S. aureus, triterpenoid.
