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1.
J Ethnopharmacol ; 336: 118522, 2025 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-38971345

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Labisia pumila (Blume) Fern.-Vill, also known as Kacip Fatimah, is a traditional medicinal herb common throughout Southeast Asia. It is primarily used to facilitate childbirth and postpartum recovery in women. Additionally, it can also be used to treat dysentery, rheumatism, gonorrhea, and as an anti-flatulent. AIM OF THIS REVIEW: This article aims to provide a comprehensive review of the traditional uses, botany, cultivation, phytochemistry, pharmacological effects, practical applications, and potential uses of L. pumila (LP). Furthermore, we also explore the safety of this plant and its potential prospects for application. MATERIALS AND METHODS: The keywords "Labisia pumila," "Kacip Fatimah," and "Marantodes pumilum" were used to collect relevant information through electronic searches (including Elsevier, PubMed, Google Scholar, Baidu Scholar, CNKI, ScienceDirect, and Web of Science). RESULTS: This review summarizes 102 chemical components from different parts of the plant, including flavonoids, phenolic acids, saponins, and other chemical components. In addition, we also address the associated cultivation conditions, traditional uses, pharmacological effects and toxicity. A large number of reports indicate that LP has various pharmacological effects such as antioxidant, phytoestrogenic, anti-inflammtory, antimicrobial, anti-osteoporosis and anti-obesity properties. These results provide valuable references for future research on LP. In addition, LP is also a potential medicinal and edible plant, and is currently sold on the market as a dietary supplement. CONCLUSIONS: LP is a renowned traditional ethnic medicine with numerous pharmacological activities attributed to its bioactive components. Therefore, isolation and identification of the chemical components in LP can be a focus of our future research. Current studies have focused only on the effects of LP on estrogen deficiency-related diseases in women and bone diseases. There is no scientific evidence for other traditional uses. Therefore, it is important to further explore its pharmacological activities and fill the research gaps related to other traditional uses. Furthermore, research on its safety should be expanded to prepare clinical applications.


Asunto(s)
Etnofarmacología , Medicina Tradicional , Fitoquímicos , Extractos Vegetales , Humanos , Fitoquímicos/farmacología , Fitoquímicos/química , Medicina Tradicional/métodos , Etnofarmacología/métodos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Animales , Fitoterapia , Plantas Medicinales/química , Primulaceae/química
2.
BMC Complement Med Ther ; 24(1): 333, 2024 Sep 11.
Artículo en Inglés | MEDLINE | ID: mdl-39261916

RESUMEN

BACKGROUND: In early 2020, COVID-19 pandemic has mobilized researchers in finding new remedies including repurposing of medicinal plant products focusing on direct-acting antiviral and host-directed therapies. In this study, we performed an in vitro investigation on the standardized Marantodes pumilum extract (SKF7®) focusing on anti-SARS-CoV-2 and anti-inflammatory activities. METHODS: Anti-SARS-CoV-2 potential of the SKF7® was evaluated in SARS-CoV-2-infected Vero E6 cells and SARS-CoV-2-infected A549 cells by cytopathic effect-based assay and RT-qPCR, respectively. Target based assays were performed on the SKF7® against the S1-ACE2 interaction and 3CL protease activities. Anti-inflammatory activity of the SKF7® was evaluated by nitric oxide inhibitory and TLR2/TLR4 receptor blocker assays. RESULTS: The SKF7® inhibited wild-type Wuhan (EC50 of 21.99 µg/mL) and omicron (EC50 of 16.29 µg/mL) SARS-CoV-2 infections in Vero-E6 cells. The SKF7® also inhibited the wild-type SARS-CoV-2 infection in A549 cells (EC50 value of 6.31 µg/mL). The SKF7® prominently inhibited 3CL protease activity. The SKF7® inhibited the LPS induced-TLR4 response with the EC50 of 16.19 µg/mL. CONCLUSIONS: In conclusion, our in vitro study highlighted anti-SARS-CoV-2 and anti-inflammatory potentials of the SKF7®. Future pre-clinical in vivo studies focusing on antiviral and immunomodulatory potentials of the SKF7® in affecting the COVID-19 pathogenesis are warranted.


Asunto(s)
Antivirales , Extractos Vegetales , SARS-CoV-2 , Animales , Humanos , Antivirales/farmacología , SARS-CoV-2/efectos de los fármacos , Células Vero , Chlorocebus aethiops , Extractos Vegetales/farmacología , Células A549 , Plantas Medicinales/química , Tratamiento Farmacológico de COVID-19 , Antiinflamatorios/farmacología , Malasia , COVID-19 , Proteasas 3C de Coronavirus
3.
Life (Basel) ; 14(2)2024 Feb 18.
Artículo en Inglés | MEDLINE | ID: mdl-38398785

RESUMEN

BACKGROUND: Lung cancer is the predominant cause of cancer-related fatalities. This prompted our exploration into the anti-lung cancer efficacy of Labisia pumila, a species meticulously selected from the preliminary screening of 600 plants. METHODS: Through the strategic implementation of activity-guided fractionation, ardisiacrispin A (1) was isolated utilizing sequential column chromatography. Structural characterization was achieved employing various spectroscopic methods, including nuclear magnetic resonance (NMR), mass spectrometry (MS), and infrared spectroscopy (IR). RESULTS: L. pumila 70% EtOH extract showed significant toxicity in A549 lung cancer cells, with an IC50 value of 57.04 ± 10.28 µg/mL, as well as decreased expression of oncogenes and induced apoptosis. Compound 1, ardisiacrispin A, induced a 50% cell death response in A549 cells at a concentration of 11.94 ± 1.14 µg/mL. CONCLUSIONS: The present study successfully investigated ardisiacrispin A extracted from L. pumila leaves, employing a comprehensive spectroscopic approach encompassing NMR, IR, and MS analyses. The anti-lung cancer efficacy of ardisiacrispin A and L. pumila extract was successfully demonstrated for the first time, to the best of our knowledge.

4.
Data Brief ; 51: 109644, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37840993

RESUMEN

The article presents data on the quantification of gallic acid (GA) and the assessment of the antioxidant and anti-inflammatory properties of Kacip Fatimah (Labisia pumila Benth. & Hook. f.) leaves using various solvents. GA was quantified using high-performance liquid chromatography analysis. Total phenolic content (TPC) was assessed using the Folin-Ciocalteu method. The antioxidant activities were evaluated using xanthine oxidase superoxide (XOD-Superoxide) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays, while anti-inflammatory activities were examined through lipoxygenase (LOX) and xanthine oxidase (XOD) inhibition assays. Results showed that the water-extracted sample had the highest GA and TPC among the solvents tested, along with the strongest inhibition activities in the XOD-Superoxide and DPPH assays. Both water and ethanol extracts showed significant inhibitory activities in the LOX assay but were inactive in the XOD assay. These findings suggest that the bioactivity of L. pumila leaf extract is associated with GA and TPC. GA and TPC strongly correlated with antioxidant and anti-inflammatory activities, except for the XOD assay. The dataset highlights the potential dietary benefits of L. pumila leaves as a natural source of antioxidants and anti-inflammatory properties for pharmaceutical and nutraceutical applications.

5.
EFSA J ; 20(11): e07611, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36381124

RESUMEN

Following a request from the European Commission, the EFSA Panel on Nutrition, Novel Foods and Food Allergens (NDA) was asked to deliver an opinion on aqueous extract of Labisia pumila as a novel food (NF) pursuant to Regulation (EU) 2015/2283. The NF is a standardised hydroalcoholic extract from a dried whole plant (including roots) of L. pumila, mixed with maltodextrin (as a drying aid), and proposed by the applicant to be used as a food supplement in amounts up to 750 mg/day. The target population is the general adult population, except pregnant and lactating women. The major constituents of this NF are carbohydrates (up to 85.5%), with a smaller amount of proteins (up to 6.5%), gallic acid (up to 3.7%) and fats (up to 1.6%). The Panel considers that taking into account the composition of the NF and the proposed conditions of use, consumption of the NF is not nutritionally disadvantageous. The provided genotoxicity studies do not raise concerns about the genotoxicity of the NF. Based on the available toxicological data, the Panel considers an intake of up to 5 mg/kg body weight per day as safe. For the target population, this level corresponds to 350 mg/day, which is lower than the use level proposed by the applicant. The Panel concludes that the NF is safe for the target population up to 350 mg/day.

6.
Front Pharmacol ; 13: 968664, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36313379

RESUMEN

Background: Burns are considered a critical care problem in emergency medicine, resulting in physical, psychological, and chronic disabilities. Silver sulfadiazine is the gold standard in topical burn treatment but was associated with toxicity to keratinocytes and fibroblasts, which may delay wound healing. In discovering potential alternative treatments for burn wound healing, this study was performed to determine the effect of Labisia Pumila (Blume) Fern.-Vill. Var. Alata (LPVa) extract on thermal-burn wounds in rats. Methods: A total of 50 Sprague-Dawley male rats were categorized into five groups. There were three control groups; normal control (left untreated), negative control (given ointment base) and positive control (given silver sulfadiazine). Meanwhile, the two intervention groups were given with 2% LPVa leaf and root extracts, respectively. Burn wounds were inflicted on the loin region of the rat by applying a heated steel rod at 80°C for 10 s. On days 3, 7, 14, and 21, wounds were measured macroscopically using a digital calliper and one animals of each group were sacrificed, and the wounded skin were excised for histomorphological assessments. The wounds were excised for hydroxyproline content on Day 14 of treatment. Result: For wound contraction percentage, both the leaf and root extracts of LPVa showed a significant reduction in burn wound size on Day 7 onwards, when compared to other groups. For hydroxyproline content, only the leaf extract of LPVa produced significantly higher content compared to both negative and normal control groups. In terms of histological examination, the leaf extract group demonstrated a superior healing effect than the root extract group. Conclusion: Both leaf and root extracts of LPVa could promote wound healing in the thermal-burn wound rat model, with leaf extract being superior to root extract.

7.
J Diabetes Metab Disord ; 21(1): 1-11, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35673507

RESUMEN

Purpose: Diabetes accelerates peripheral, distal symmetric polyneuropathy, small fiber predominant neuropathy, radiculoplexopathy, and autonomic neuropathy. This study investigated the neuroprotective effects of gallic acid and myricetin-rich Labisia pumila extract in a diabetic neuropathy rat model and evaluated the neuropathy correlationship with serum inflammatory biomarkers. Methods: Thirty male rats were divided into 5 groups (n = 6), namely: healthy control; non-treated diabetic control; and diabetic-rats treated with 200 mg/kg metformin; Labisia pumila ethanol extract (LP) at 150 mg/kg or 300 mg/kg doses. Diabetes was induced by 60 mg streptozotocin /kg intraperitoneal injection. Rats were orally treated daily for ten weeks. Their fasting blood glucose (FBG), neurological functions (hot plate and tail immersion; thermal hyperalgesia; cold allodynia; motor walking function), biomarkers for inflammation and oxidative stress, the neuro-histopathological changes, and brain somatic index were measured. Results: The extract significantly prevented abnormal increases in FBG and decreases in body weight gain. It attenuated behavioral dysfunctions (hot plate and tail immersion; thermal hyperalgesia; cold allodynia; motor walking function), systemic inflammation (serum TNF-α, prostaglandin-E2) oxidative tension (malondialdehyde), histological brain and sciatic nerve injuries in the diabetic-rats, better than Metformin. Conclusion: LP mitigated neural dysfunction better than metformin partly by amending diabetic systemic inflammation, oxidative tension, and diabetic abnormalities. The nerve injuries were strongly correlated to serum prostaglandin-E2, TNF-α levels, and walking functions. The motor function was correlated to sensory neuronal functions, inflammation, and oxidation. The sensory neuronal functions were more affected by TNF-α than prostaglandin-E2 or oxidation. Diabetic brain and sciatic nerve deteriorations were influenced by serum TNF-α, PGE2, and MDA levels. Supplementary Information: The online version contains supplementary material available at 10.1007/s40200-021-00905-0.

8.
Molecules ; 26(11)2021 May 27.
Artículo en Inglés | MEDLINE | ID: mdl-34072168

RESUMEN

This study aims to investigate whether the in vitro-cultured L. pumila var. alata has higher antioxidant activity than its wild plant. An 8-week-old L. pumila var. alata nodal segment and leaf explants were cultured onto Murashige and Skoog (MS) medium supplemented with various cytokinins (zeatin, kinetin, and 6-benzylaminopurine (BAP)) for shoot multiplication and auxins (2,4-dichlorophenoxyacetic acid (2,4-D) and picloram) for callus induction, respectively. The results showed that 2 mg/L zeatin produced the optimal results for shoot and leaf development, and 0.5 mg/L 2,4-D produced the highest callus induction results (60%). After this, 0.5 mg/L 2,4-D was combined with 0.25 mg/L cytokinins and supplemented to the MS medium. The optimal results for callus induction (100%) with yellowish to greenish and compact texture were obtained using 0.5 mg/L 2,4-D combined with 0.25 mg/L zeatin. Leaves obtained from in vitro plantlets and wild plants as well as callus were extracted and analyzed for their antioxidant activities (DPPH and FRAP methods) and polyphenolic properties (total flavonoid and total phenolic content). When compared with leaf extracts of in vitro plantlets and wild plants of L. pumila var. alata, the callus extract displayed significantly higher antioxidant activities and total phenolic and flavonoid content. Hence, callus culture potentially can be adapted for antioxidant and polyphenolic production to satisfy pharmaceutical and nutraceutical needs while conserving wild L. pumila var. alata.


Asunto(s)
Callo Óseo/efectos de los fármacos , Reguladores del Crecimiento de las Plantas/metabolismo , Brotes de la Planta/efectos de los fármacos , Polifenoles/química , Primulaceae/efectos de los fármacos , Ácido 2,4-Diclorofenoxiacético/química , Antioxidantes/química , Compuestos de Bencilo/química , Compuestos de Bifenilo/química , Medios de Cultivo , Suplementos Dietéticos , Flavonoides/química , Técnicas In Vitro , Cinetina/química , Fenol/química , Picloram/química , Picratos/química , Hojas de la Planta , Proteínas de Plantas , Raíces de Plantas/efectos de los fármacos , Plantas/efectos de los fármacos , Purinas/química , Zeatina/química
9.
Plants (Basel) ; 10(4)2021 Apr 07.
Artículo en Inglés | MEDLINE | ID: mdl-33917172

RESUMEN

Labisia pumila is a precious herb in Southeast Asia that is traditionally used as a health supplement and has been extensively commercialized due to its claimed therapeutic properties in boosting a healthy female reproductive system. Indigenous people used these plants by boiling the leaves; however, in recent years it has been marketed as powdered or capsuled products. Accordingly, accuracy in determination of the authenticity of these modern herbal products has faced great challenges. Lack of authenticity is a public health risk because incorrectly used herbal species can cause adverse effects. Hence, any measures that may aid product authentication would be beneficial. Given the widespread use of Labisia herbal products, the current study focuses on authenticity testing via an integral approach of DNA barcoding and qualitative analysis using HPLC. This study successfully generated DNA reference barcodes (ITS2 and rbcL) for L. pumila var. alata and pumila. The DNA barcode that was generated was then used to identify species of Labisia pumila in herbal medicinal products, while HPLC was utilized to determine their quality. The findings through the synergistic approach (DNA barcode and HPLC) implemented in this study indicate the importance of both methods in providing the strong evidence required for the identification of true species and to examine the authenticity of such herbal medicinal products.

10.
Pharmaceuticals (Basel) ; 14(2)2021 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-33579048

RESUMEN

A combined polyherbal formulation containing tongkat ali (Eurycoma longifolia) and kacip fatimah (Labisia pumila) aqueous extracts was evaluated for its safety aspect. A repeated dose 28-day toxicity study using Wistar rats was conducted where the polyherbal formulation was administered at doses 125, 500 and 2000 mg/kg body weight to male and female treatment groups daily via oral gavage, with rats receiving only water as the control group. In-life parameters measured include monitoring of food and water consumption and clinical and functional observations. On day 29, blood was collected for haematological and biochemical analysis. The rats were necropsied and the organs were collected for histopathological examination. This study showed that the combined formulation did not induce any significant toxicity effect at any dose level in terms of morbidity, mortality, behaviour, functional observation, body weight, food and water consumption, whole blood haematology and serum biochemistry. However, there were some microscopic changes in the histopathological examinations of some organs given 2000 mg/kg body weight, which may suggest an early response to the polyherbal formulation. From this study, the no observed adverse effect level is estimated to be more than 500 mg/kg body weight but not exceeding 2000 mg/kg body weight. The observed effects at the highest dose indicate the need for further study of longer dosing duration.

11.
Food Nutr Res ; 642020.
Artículo en Inglés | MEDLINE | ID: mdl-33061884

RESUMEN

BACKGROUND: Interest in herbal medicines and non-hormonal therapies for the treatment of menopausal symptoms has increased since the publication of adverse effects of estrogen replacement therapy. Vasomotor symptoms are the most characteristic and notable symptoms of menopause. OBJECTIVE: To investigate the changes in the frequency and severity of hot flush and associated vasomotor symptoms experienced by peri-menopausal and menopausal women supplemented with the herbal formulation (Nu-femme™) comprising Labisia pumila (SLP+®) and Eurycoma longifolia (Physta®) or placebo. DESIGN: Randomised, double-blind, placebo-controlled, 24-week study enrolled 119 healthy women aged 41-55 years experiencing peri-menopausal or menopausal symptoms and supplemented with Nu-femme™ or placebo. The primary endpoint was comparative changes between treatment groups in the change in the frequency and severity of hot flushes. The secondary objectives were to assess the changes in the frequency and severity of joint pain, Menopause Rating Scale (MRS) and Menopause-Specific Quality of Life (MENQOL) questionnaire domain scores. Concentrations of serum hormone, lipid profile, bone markers, sleep quality and vitality were also studied as secondary objectives. RESULTS: At week 12, significant (P < 0.01) improvements in hot flush symptoms were observed in Nu-femme™ and placebo groups. Even though there was no significant difference between groups, higher percentage of improvement, 65%, was seen in Nu-femme™ compared to 60% in placebo. Significant improvements (P < 0.001) in MRS and MENQOL scores at weeks 12 and 24 were observed in both groups, respectively. Luteinising hormone and follicle-stimulating hormone levels were significantly reduced (P < 0.05) at weeks 12 and 24, respectively, compared to baseline in the Nu-femme™ group, with no significant changes observed in the placebo group. There were significant (P < 0.05) reductions in serum low-density lipid and triglycerides levels at week 12 in Nu-femme™ group, but no changes seen in placebo group. At the end of week 24, changes in haematology and clinical chemistry parameters remained within normal clinical ranges in both groups. CONCLUSION: Herbal formulation consists of L. pumila and E. longifolia (Nu-femme™) may support reduction in hot flushes and improvements in hormone and lipid profile in healthy peri-menopausal and menopausal women.

12.
Front Pharmacol ; 11: 289, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32256360

RESUMEN

Marantodes pumilum (Primulaceae) has been used in Malaysian folk medicine to help women regain strength after delivery and for "sickness in the bones." It was previously revealed that its extracts inhibited xanthine oxidase (XO) activity in vitro. The leaves and roots of M. pumilum var. alata (MPA), var. pumila (MPP), and var. lanceolata (MPL) were individually extracted in ethanol (80%). The anti-hyperuricemic activity was initially assessed by XO inhibition with a spectrophotometric in vitro assay. The most active extract was further investigated on hyperuricemic rat model induced by potassium oxonate to determine serum uric acid levels and liver XO effect. The in vitro anti-inflammatory activity was carried out on monosodium urate (MSU) crystal-induced pro-inflammatory cytokines (i.e., interleukin (IL)1α, IL-1ß, IL-6, IL-8, and tumor necrosis factor (TNF)-α) secretion using human peripheral blood mononuclear cells and ELISA technique, and prostaglandin E2 (PGE2)secretion using radioimmunoassay. The active extract was then investigated on gout-induced inflammation with MSU crystals to determine pro-inflammatory cytokines and PGE2 secretion levels in the synovial fluid of rat knee joint. Quantitative analysis using validated HPLC was performed on the extracts to determine presence of bioactive flavonoids. The findings revealed that extract of MPP leaves gave the highest inhibitory activity on XO (IC50 130.5 µg/mL) compared to other extracts tested. However, all extracts possessed significantly lower activity compared to allopurinol (IC50 0.13 µg/mL). Oral administration of MPP leaf extract (200 mg/kg) significantly reduced serum uric acid level in hyperuricemic rats in time-dependent manner to the baseline level and it was as effective as allopurinol (5 mg/kg). The extract also inhibited liver XO activity (25%) compared to allopurinol (45%). In vitro anti-inflammatory assay showed that extract of MPP roots inhibited MSU crystals-induced secretion of IL-1α, IL-1ß, IL-8, TNF-α, and PGE2 with IC50 values of 36, 25, 38, 18, and 46 µg/mL, respectively. Oral administration of the MPP root extract (200 mg/kg) significantly decreased IL-1α, IL-1ß, IL-6, TNF-α, and PGE2 levels in rat's synovial fluid as effective as indomethacin. There were no significant body weight changes of all experimental animals. MPP extracts showed presence of myricetin, quercetin and kaempferol. Myricetin was detected with values of 0.2 and 0.6 mg/g for root and leaf extracts, respectively. The anti-hyperuricemic of MPP leaf and anti-inflammatory of MPP root indicated that MPP may be promising for complementary therapy of gout.

13.
Asian Pac J Cancer Prev ; 21(4): 943-951, 2020 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-32334454

RESUMEN

BACKGROUND: Uterine fibroids are a common type of solid tumor presenting in women of reproductive age. There are very few alternative treatment available from conventional treatment involving surgeries. Labisia pumila var. alata or locally known as 'Kacip Fatimah' was widely used as traditional medicine in Malaysia. This plant has been used to maintain a healthy female reproductive system. The present study aimed to evaluate anti fibroid potential of L. pumila extracts through in vitro apoptosis activity against uterine leiomyoma cells (SK-UT-1) and in uterine leiomyoma xenograft model. Evaluation of bioactive markers content were also carried out. METHODS: Apoptotic induction of the extracts was determined by morphological examination of AO/PI dual staining assay by flourescent microscopy and flow cytometry analysis on Annexin V-FITC/PI stained cells. In vivo study was done in immune-compromised mouse xenograft model. HPLC analysis was employed to quantify marker compounds. RESULTS: Morphological analysis showed L. pumila induced apoptosis in a dose dependent manner against SK-UT-1 cells. In vivo study indicated that L. pumila significantly suppressed the growth of uterine fibroid tumor. All tested extracts contain bioactive marker of gallic acid and cafeic acid. CONCLUSION: This work provide significant data of the potential of L. pumila in management of uterine fibroids.
.


Asunto(s)
Antineoplásicos/farmacología , Leiomioma/tratamiento farmacológico , Extractos Vegetales/farmacología , Primulaceae/química , Neoplasias Uterinas/tratamiento farmacológico , Animales , Apoptosis , Proliferación Celular , Femenino , Humanos , Técnicas In Vitro , Leiomioma/patología , Ratones , Ratones Desnudos , Células Tumorales Cultivadas , Neoplasias Uterinas/patología , Ensayos Antitumor por Modelo de Xenoinjerto
14.
Int J Cardiol Hypertens ; 4: 100024, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-33447753

RESUMEN

INTRODUCTION: Labisia pumila has been reported to possess activities including antioxidant, anti-aging and anti-cancer but there is no report on its vasorelaxant effects. OBJECTIVE: This study aims to fractionate water extract of Labisia pumila, identify the compound(s) involved and elucidate the possible mechanism(s) of its vasorelaxant effects. METHODS: Water extract of Labisia pumila was subjected to liquid-liquid extraction to obtain ethyl acetate, n-butanol and water fractions. In SHR aortic ring preparations, water fraction (WF-LPWE) was established as the most potent fraction for vasorelaxation. The pharmacological mechanisms of the vasorelaxant effect of WF-LPWE were investigated with and without the presence of various inhibitors. The cumulative dose-response curves of potassium chloride (KCl)-induced contractions were conducted to study the possible mechanisms of WF-LPWE in reducing vasoconstriction. RESULTS: WF-LPWE produced dose-dependent vasorelaxant effect in endothelium-denuded aortic ring and showed non-competitive inhibition of dose-response curves of PE-induced contraction, and at its higher concentrations reduced KCl-induced contraction. 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) significantly inhibited vasorelaxant effect of WF-LPWE. WF-LPWE significantly reduced the release of intracellular calcium ion (Ca2+) from the intracellular stores and suppressed the calcium chloride (CaCal2)-induced contraction. Nω-nitro-L-arginine methyl ester (L-NAME), methylene blue, indomethacin and atropine did not influence the vasorelaxant effects of WF-LPWE. CONCLUSION: WF-LPWE exerts its vasorelaxant effect independently of endothelium and possibly by inhibiting the release of calcium from intracellular calcium stores, receptor-operated calcium channels and formation of inositol 1,4,5- triphosphate. WF-LPWE vasorelaxant effect may also mediated via nitric oxide-independent direct involvement of soluble guanylate cyclase (sGC)/ cyclic guanosine monophosphate (cGMP) pathways.

15.
Fitoterapia ; 137: 104256, 2019 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-31295513

RESUMEN

Labisia pumila var. alata (Myrsinaceae) or "Kacip fatimah" is a famous Malay traditional herb used for the maintenance of women's health. The extracts of L.pumila displayed estrogenic activity in rats. Nonetheless, the estrogenic bioactives were not identified. The aim of the study is to identify estrogenic compounds contributing to the established estrogenic activity. Bioactivity-guided-isolation method guided the isolation of pure bioactives. The hexane extract was subjected to a series of silica gel flash and open column chromatography with increasing amount of ethyl acetate in hexane or methanol in chloroform. Each fraction or pure compounds were evaluated on it's estrogen receptor (ER) binding activity with the fluorescence polarization competitive ERα and ERß binding assay kit. Cytotoxic assay using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method was used to establish the cytotoxic activity of the compounds. Four alkyl resorcinols and a dimeric 1,4-benzoquinone, namely belamcandol B (1), 5-pentadec-10'-(Z)-enyl resorcinol (2), 1,3-dihydroxy-5-pentadecylbenzene (3), 5-(heptadec-12'-(Z)-enyl) resorcinol (4) and demethylbelamcandaquinone B (5) were identified with selective binding affinities towards either ERα or ERß exhibiting selectivity ratio from 0.15-11.9. Alkyl resorcinols (2)-(4) exhibited cytotoxic activity towards HL60 cells with IC50 values from 19.5-22.0 µM. Structural differences between compounds influence the binding affinities to ER subtypes. Further study is needed to establish the agonist or antagonist effect of these compounds on various tissues and to identify if these compounds exert cytotoxic activity through the ERs. When consuming L.pumila as a complementary medicine, careful consideration regarding it's estrogenic compound content should be given due consideration.


Asunto(s)
Receptor alfa de Estrógeno/efectos de los fármacos , Receptor beta de Estrógeno/efectos de los fármacos , Estrógenos/farmacología , Primulaceae/química , Benzoquinonas/aislamiento & purificación , Benzoquinonas/farmacología , Estrógenos/aislamiento & purificación , Células HL-60 , Humanos , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Resorcinoles/aislamiento & purificación , Resorcinoles/farmacología
16.
Inflammopharmacology ; 26(5): 1207-1217, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29460078

RESUMEN

The tropical herb Labisia pumila is traditionally used in facilitating childbirth and post-partum care. The effects of L. pumila leaf extract (LP) in explant cartilage culture and on postmenopausal osteoarthritis (OA) rat model were assessed. The LP (10, 25 and 50 µg/ml) or diclofenac (10 µg/ml) was added to the cartilage explants containing bovine IL-1ß (20 ng/ml), to evaluate their direct effects on cartilage degradation. In the preclinical study, rats were grouped (n = 8) into: non-treated OA; OA + diclofenac (5 mg/kg); OA + LP extract (150 and 300 mg/kg); and healthy control. To induce OA, monosodium iodoacetate was injected into the ovariectomised female rats' intra-articular knee joints and evaluated for OA severity after 8 weeks via physical (radiological, macroscopic and histological observations), biochemical, ELISA and mRNA expression analysis (for inflammation and cartilage degradation biomarkers). The LP reduced the nitric oxide and proteoglycan release from the cartilage explants under IL-1ß induction. The radiological, macroscopic, microscopic and histological images showed the OA rats treated with LP and diclofenac had significantly reduced osteophytes and cartilage erosions compared to non-treated OA rats. The extract significantly up-regulated the anti-inflammatory interleukin-10, collagen type II and down-regulated pro-inflammatory PTGS2 (prostaglandin-endoperoxide synthase 2) mRNA expressions compared to non-treated control. The LP treatment significantly reduced serum collagenases (MMP-1 and MMP-3) and collagen type II degradation biomarker (CTX-II) levels in OA rats. The LP containing myricetin and gallic acid suppressed inflammation, collagenases and cartilage degradation, and helped cartilage matrix synthesis, to prevent OA at the dose equivalent to 30-60 mg/kg daily for humans.


Asunto(s)
Cartílago/efectos de los fármacos , Colágeno/metabolismo , Osteoartritis/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Primulaceae , Animales , Cartílago/metabolismo , Cromatografía Líquida de Alta Presión , Modelos Animales de Enfermedad , Femenino , Articulación de la Rodilla/diagnóstico por imagen , Metaloproteinasa 1 de la Matriz/metabolismo , Metaloproteinasa 3 de la Matriz/metabolismo , Osteoartritis/diagnóstico por imagen , Osteoartritis/patología , Extractos Vegetales/análisis , Primulaceae/química , Ratas , Ratas Sprague-Dawley , Microtomografía por Rayos X
17.
J Diet Suppl ; 14(2): 132-145, 2017 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-27487244

RESUMEN

The tableting properties of Labisia pumila herbal powder, which is well known for its therapeutic benefits was investigated. The herbal powder was compressed into tablets using a stainless steel cylindrical uniaxial die of 13-mm- diameter with compaction pressures ranging from 7 to 25 MPa. Two feed weights, 0.5 and 1.0 g were used to form tablets. Some empirical models were used to describe the compressibility behavior of Labisia pumila tablets. The strength and density of tablets increased with increase in compaction pressure and resulted in reduction in porosity of the tablets. Smaller feeds, higher forces and increase in compaction pressure, contributed to more coherent tablets. These findings can be used to enhance the approach and understanding of tableting properties of Labisia pumila herbal powder tablets.


Asunto(s)
Composición de Medicamentos/métodos , Polvos/química , Primulaceae/química , Comprimidos/química , Fuerza Compresiva , Porosidad
18.
J Xray Sci Technol ; 25(1): 101-112, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-27768005

RESUMEN

BACKGOUND: Labisia pumila (LP) is a popular herb used by women over the past few decades. This herb has shown potentials as an alternative agent for treatment and prevention of postmenopausal osteoporosis. It was observed in previous studies that supplementation to ovariectomized rats were associated with increased bone antioxidative enzymes and reduced lipid peroxidation activity. It had also improved bone formation markers in ovariectomized rats. This study aimed to evaluate the effects of giving different forms of LP extracts on the trabecular bone microarchitecture of ovariectomised rats. METHODS: Forty-eight female Sprague-Dawley rats were randomly divided into sham-operated (Sham), ovariectomized control (OVX), ovariectomized and given estrogen at 64.5 µg/kg (ERT), ovariectomized and given LP aqueous extract (LPaq), LP methanol extract (LPmet) and LP ethanol extract (LPet) at 100 mg/kg, respectively. Treatments were given daily via oral gavages for nine weeks. Following sacrifice, femora were dissected out for bone microarchitectural analysis using an in vitro micro-CT, which provided three dimensional informations on bone microarchitecture. RESULTS: LPaq was the most effective extract found to improve the bone microarchitectural paramaters which comprised ofBone volume fraction (BV/TV), Trabecular separation (Tb.Sp), Trabecular number (Tb.N), Connective density (Conn.dens), Structure model index (SMI) and Degree of anisotropy (DA). CONCLUSION: LPaq was effective in protecting the bone of postmenopausal osteoporosis rat model against microarchitectural deterioration.


Asunto(s)
Densidad Ósea/efectos de los fármacos , Fémur , Osteoporosis/patología , Extractos Vegetales/farmacología , Primulaceae , Animales , Modelos Animales de Enfermedad , Femenino , Fémur/diagnóstico por imagen , Fémur/efectos de los fármacos , Fémur/patología , Imagenología Tridimensional , Ovariectomía , Ratas , Ratas Sprague-Dawley , Microtomografía por Rayos X
19.
Phytomedicine ; 23(8): 810-7, 2016 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-27288916

RESUMEN

BACKGROUND: Previous studies on Labisia pumila var. alata (LPva) have showed that it could inhibit low-density lipoprotein (LDL) oxidation and provide protection on myocardial infarction in rats. HYPOTHESIS/PURPOSE: We hypothesized that LPva extracts can modulate the lipid profiles and serum antioxidant status of hypercholesterolemic rats. In the present study, we investigated the effects of aqueous and 80% ethanol extracts of LPva on atherogenic and serum antioxidant parameters as well as changes in abdominal aorta of high-cholesterol diet rats. METHODS: The major components of the extracts, gallic acid, flavonoids and alkyl resorcinols were analyzed by using a validated reversed phase HPLC method. The rats were induced to hypercholesterolemic status with daily intake of 2% cholesterol for a duration of 8 weeks. Three different doses (100, 200 and 400mg/kg) of the extracts were administered daily on the 4th week onwards. The rats were then sacrificed and the blood was collected via abdominal aorta and serum was separated by centrifugation for biochemical analysis. Part of the aorta tissues were excised immediately for histopathological examination. RESULTS: The serum of LPva treated rats showed significant reduction in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT) and lactate dehydrogenase (LDH) levels and the abdominal aorta showed a significant decrease of atheroma lesions in treated rats. Serum lipid profiles of treated rats showed a decrease in total cholesterol, total triglycerides and low-density lipoprotein (LDL) levels as compared to control group. The atherogenic indices in treated rats were significantly improved along with an increasing level of serum high-density lipoprotein (HDL). The extracts also exhibited significant increase of antioxidant enzymes and decrease of MDA as a product of lipid peroxidation. CONCLUSION: LPva extracts can reduce the risk of dyslipidemia by improving the serum lipid profiles and modulating serum antioxidants.


Asunto(s)
Antioxidantes/farmacología , Aorta Abdominal/efectos de los fármacos , Colesterol en la Dieta/efectos adversos , Hipolipemiantes/farmacología , Lípidos/sangre , Extractos Vegetales/farmacología , Primulaceae/química , Alanina Transaminasa/sangre , Animales , Aspartato Aminotransferasas/sangre , Aterosclerosis/prevención & control , Dieta , Relación Dosis-Respuesta a Droga , Dislipidemias/inducido químicamente , Dislipidemias/tratamiento farmacológico , L-Lactato Deshidrogenasa/sangre , Masculino , Ratas , Ratas Wistar
20.
Braz. arch. biol. technol ; 59: e16160062, 2016. tab, graf
Artículo en Inglés | LILACS | ID: biblio-951395

RESUMEN

ABSTRACT The anticancer potential of aqueous extracts of tropical plants Ficus deltoidea and Labisia pumila were tested on human prostate carcinoma (DU145) cells. The effects of these extracts on the cells were observed through several tests such as cytotoxicity MTT assay, trypan blue exclusion assay (for cell viability), fluorescence and morphological observations. Both of the plant extracts had a growth repression effect on the cells with different concentrations. The best concentration (1x10-3 μg/mL) was chosen by determining their cytotoxic effects on human prostate cancer as well as fibroblast (normal) cells. The F. deltoidea extract showed more potency and killed the cells faster than L. pumila. Morphologically both extracts affected the cells in a similar way, i.e. the cells became irregular shaped, detached themselves and kept floating in the medium.

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