The antioxidant activities of the ethanol, petroleum ether, ethyl acetate, n-butanol and water extract fractions from the seeds of papaya were evaluated in this study. The ethyl acetate fraction showed the strongest DPPH and hydroxyl free radical-scavenging activities, and its activities were stronger than those of ascorbic acid and sodium benzoate, respectively. The n-butanol fraction demonstrated the greatest ABTS+ radicals scavenging activity. The ethyl acetate fraction and the n-butanol fraction not only showed higher antioxidant activities than the petroleum ether fraction, water fraction and ethanol fraction, but also showed higher superoxide anion and hydrogen peroxide radicals scavenging activities than those of the other extract fractions. The high amount of total phenolics and total flavonoids in the ethyl acetate and n-butanol fractions contributed to their antioxidant activities. The ethyl acetate fraction was subjected to column chromatography, to yield two phenolic compounds, p-hydroxybenzoic acid (1) and vanillic acid (2), which possessed significant antioxidant activities. Therefore, the seeds of papaya and these compounds might be used as natural antioxidants.

https://www.mdpi.com/1420-3049/16/8/6179/pdf

Antioxidant Activity of Papaya Seed Extracts

The Influenza A virus is a great threat for human health, while various subtypes of the virus made it difficult to develop drugs. With the development of state-of-art computational chemistry, computational molecular docking could serve as a virtual screen of potential leading compound. In this study, we performed molecular docking for influenza A H1N1 (A/PR/8/34) with small molecules such as quercetin and chlorogenic acid, which were derived from traditional Chinese medicine. The results showed that these small molecules have strong binding abilities with neuraminidase from H1N1 (A/PR/8/34). Further details showed that the structural features of the molecules might be helpful for further drug design and development. The experiments in vitro, in vivo have validated the anti-influenza effect of quercetin and chlorogenic acid, which indicating comparable protection effects as zanamivir. Taken together, it was proposed that chlorogenic acid and quercetin could be employed as the effective lead compounds for anti-influenza A H1N1.

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Computational screen and experimental validation of anti-influenza effects of quercetin and chlorogenic acid from traditional Chinese medicine

Chaenomeles speciosa (Sweet) Nakai (C. speciosa, Rosaceae family) is an effective medicinal plant, which has long been used in China to treat various diseases, such as rheumatism, cholera, dysentery, enteritis, beriberi and vitamin C deficiency syndrome. A series of chemical constituents, including triterpenoid, phenolic and phenylpropionic acids, flavonoids, saccharides, essential oils and alkaloids, have been isolated from this plant and some have already been evaluated for their biological activities. Pharmacological investigations demonstrated that C. speciosa possesses anti-inflammatory, antinociceptive, antimicrobial, antioxidant, immunoregulatory, antiparkinsonian, hepatoprotective and antitumor properties. The objective of this review was to summarise available up-to-date and comprehensive information on C. speciosa and provide a relevant reference for further investigations.

/pdf/chaenomeles-speciosa-a-review-of-chemistry-and-pharmacology-1hkv9uy0eu.pdf

Chaenomeles speciosa: A review of chemistry and pharmacology.

Drug resistance of non-small cell lung cancer (NSCLC) is highly correlated to the mutation of the epidermal growth factor receptor (EGFR). Although EGFR tyrosine kinase inhibitors (TKIs) are available clinically, the molecular complexity of NSCLC has made it necessary to search for alternative therapeutic approaches to overcome the drug resistance of NSCLC. In the present study, we identified a triterpene molecule derived from the herbal plant Tripterygium wilfordii, celastrol, as a novel autophagy inducer. We demonstrate that celastrol exhibited selective cytotoxic effect towards EGFR mutant NSCLCs. In addition, celastrol also facilitated the autophagic degradation of Hsp90 client protein including EGFR and Akt on both EGFR wild-type and mutant NSCLCs via calcium-mediated autophagy. Blockage of celastrol-induced autophagic degradation of EGFR by autophagic inhibitor or calcium chelator decreased celastrol-mediated cell death in gefitinib-resistant NSCLCs. Overall, our findings suggest that celastrol may be developed as an effective anticancer agent for treatment of gefitinib-resistant NSCLC in the future.

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Autophagic degradation of epidermal growth factor receptor in gefitinib-resistant lung cancer by celastrol.

Chaenomeles plants are adapted to diverse ecological zones particularly the temperate areas of Korea, Japan, and China. In China, Chaenomeles speciosa is mainly planted in Chongqing, Anhui, and Hubei provinces. Most of the studies till date have been focused on the anti-inflammatory activities of C. speciosa fractions. The present study aimed to review the maximum literature reported for the presence of various phytochemicals in C. speciosa. In addition, the pharmacological properties of these chemical compounds of this plant shall also be discussed. The extracts of the various parts of the plant are rich in diversity of antioxidants, organic acids, phenolics, terpenoids, and many different phytochemicals that bear strong anticancer, antioxidant, antiviral, antibacterial properties, anti-inflammation, antihyperlipidemic, antihyperglycemic, and anti-Parkinson properties. C. speciosa fruits have broad scope in industry as well as in medicines. Not only the leaves and fruits of C. speciosa plant, but various other parts including roots, seeds, bark twigs, and flowers all have long history of clinical trials in curing many human ailments. However, the maximum accessible data concerning the chemical compositions and their broad pharmacological properties of C. speciosa plant parts is pretty restricted that make it more appealing for in-depth investigations.

/pdf/phytochemical-and-pharmacological-properties-of-chaenomeles-4prjf23w5k.pdf

Phytochemical and Pharmacological Properties of Chaenomeles speciosa: An Edible Medicinal Chinese Mugua.

OBJECTIVE To study the chemical constituents of Chaenomeles speciosa. METHODS Isolation and purification were carried out by varied chromatographies, and structure identifications of compounds were carried out by physical methods, chemical methods and spectral data. RESULTS Seven compounds were obtained from the ethyl acetate fraction of C. speciosa, and were identified as cinnamic acid (I), 2'-methoxyaucuparin (II), 2-hydroxyl-butanedioic acid-4-methylester (III), esculetin (IV), p-hydroxybenzoic acid (V), chlorogenic acid (VI), caffeic acid (VII). CONCLUSION Compounds I - IV are obtained from Chaenomeles genus for the first time.

Studies on the chemical constituents of Chaenomeles speciosa

A new hydroxyjasmonic acid derivative, named β-D-glucopyranosyl-12-hydroxy-12-(2″-hydroxy-2″-carboxyethyl)jasmonic acid (1), together with 13 known compounds, were isolated from the n-butanol fraction of the ethanol extract of Polygonum capitatum. Their structures were determined on the basis of spectral analysis. Compounds 2, 8–10, and 12–14 were obtained from P. capitatum for the first time.

Ying-bo Yang

Papers

Studies on the chemical constituents of Chaenomeles speciosa

A New Hydroxyjasmonic Acid Derivative from Polygonum capitatum