Frutescone O from Baeckea frutescens Blocked TLR4-Mediated Myd88/NF-κB and MAPK Signaling Pathways in LPS Induced RAW264.7 Macrophages

Frutescone O was isolated from the aerial parts of Baeckea frutescens L., which was commonly used as a folk medicinal material for treating anti-inflammatory disease in South East Asia. This study aimed to investigate the anti-inflammatory activity and related signaling cascade of Frutescone O (Fru) in LPS induced RAW264.7 cells. The anti-inflammation activity of Frutescone O was determined according to the inhibitory effects on the secretion of nitric oxide (NO), expression of inducible NO synthase, and pro-inflammatory cytokines. The regulation of Myeloid differentiation factor 88 (Myd88), inhibition of NF-κB, and MAPK pathways were further investigated for molecular mechanisms. Fru significantly decreased the expression of iNOS and the production of NO in LPS-stimulated RAW264.7 cells. It also dose-dependently suppressed LPS induced expression of IL-1β, IL-6, and TNF-α. Furthermore, Fru remarkably inhibited the upregulation of NF-κB (p50) expression in the nucleus and the phosphorylation ratio of p38, JNK, ERK, and Myd88 signaling protein. The molecular docking and cellular thermal shift assay (CETSA) results indicated that Fru participated in a robust and stable interaction with the active site of TLR4-MD2. Thus, Fru suppressed the LPS induced inflammation in RAW264.7 cells by blocking the TLR4 mediated signal transduction through the NF-κB and MAPK signaling pathways and inhibiting the Myd88 and iNOS expression.

Skrining Fitokimia dan Penetapan Kandungan Total Fenolik Ekstrak Daun Tumbuhan Sapu-Sapu (Baeckea frutescens L.)

Tumbuhan sapu-sapu (Baeckea frutescens L.) merupakan salah satu jenis keanekaragaman hayati yang tumbuh dan persebarannya cukup banyak di Indonesia. B. frutescens L diketahui memiliki senyawa metabolit sekunder aktif yang dapat dimanfaatkan sebagai obat, antibakteri, dan antioksidan. Penelitian ini dilakukan untuk menganalisis kandungan senyawa metabolit sekunder yang terdapat pada B. frutescens L. Metode yang digunakan adalah ekstraksi dilanjutkan dengan pengujian fitokimia kualitatif yang terdiri dari tujuh pengujian yakni uji fenol, tanin, flavonoid, saponin, alkaloid, steroid dan terpenoid serta pengujian kuantitatif yakni pengujian total fenolik ekstrak B. frutescens L. Hasil penelitian menunjukkan bahwa didapatkan persentase bobot rendemen ekstrak daun B. frutescens L. sebesar ekstrak n-heksan 5,39%, ekstrak etil asetat 14,54% dan ekstrak etanol yakni 19,81%. Hasil pengujian fitokimia kualitatif menujukkan senyawa fitokimia yang terkandung di dalam tumbuhan B. frutescens L. yakni pada ekstrak n-heksan hanya terdapat senyawa steroid dan pada ekstrak etil asetat terdapat senyawa fenolik, tanin, flavonoid, dan alkaloid. Selain itu, pada ekstrak etanol terdapat senyawa fenolik, tanin, flavonoid, saponin, steroid, dan alkaloid. Pengujian total fenolik ekstrak daun tumbuhan B. frutescens L. untuk pelarut etil asetat yakni 0,24% dan pelarut etanol yakni sebesar 0,14% dihitung terhadap senyawa fenol asam galat. Hasil penelitian ini diharapkan dapat menjadi informasi untuk penelitian lebih lanjut mengenai pemanfaatan kandungan metabolit sekunder B. frutescens L.

Checklist of vascular plants of Klang Gates Quartz Ridge, Malaysia, a 14-km long quartz dyke

The Klang Gates Quartz Ridge (KGQR) is proposed for protection as National Heritage and as a UNESCO World Heritage Site because of its spectacular size, exceptional beauty and significant biodiversity. The checklist of vascular plants documents 314 species that comprise a unique combination that grows on lowland quartz and that is distinct from the surrounding lowland equatorial rain forest by the absence of orchids, palms, gingers and tree canopy families. The Rubiaceae, Gramineae, Moraceae, Apocynaceae, Melastomataceae and Polypodiaceae are the most speciose families. The summit vegetation at 200–400 m elevation is dominated by Baeckea frutescens (Myrtaceae) and Rhodoleia championii (Hamamelidaceae) and shows similarities to the plant community on rocky mountain peaks above 1500 m. About 11% of its species are endemic in Peninsular Malaysia and four are endemic to KGQR: Aleisanthia rupestris (Rubiaceae), Codonoboea primulina (Gesneriaceae), Spermacoce pilulifera (Rubiaceae), and Ilex praetermissa (Aquifoliaceae). All four are provisionally assessed as Critically Endangered. Two, Eulalia milsumi (Gramineae) and Sonerila prostrata (Melastomataceae), are endemic to KGQR and a few neighbouring smaller quartz dykes. They are assessed as Endangered. The KGQR is a fragile habitat and conservation management is urgently required to halt the spread of the aggressive alien grass, Pennisetum polystachion and to prevent further habitat degradation from visitors. Based on KGQR being a threatened habitat, its biodiverse flora, and endangered species, it qualifies as an Important Plant Area.

Chemical Composition of a Supercritical Fluid (Sfe-CO2) Extract from Baeckea frutescens L. Leaves and Its Bioactivity Against Two Pathogenic Fungi Isolated from the Tea Plant (Camellia sinensis (L.) O. Kuntze)

Colletotrichum gloeosporioides and Pseudopestalotiopsis camelliae-sinensis are the two most important tea plant (Camellia sinensis L.) pathogenic fungi. Interest in natural plant extracts as alternatives to synthetic chemical fungicides to control plant pathogens is growing. In this study, the volatile fraction of Baeckea frutescens L. was extracted by supercritical fluid extraction (SFE-CO2), and its chemical composition was analyzed, and investigated for its antifungal activity against C. gloeosporioides and P. camelliae. The major constituents of the volatile fraction were β-caryophyllene (28.05%), α-caryophyllene (24.02%), δ-cadinene (6.29%) and eucalyptol (5.46%) in B. frutescens SFE-CO2 extracts. The terpineol, linalool, terpinen-4-ol and eucalyptol showed strong contact antifungal activity against P. camelliae and C. gloeosporioides with median inhibitory concentration (MIC50) in the range of 0.69 μL/mL to 2.79 μL/mL and 0.62 μL/mL to 2.18 μL/mL, respectively. Additionally, the volatile fraction had high fumigation antifungal activity against P. camelliae and C. gloeosporioides with an inhibition rate between 20.87% and 92.91%. Terpineol presented the highest antifungal activity in the contact and fumigation toxicity assays. Terpineol, linalool, terpinen-4-ol and eucalyptol were associated with the most active chemical compounds in the volatile fraction against the fungi. The results suggest that B. frutescens SFE-CO2 extracts are potential ingredients to develop a natural fungicide for control of tea plant pathogens.

Chemical Composition of the Essential Oil Extracted from Baeckea frutescens L. Harvested in Hai Duong Province, Vietnam using GC-MS

Baeckea frutescens is a tropical plant with great medicinal potential. The oil of B. frutescens has high inhibitory, antibacterial and antifungal properties, especially against Staphylococcus aureus strains. The oil of B. frutescens has a spicy, bitter and warm properties that can cure aches and pains. In this study, the essential oils were obtained by hydrodistillation and the chemical analysis of B. frutescens essential oils was carried out using GC-MS. It was revealed that main components of leaf oil B. frutescens included 26 compounds such as tasmanone (21.46%), β-pinene (15.64%), 1,8-cineole (11.32%), α-thujene (8.74%), α-pinene (7.18%), linalool (7.44%), terpinen-4-ol (5.11%), α-terpineol (4.46%), γ-terpinene (3.37%), o-cymene (2.72%). The results open new directions in the application of compounds in B. frutescens essential oils to expand research and development of pharmaceutical, cosmetic and food industries.

The Cytotoxic Properties of Baeckea frutescens Branches Extracts in Eliminating Breast Cancer Cells

Breast cancer is the leading cause of cancer death in women in over 100 countries worldwide and accounts for almost 1 in 4 cancer cases among women. Baeckea frutescens of the family Myrtaceae has been used in traditional medicine and is known to possess antibacterial, antipyretic, and cytoprotective properties. In this study, we investigated the role of Baeckea frutescens branches extracts against human breast cancer cells. Baeckea frutescens branches extracts were prepared using Soxhlet apparatus with solvents of different polarity. The selective cytotoxic activity and the glucose consumption rate of Baeckea frutescens branches extracts of various concentrations (20 to 160 ug/ml) at 24-, 48-, and 72-hour time points were studied using MTT and glucose uptake assay. The IC50 values in human breast cancer (MCF-7 and MDA-MB-231) and mammary breast (MCF10A) cell lines were determined. Apoptotic study using AO/PI double staining was performed using fluorescent microscopy. The glucose uptake was measured using 2-NBDG, a fluorescent glucose analogue. The phytochemical screening of major secondary metabolites in plants was performed. This study reports that Baeckea frutescens branches extracts showed potent selective cytotoxic activity against MCF-7 cells compared to MDA-MB-231 cells after 72 hours of treatment. Evidence of early apoptosis which includes membrane blebbing and chromatin condensation was observed after 72 hours of treatment with Baeckea frutescens branches extracts. Interestingly, for the glucose uptake assay, the inhibition was observed as early as 24 hours upon treatment. All Baeckea frutescens extracts showed the presence of major secondary metabolites such as tannin, triterpenoid, flavonoid, and phenol. However, alkaloid level was unable to be determined. The identification of Baeckea frutescens and its possible role in selectively inhibiting glucose consumption in breast cancer cells defines a new role of natural product that can be utilised as an effective agent that regulates metabolic reprogramming in breast cancer.