Che Puteh Osman

This contribution provides a comprehensive review of the biologically active compounds present in 21 high-value medicinal and aromatic plant species from Malaysia, with a particular focus on their phytochemical diversity and biological activities. Several plants, including well-known species such as Eurycoma longifolia, Andrographis paniculata, Morinda citrifolia, Centella asiatica, and Moringa oleifera, have been designated as high-priority herbal products under Malaysia’s National Key Economic Area (NKEA) in the Eleventh Malaysia Plan (RMK-11). Their significance extends beyond traditional uses in herbal medicine, as they are being recognized increasingly for their potential to contribute to the national economy and modern healthcare solutions. The compilation provided describes the pharmacological properties of these plants, highlighting their anti-inflammatory, antioxidant, antimicrobial, and cytotoxic activities, among others. Additionally, the aromatic plants Clinacanthus nutans, Cananga odorata, Citrus hystrix, and Polygonum minus are included in terms of their bioactive compounds produced and their potential therapeutic and industrial applications. By highlighting the relevant current research, this compilation aims to provide valuable insight for researchers, policymakers, and industry stakeholders, in terms of enhancing the understanding of both the therapeutic potential of these plants and their possible future contributions to healthcare and sustainable economic development.

Context: Andrographis paniculata has been used as a traditional medicine to treat malaria. The ethyl acetate fraction of A. paniculata containing diterpene lactone compounds was developed into a tablet dosage form, AS201-01. Aims: To determine the antimalarial activity and toxicity of AS201-01 to guarantee its efficacy and safety. Methods: Antimalarial assay in male Balb/c mice based on Peter’s four-day suppressive test at a dose of 6.25, 12.5, 25, and 50 mg/kg BW and 10 mg/kg BW of chloroquine as a positive control. In acute toxicity, AS201-01 was administered orally at a dose of 5, 50, 200, and 2,000 mg/kg BW in male rats (Wistar rats) and observed for 14 days to identify signs of toxicity and mortality. Meanwhile, AS201-01 was administered at 50, 327, and 1,000 mg/kg BW per day for 28 days in male and female rats to assess subchronic toxicity. Results: AS201-01 has antimalarial activity and exhibited the highest suppressive effect at 50 mg/kg BW dose with inhibition of 73.48%. Meanwhile, chloroquine at 10 mg/kg BW has an inhibition of 97.94%. AS201-01 was highly active as an antimalarial with an ED50 value of 5.95 mg/kg BW and increased survival time. Administration of AS201-01 is relatively safe in acute and subchronic toxicity studies. No clinical signs and mortality were observed in either study. The 50% lethal dose (LD50) was above 2,000 mg/kg BW. Conclusions: AS201-01 is effective as an antimalarial and non-toxic when administered orally at an equivalent therapeutic dose in an animal model.

Aims: To investigate the potential antimalarial plant belonging to the Artocarpus genus, Artocarpus sericicarpus, and isolate the antimalarial active compound from leaves extract. Methods: The isolation of the antimalarial compound was based on bioassay-guided isolation. The compound isolation was conducted by chromatography and identified using spectroscopic techniques, including 1H, 13C, and 2D NMR. The compound was tested for its antimalarial activity against Plasmodium falciparum and evaluated for cytotoxicity using several cell lines, including Huh7, HepG2, BHK-21, and Vero cells. In silico investigation of the compound against falcipain-2 protein was conducted as well. Results: Fractionation and purification of dichloromethane leaves extract led to the isolation of a dihydrochalcone compound identified as 1-(2,4-dihydroxyphenyl)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]propan-1-one. The dihydrochalcone compound exhibited antimalarial activity with an IC50 value of 34.80 µM. Cytotoxicity test revealed CC50 values of the compound were more than 20 µg/mL, and the selectivity indexes (SI) were 4.50, 5.52, 3.02, and 6.68 on Huh7, HepG2, BHK-21, and Vero cells, respectively. The CC50 and SI indicated the nontoxic criteria of the compound. In silico investigation showed that the compound could bind to the falcipain-2 active sites. Conclusions: The dihydrochalcone compound identified as 1-(2,4-dihydroxyphenyl)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]propan-1-one was isolated from Artocarpus sericicarpus leaves extract showed antimalarial activity and the ability to bind to the falcipain-2 active sites on in silico investigation.

α-guaiene is one of the primary sesquiterpene compounds used as a flavor and fragrance agent in patchouli oil. The fraction of patchouli oil that is rich in α-guaiene has been successfully isolated. In the present work, α-guaiene was isolated from crude patchouli oil through vacuum fractional distillation followed by GC-MS identification. Three important process parameters—feed volume, reflux ratio, and applied run pressure—were investigated and optimized using Box–Behnken design. The research methodology was an experimental laboratory using response surface methodology (RSM) with a feed volume level from 75 mL to 125 mL, a reflux ratio from 10:1 to 30:1, and an applied run pressure from 5 mmHg to 15 mmHg. The α-guaiene-enriched fraction was found in the first distillate fraction patchouli. The optimum condition that generated α-guaiene fraction at 44.70% purity was the treatment with a feed volume of 75 mL, a reflux ratio of 24:1, and applied run pressure of 14.80 mmHg. Results indicated that feed volume did not significantly affect the α-guaiene content, while the applied run pressure and reflux ratio used had a significant effect. A quadratic mathematical model with R² 0.861 and validation 96.14% was suitable for predicting the optimum α-guaiene fraction content during the vacuum fractional distillation process.

Steroidal alkaloids are derived from the steroid skeleton with one or two nitrogen atoms. They are widely distributed in tropical and subtropical regions and possess a range of biological activities. The structures of steroidal alkaloids are comparable to those of anabolic steroids, steroidal hormones, and corticosteroids, making them a valuable source for drug discovery. Taxonomically, steroidal alkaloids are limited in distribution to certain plant families, predominantly the Apocynaceae, Buxaceae, Solanaceae, and Liliaceae. This review highlights the steroidal alkaloids from the Apocynaceae family and their biological activities. The articles published from 1919 to 2021 were included in this review. A total of 163 steroidal alkaloids and 12 biological activities were reported from plant species belonging to the Apocynaceae family in this period. Of the 410 genera in the Apocynaceae, only 10 contain steroidal alkaloids. Although some alkaloids from the Apocynaceae family were also reported in the Buxaceae family, especially tetracyclic triterpenes with a pregnane side chain, most steroidal alkaloids can only be found in several genera of the Apocynaceae family.