Compendium of the most significant studies with reference to properties, effects.

Baumgartner L, Sosa S, Atanasov AG, Bodensieck A, Fakhrudin N, Bauer J, Del Favero G, Ponti C, Heiss EH, Schwaiger S, Ladurner A, Widowitz U, Della Loggia R, Rollinger JM, Werz O, Bauer R, Dirsch VM, Tubaro A, Stuppner H. Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and proinflammatory mediators in vitro. J Nat Prod. 2011;74:1779–1786. Abstract The roots of Krameria lappacea are used traditionally against oropharyngeal inflammation. So far, the astringent and antimicrobial properties of its proanthocyanidin constituents are considered to account for the anti-inflammatory effect...

Dixit M, Saeed U, Kumar A, Siddigi M, Tamrakar AK, Srivastava AK, Goel A. Synthesis, molecular docking and PTP1B inhibitory activity of functionalized 4,5-dihydronaphtofurans and dibenzofurans. Med Chem. 2010;20:3329–3337. Abstract  Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Inhibitors of PTP1B showed increased insulin sensitivity and normalize plasma glucose level and thus are useful therapeutic agents for the treatment of diabetes. A series of functionalized 4,5-dihydronaphthofurans and dibenzofurans were synthesized, studied through molecular docking and evaluated for their PTP1B inhibitory activity.

Choi HD, Seo PJ, Son BW. Total synthesis of a norneolignan from Ratanhia radix. Arch Pharm Res. 2002 Dec;25(6):786-9. doi: 10.1007/BF02976992. Abstract  The total synthesis of a norneolignan isolated from Ratanhia, 5-(3-hydroxypropyl)-2-(2-methoxy-4'-hydroxyphenyl)benzofuran (8), is described. The key steps contain the one-pot reaction for a 2-arylbenzofuran 6 from methyl 3-(4-hydroxyphenyl)propionate with 2-chloro-2-methylthio-(2'-methoxy-4'-acetoxy)acetophenone (5) in the presence of ZnCl2, and reductive desulfurization of the resulting product 6.

Stahl E, Ittel I. Neue, lipophile Benzofuranderivate aus Ratanhiawurzel. Planta Med. 1981 Jun;42(6):144-54. doi: 10.1055/s-2007-971618. Abstract Two phenols have been isolated from the petroleum-ether extract of Ratanhiae radix Ph. Eur.; structure elucidation has been made by means of the following chemico-physical methods: UV, IR, (1)H-NMR, (13)C-NMR-spectroscopy and mass spectrometry, microhydrogenation and thermofractography. Structures are: 2-(p-methoxy-o-hydroxyphenyl) -5-propenyl (trans)-benzofurane; 2-(p-hydroxyphenyl)-3-methyl-5-propenyl-(trans)-benzofurane. Both compounds - newly discovered in Ratanhiae radix - proved to be effective UV-light filters. They could be useful in sun protection preparations.

Al-Oqail MM. Anticancer efficacies of Krameria lappacea extracts against human breast cancer cell line (MCF-7): Role of oxidative stress and ROS generation. Saudi Pharm J. 2021 Mar;29(3):244-251. doi: 10.1016/j.jsps.2021.01.008. Abstract  Breast cancer is a growing health issue globally and accounts as a second most cause of mortality. Natural products have been a fundamental of health care for long. Plants derived natural products have gained considerable attention over synthetic medicines, since they are safe and non-toxic. Krameria lappacea (Dombey) Burdet and B.B. Simpson plant belonging to Krameriaceae family, has been known for its beneficial effects against diseases. Herein, firstly, cytotoxic potential of petroleum ether (KLH), chloroform (KLC), ethyl acetate (KLEA), and ethanolic (KLET) extracts of K. lappacea was screened against MCF-7 cells exposed to 10-1000 μg/mL for 24 h. Secondly, the most cytotoxic extract (KLH) was used to explore the mechanisms of cytotoxicity in MCF-7 cells. MCF-7 cells were treated with KLH at 250-1000 μg/mL to measure the oxidative stress markers (glutathione (GSH) and lipid peroxidation (LPO)) and reactive oxygen species (ROS) generation. Further, loss of mitochondrial membrane potential (MMP) and caspase-3 and -9 enzyme activities were studied. The viability of MCF-7 cells were decreased from 44% to 90% for KLH, from 7% to 71% for KLEA, from 39% to 80% for KLC, and from 3% to 81% for KLET, respectively at 250-1000 μg/mL as observed by MTT assay. An increase of 91% in LPO and 2.2-fold in ROS generation and a decrease of 59% in GSH and 68% in MMP levels at 1000 μg/mL showed that KLH induced MCF-7 cell death via oxidative stress and elevated level of ROS generation which further leads to mitochondrial membrane dysfunction and activation of caspase enzymes. The findings of this study provide a mechanistic insight on anticancer efficacies of K. lappacea extracts against MCF-7 cells and support the use of it for the treatment of breast cancer diseases.

Genovese C, D'Angeli F, Bellia F, Distefano A, Spampinato M, Attanasio F, Nicolosi D, Di Salvatore V, Tempera G, Lo Furno D, Mannino G, Milardo F, Li Volti G. In Vitro Antibacterial, Anti-Adhesive and Anti-Biofilm Activities of Krameria lappacea (Dombey) Burdet & B.B. Simpson Root Extract against Methicillin-Resistant Staphylococcus aureus Strains. Antibiotics (Basel). 2021 Apr 13;10(4):428. doi: 10.3390/antibiotics10040428. Erratum in: Antibiotics (Basel). 2021 Jun 30;10(7): Abstract Methicillin-resistant Staphylococcus aureus (MRSA) represents a serious threat to public health, due to its large variety of pathogenetic mechanisms. Accordingly, the present study aimed to investigate the anti-MRSA activities of Krameria lappacea, a medicinal plant native to South America. Through Ultra-High-Performance Liquid Chromatography coupled with High-Resolution Mass spectrometry, we analyzed the chemical composition of Krameria lappacea root extract (KLRE). The antibacterial activity of KLRE was determined by the broth microdilution method, also including the minimum biofilm inhibitory concentration and minimum biofilm eradication concentration. Besides, we evaluated the effect on adhesion and invasion of human lung carcinoma A549 cell line by MRSA strains. The obtained results revealed an interesting antimicrobial action of this extract, which efficiently inhibit the growth, biofilm formation, adhesion and invasion of MRSA strains. Furthermore, the chemical analysis revealed the presence in the extract of several flavonoid compounds and type-A and type-B proanthocyanidins, which are known for their anti-adhesive effects. Taken together, our findings showed an interesting antimicrobial activity of KLRE, giving an important contribution to the current knowledge on the biological activities of this plant.