In-vitro antitumor activity evaluation of hyperforin derivatives

  title={In-vitro antitumor activity evaluation of hyperforin derivatives},
  author={Feng Sun and Jin-Yun Liu and Feng He and Zhong Liu and Rui Wang and Dong-mei Wang and Yifei Wang and Depo Yang},
  journal={Journal of Asian Natural Products Research},
  pages={688 - 699}
The derivatives of hyperforin, namely hyperforin acetate (2), 17,18,22,23,27,28,32,33-octahydrohyperforin acetate (3), and N,N-dicyclohexylamine salt of hyperforin (4), have been investigated for their antitumor properties. In-vitro studies demonstrated that 2 and 4 were active against HeLa (human cervical cancer), A375 (human malignant melanoma), HepG2 (human hepatocellular carcinoma), MCF-7 (human breast cancer), A549 (human nonsmall cell lung cancer), K562 (human chronic myeloid leukemia… 

Mechanistic insights into the antileukemic activity of hyperforin.

In summary, hyperforin targets molecules involved in signaling pathways that control leukemic cell proliferation, survival, apoptosis, migration and angiogenesis, and shows interesting in vivo properties in animal models.

Chemistry and Biology of the Polycyclic Polyprenylated Acylphloroglucinol Hyperforin

An overview of the synthetic studies reported so far for the racemic and enantioselective syntheses of (+)-hyperforin (1) and analogues is presented, and light is shed on the intriguing structure–activity relationships (SARs) of the natural product.

Biotechnological production of hyperforin for pharmaceutical formulation

  • M. GaidEline Biedermann L. Beerhues
  • Biology
    European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
  • 2018

Super Antibiotics, Part II. Hyperforin, Mass Spectroscopy (MS) and Gas Chromatography-Mass Spectrometry (GC-MS), Evidence of Permeability of the Blood-Testis Barrier (BTB) and the Blood-Brain Barrier (BBB) to Hyperforin

Evidence of the permeability of the blood-testis barrier (BTB) and blood-brain barrier (BBB) to hyperforin and its distribution in other organs of the domestic pig (Sus scrofa domesticus) are revealed.

Evaluation of the Effect of Topical Hypericum perforatum Oil on Excisional Palatal Wound Healing in Rabbits

The results of this study demonstrated that topical HP oil treatment did not provide an additional benefit to its base, olive oil, in the early phase of secondary wound healing.

The Melding of Drug Screening Platforms for Melanoma

The union of these three approaches (in silico, in vitro, and in vivo) is essential for improving the discovery and development of new molecules with potential antimelanoma action and would provide greater confidence and safety for preclinical trials, which will translate to more successful clinical trials.

An unusual Michael-induced skeletal rearrangement of a bicyclo[3.3.1]nonane framework of phloroglucinols to a novel bioactive bicyclo[3.3.0]octane.

A novel skeletal rearrangement of bicyclo[3.3.1]nonane-2,4,9-trione to an unprecedented highly functionalized bicyclo-octane system induced by an intramolecular Michael addition, found to be similarly active to hyperforin, against PC-3 cell lines.



Aristoforin, a Novel Stable Derivative of Hyperforin, Is a Potent Anticancer Agent

One of these hyperforin derivatives, Aristoforin, is more soluble in aqueous solution than hyper forin and is additionally highly stable and retains the antitumor properties of the parental compound without inducing toxicity in experimental animals, suggesting that Aristo forin has potential as an anticancer drug.

Hyperforin Inhibits Cancer Invasion and Metastasis

Hyperforin (Hyp), the major lipophilic constituent of St. John’s wort, was assayed as a stable dicyclohexylammonium salt (Hyp-DCHA) for cytotoxicity and inhibition of matrix proteinases, tumor invasion, and metastasis and qualifies as an interesting lead compound to prevent and contrast cancer spread and metastatic growth.

Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo

Together, hyperforin is a novel type of 5-LO inhibitor apparently acting by interference with the C2-like domain, with high effectiveness in vivo.

Hyperforin and aristoforin inhibit lymphatic endothelial cell proliferation in vitro and suppress tumor‐induced lymphangiogenesis in vivo

In thoracic duct ring outgrowth assays, hyperforin and aristoforin both inhibited lymphangiogenesis, as evidenced by the suppression of lymphatic capillary outgrowth, and in an in vivo animal model, both compounds were able to inhibit tumor‐induced lymphang iogenesis.

Inhibition of tumour cell growth by hyperforin, a novel anticancer drug from St. John's wort that acts by induction of apoptosis

In vivo, hyperforin inhibited the growth of autologous MT-450 breast carcinoma in immunocompetent Wistar rats to a similar extent as the cytotoxic drug paclitaxel, without any signs of acute toxicity.

Hyperforin, a bio‐active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process

It is shown that hyperforin inhibits angiogenesis in vitro in bovine aortic endothelial cells and in vivo in the chorioallantoic membrane assay, confirming the recent and growing evidence about a potential role of this compound in cancer and metastasis inhibition and making it a promising drug for further evaluation in the treatment of angiogenic‐related pathologies.

Inhibition of prostaglandin E(2) production by anti-inflammatory hypericum perforatum extracts and constituents in RAW264.7 Mouse Macrophage Cells.

Constituents that were present in the Hp extracts at concentrations that inhibited the production of prostaglandin E(2) (PGE(2)) were pseudohypericin and hyperforin, suggesting that they are the primary anti-inflammatory constituents along with the flavonoids, and perhaps the interactions of these constituents and other unidentified compounds are important for the anti- inflammation activity of the H p extracts.