The marine-derived fungus Coniothyrium cereale was isolated from the green alga Enteromorpha sp. and found to produce the new phenalenone derivatives 1–7 as well as the known compounds lactone 8, (−) sclerodin (9), lamellicolic anhydride (10), (−) scleroderolide (11), and (−) sclerodione (12). The structures of these closely related compounds were established from extensive spectroscopic investigations on the basis of one and two dimensional NMR spectroscopic studies (1H, 13C, COSY, NOESY, HSQC and HMBC) as well as mass spectrometric analysis (LC/MS, HREIMS and HRESIMS), UV and IR spectra. Compounds 5 and 11 showed the same antimicrobial activity toward Staphylococcus aureus SG 511 with an MIC value of 24 μM. The presence of a diketo-lactone ring as in compounds 5 and 11 was found to be essential for this activity. In agar diffusion assays with Mycobacterium phlei considerable inhibition zones were observed for compounds 2, 4 and 7. Compounds 1, 5 and 9 showed potent inhibition of human leukocyte elastase (HLE) with IC50 values of 7.2, 13.3 and 10.9 μM, respectively.
Covering up to the end of August 2013 Phenalenones are members of a unique class of natural polyketides exhibiting diverse biological potential. This is a comprehensive review of 72 phenalenones with diverse structural features originating from fungal sources. Their bioactive potential and structure elucidation are discussed along with a review of their biosynthetic pathways and the taxonomical relationship between the fungi producing these natural products.
The different pharmacologic properties of plants-containing cynaropicrin, especially artichokes, have been known for many centuries. More recently, cynaropicrin exhibited a potential activity against all genotypes of hepatitis C virus (HCV). Cynaropicrin has also shown a wide range of other pharmacologic properties such as anti-hyperlipidemic, anti-trypanosomal, anti-malarial, antifeedant, antispasmodic, anti-photoaging, and anti-tumor action, as well as activation of bitter sensory receptors, and anti-inflammatory properties (e.g., associated with the suppression of the key pro-inflammatory NF-κB pathway). These pharmacological effects are very supportive factors to its outstanding activity against HCV. Structurally, cynaropicrin might be considered as a potential drug candidate, since it has no violations for the rule of five and its water-solubility could allow formulation as therapeutic injections. Moreover, cynaropicrin is a small molecule that can be easily synthesized and as the major constituent of the edible plant artichoke, which has a history of safe dietary use. In summary, cynaropicrin is a promising bioactive natural product that, with minor hit-to-lead optimization, might be developed as a drug for HCV.
27 September 2011 in ACS Medicinal Chemistry Letters
Herbal products are a major source of herbal medicines and other medicines. Essential oils have shown various pharmacological activities, such as antiviral activity, and therefore are proposed to have potential activity against SARS-CoV-2. Due to their lipophilicity, essential oils can easily penetrate the viral membrane and cause the viral membrane to rupture. In addition, crude essential oils usually have many active constituents that can act on different parts of the virus including its cell entry, translation, transcription, and assembly. They have further beneficial pharmacological effects on the host’s respiratory system, including anti-inflammatory, immune regulation, bronchiectasis, and mucolytics. This review reported potential essential oils which could be promising drugs for COVID-19 eradication. Essential oils have many advantages because they are promising volatile antiviral molecules, making them potential drug targets for the prevention and treatment of COVID-19, whether used alone or in combination with other chemotherapeutic drugs. The aim of the current review is to shed light on the potential essential oils against enveloped viruses and their proposed activity against SARS-CoV-2 which is also an enveloped virus. The objectives were to present all data reflecting the promising activities of diverse essential oils against enveloped viruses and how they could contribute to the eradication of COVID disease, especially in indoor places. The data collected for the current review were obtained through the SciFinder database, Google scholar, PubMed, and Mendeley database. The data of the current review focused on the most common essential oils which are available in the pharmaceutical market and showed noticeable activities against enveloped viruses such as HSV and influenza.