Meroterpenoids with Antitumor Activities from Guava (<i>Psidium guajava</i>)

Qin, Xu‐Jie; Qian, Yu; Yan, Hong‐Bin; Khan, Afsar; Feng, Mi-Yan; Li, Pan-Pan; Hao, Xiao‐Jiang; An, Lin‐Kun; Liu, Haiyang

doi:10.1021/acs.jafc.7b01762

Cited by 99 publications

(44 citation statements)

References 27 publications

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“…The annotation results were confirmed by commercial authentic standards (Table 1, compounds 2, 5, and 6) or a purification process (1). Guajadial B exhibited antitumor activity in five human cancer cell lines (HCT116, CCRFCEM, DU145, Huh7, and A549) at an IC50 value of 150 nM [28]. Medicagenic acid has been identified as an antifungal agent against Pyricularia pryzae (minimum inhibitory concentration (MIC) = 0.01 mg/mL and minimum fungicidal concentration (MFC) = 0.03 mg/mL) [29].…”

Section: Discussionmentioning

confidence: 99%

Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach

et al. 2019

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With an estimated annual incidence of one million cases, leishmaniasis is one of the top five vector-borne diseases. Currently available medical treatments involve side effects, including toxicity, non-specific targeting, and resistance development. Thus, new antileishmanial chemical entities are of the utmost interest to fight against this disease. The aim of this study was to obtain potential antileishmanial natural products from Psidium guajava leaves using a metabolomic workflow. Several crude extracts from P. guajava leaves harvested from different locations in the Lao People's Democratic Republic (Lao PDR) were profiled by liquid chromatography coupled to high-resolution mass spectrometry, and subsequently evaluated for their antileishmanial activities. The putative active compounds were highlighted by multivariate correlation analysis between the antileishmanial response and chromatographic profiles of P. guajava mixtures. The results showed that the pooled apolar fractions from P. guajava were the most active (IC 50 = 1.96 ± 0.47 µg/mL). Multivariate data analysis of the apolar fractions highlighted a family of triterpenoid compounds, including jacoumaric acid (IC 50 = 1.318 ± 0.59 µg/mL) and corosolic acid (IC 50 = 1.01 ± 0.06 µg/mL). Our approach allowed the identification of antileishmanial compounds from the crude extracts in only a small number of steps and can be easily adapted for use in the discovery workflows of several other natural products.Molecules 2019, 24, 4536 2 of 13 of the human population to the parasite, and human behavior [3]. The disease is characterized by four forms; visceral leishmaniasis, post-kala-azar dermal leishmaniasis, cutaneous leishmaniasis, and mucocutaneous leishmaniasis [4]. Available medical treatments are not sufficient because of their extensive toxicity (e.g., the nephrotoxicity of amphotericin B, the teratogenicity of miltefosine), their lack of efficacy, their expensive cost (amphotericin B), the development of drug resistance (sodium stibogluconate and meglumine antimoniate), and non-specific targeting [4,5]. Fexinidazole, a 5-nitroimidazole, was recently in phase II of clinical trials on visceral leishmaniasis but exhibited a lack of efficacy, and in 2018 no new lead molecules were included in clinical trials [4].Control of leishmaniasis by traditional approaches (vector control and treatment of patients) is facing the difficulties of identifying new cost-effectively produced bioactive molecules able to be produced on an industrial scale, rapid development of drug resistance, and the lack of access to drugs by the threatened populations. These issues are at the heart of concerns of the WHO regarding the control of tropical diseases [6]. Therefore, combination therapies are used to improve the efficacy of antileishmanial therapies and can shorten treatment duration [7]. Furthering our fundamental knowledge through original approaches, herein concerning the activity of natural compounds from a promising plant species active against Leishmania spp., is vital to ov...

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Section: Discussionmentioning

confidence: 99%

Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach

et al. 2019

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“…These functions of guava extracts are related to numerous bio-active molecules such as beta-caryophyllene oxide, vitamins, tannins, phenolic compounds, flavonoids and triterpenoid acids [2,[4][5][6]. Previous studies have demonstrated that guava extracts can inhibit cell growth in various cancers such as lung cancer, colorectal carcinoma, myeloid leukemia, squamous cell carcinoma, myeloma, cervical cancer and gastric cancer [3,7,8]. However, the mechanisms induced by guava extracts that result in anti-cancer activities remain unknown.…”

Section: Introductionmentioning

confidence: 99%

Anti-cancer therapeutic benefit of red guava extracts as a potential therapy in combination with doxorubicin or targeted therapy for triple-negative breast cancer cells

et al. 2020

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Guava extracts purified from leaf and bark have many bio-active molecules with anti-cancer activities. In addition, lycopene-rich extracts obtained from red guava fruit can induce apoptosis in estrogen receptor−positive breast cancers. Triple-negative breast cancer (TNBC) lacks estrogen receptors, progesterone receptors and human epidermal growth factor receptor 2 (HER2) and, therefore, hormone therapy and targeted therapy are not used in the clinic. The purpose of this study was to determine whether red guava fruit extracts can affect the proliferation of TNBC cells. In this study, cell viability was determined by using the MTT assay. Apoptosis and necrosis were analyzed using flow cytometry. Cleaved caspase-3 and PARP were analyzed by western blotting. We found that red guava extracts can, through caspase-3 activation and PARP cleavage signaling, induce apoptotic and necrotic death in TNBC cells. Our results thus show the therapeutic benefit of red guava extracts as a potential cancer treatment for TNBC in combination with doxorubicin or targeted therapy.

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“…and He et al [33]. These compounds showed interesting anti-cancer activity in vitro against cervical cancer, gastric adenocarcinoma and breast cancer cells, while berkeleyacetal C [34,35,36] and rubratoxin B [37,38,39] showed anti-inflammatory activity and anticancer in vitro.…”

Section: P Purpurogenum Extract Showed Activity Against Ehrlich's Somentioning

confidence: 97%

Penicillium purpurogenumexerts antitumor effects and ameliorates inflammations in Erlich mice model

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Pontes

Guimarães

et al. 2020

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ABSTRACTBackgroundThe bioactive metabolites production contributes to the resistance of fungi towards adverse environmental conditions. Some metabolites often have interesting health-promoting activities. This study addressed the anti-tumoural properties of Penicillium purpurogenum isolated from a polluted lagoon in Northeastern Brazil.MethodsThe extract obtained from the polished environment strain P. purpurogenum was fermented, filtered, concentrated and lyophilized, giving rise to the Ethyl Acetate Extracellular Extract (EAE). The metabolites of the extracellular extract of P. purpurogenum were studied using direct infusion mass spectrometry. The solid Ehrlic tumor model was used to evaluate the extract antitumor activity. Female Swiss mice were divided in groups (n=10/group) as follow: Negative control (CTL-) treated with phosphate buffered solution; Positive Control (CTL+) treated with cyclophosphamide (25mg/mL); Extracts treatment at doses 4, 20 and 100mg/Kg; Animals without tumor or treatment (Sham); and animals without tumor treated with intermediate dose (EAE20). All treatments were performed intraperitoneally, daily during 15 days. After, the animals were eutanized and the tumor, lymphoid organs and serum were used for immunological, histological and biochemical parameters evaluation.ResultsThe extract was rich in meroterpenoids. All doses of the extract significantly reduced tumor size compared to CLT- and were associated with 100% survival. Histologically, the 20 and 100mg/kg doses reduced tumour-associated inflammation and tumour necrosis. The extract also reduced cellular infiltration of lymphoid organs and circulating TNF-α levels when compared with CLT-. The extract did not induce weight loss and renal or hepatic toxic changes.ConclusionsThese results indicate that P. purpurogenum from a polluted marine environment produce hybrid natural products of the terpenoid pathway that exhibits immunomodulatory and antitumor properties in vivo. Thus, fungal fermentation is a biotechnological approach for the production of antitumour agents.

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Meroterpenoids with Antitumor Activities from Guava (Psidium guajava)

Cited by 99 publications

References 27 publications

Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach

Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach

Anti-cancer therapeutic benefit of red guava extracts as a potential therapy in combination with doxorubicin or targeted therapy for triple-negative breast cancer cells

Penicillium purpurogenumexerts antitumor effects and ameliorates inflammations in Erlich mice model

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